首页 > 最新文献

Future Journal of Pharmaceutical Sciences最新文献

英文 中文
Novel paradigm of therapeutic intervention for skin cancer: challenges and opportunities 皮肤癌治疗干预的新模式:挑战与机遇
IF 3.4 Q2 PHARMACOLOGY & PHARMACY Pub Date : 2024-09-02 DOI: 10.1186/s43094-024-00686-2
Modassir Nasim, Mariya Khan, Rabea Parveen, Azka Gull, Saba Khan, Javed Ali

Background

Skin cancer continues to be an imperative global health issue, urging continuous exploration of treatment methodologies. Conventional treatments for skin cancer include surgical interventions, immunotherapy, targeted therapy, chemotherapy, and radiation therapy. However, these methods often present obstacles like treatment resistance, systemic toxicity, limited effectiveness in advanced stages, infection risk, pain, long recovery, and impact on healthy tissue.

Main body of the abstract

Nanomedicine holds promise by facilitating precise drug administration, early detection, and heightened therapeutic efficiency via targeted and localized delivery systems. The integration of nanomedicine into skin cancer alleviation therapies demonstrates optimistic outcomes, including refined drug delivery, augmented bioavailability, minimized adverse effects, and potential theranostic applications. Recent breakthroughs in nanomedicine have propelled advancements in skin cancer treatment, showing significant potential in transforming the treatment paradigm. The presents review provides comprehensive aspects of existing skin cancer treatments and their challenges, spotlighting recent breakthroughs propelled by nanomedicine.

Short conclusion

This abstract delineates the present landscape of skin cancer treatments, underscores their constraints, and highlights recent strides in nanomedicine that have the potential to transform the paradigm of skin cancer treatment, ultimately elevating patient prognosis. Importantly, the present review emphasizes substantial challenges that hinder the clinical translation of nanomedicines and suggests possible remedies to surpass them.

Graphic abstract

背景皮肤癌仍然是一个紧迫的全球健康问题,需要不断探索治疗方法。皮肤癌的传统治疗方法包括外科手术、免疫疗法、靶向疗法、化疗和放疗。然而,这些方法往往存在耐药性、全身毒性、晚期疗效有限、感染风险、疼痛、恢复期长以及对健康组织的影响等障碍。摘要正文纳米医学有望通过靶向和局部给药系统促进精确给药、早期检测和提高治疗效率。将纳米医学整合到皮肤癌缓解疗法中显示出乐观的结果,包括精细给药、提高生物利用度、减少不良反应以及潜在的治疗应用。纳米医学的最新突破推动了皮肤癌治疗的进步,显示出改变治疗模式的巨大潜力。本综述全面介绍了现有的皮肤癌治疗方法及其面临的挑战,并重点介绍了纳米医学最近取得的突破性进展。重要的是,本综述强调了阻碍纳米药物临床转化的重大挑战,并提出了超越这些挑战的可能补救措施。
{"title":"Novel paradigm of therapeutic intervention for skin cancer: challenges and opportunities","authors":"Modassir Nasim,&nbsp;Mariya Khan,&nbsp;Rabea Parveen,&nbsp;Azka Gull,&nbsp;Saba Khan,&nbsp;Javed Ali","doi":"10.1186/s43094-024-00686-2","DOIUrl":"10.1186/s43094-024-00686-2","url":null,"abstract":"<div><h3>Background</h3><p>Skin cancer continues to be an imperative global health issue, urging continuous exploration of treatment methodologies. Conventional treatments for skin cancer include surgical interventions, immunotherapy, targeted therapy, chemotherapy, and radiation therapy. However, these methods often present obstacles like treatment resistance, systemic toxicity, limited effectiveness in advanced stages, infection risk, pain, long recovery, and impact on healthy tissue.</p><h3>Main body of the abstract</h3><p>Nanomedicine holds promise by facilitating precise drug administration, early detection, and heightened therapeutic efficiency via targeted and localized delivery systems. The integration of nanomedicine into skin cancer alleviation therapies demonstrates optimistic outcomes, including refined drug delivery, augmented bioavailability, minimized adverse effects, and potential theranostic applications. Recent breakthroughs in nanomedicine have propelled advancements in skin cancer treatment, showing significant potential in transforming the treatment paradigm. The presents review provides comprehensive aspects of existing skin cancer treatments and their challenges, spotlighting recent breakthroughs propelled by nanomedicine.</p><h3>Short conclusion</h3><p>This abstract delineates the present landscape of skin cancer treatments, underscores their constraints, and highlights recent strides in nanomedicine that have the potential to transform the paradigm of skin cancer treatment, ultimately elevating patient prognosis. Importantly, the present review emphasizes substantial challenges that hinder the clinical translation of nanomedicines and suggests possible remedies to surpass them.</p><h3>Graphic abstract</h3><div><figure><div><div><picture><source><img></source></picture></div></div></figure></div></div>","PeriodicalId":577,"journal":{"name":"Future Journal of Pharmaceutical Sciences","volume":"10 1","pages":""},"PeriodicalIF":3.4,"publicationDate":"2024-09-02","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://fjps.springeropen.com/counter/pdf/10.1186/s43094-024-00686-2","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142117932","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Healthcare providers' perspectives on corticosteroid-containing drugs: a cross-sectional study in the United Arab Emirates 医疗服务提供者对含皮质类固醇药物的看法:阿拉伯联合酋长国的一项横断面研究
IF 3.4 Q2 PHARMACOLOGY & PHARMACY Pub Date : 2024-09-02 DOI: 10.1186/s43094-024-00690-6
Muna Barakat, Diana Malaeb, Ahmad El Ouweini, Salah Aburuz, Sham ZainAlabdin, Omar El Khatib, Bassem Sadek, Razan I. Nassar, Amal Akour

Background

Addressing knowledge and concerns related to corticosteroid is essential to enhance patient care, promote optimal utilization, and minimize their potential side effects.

Methods

A cross-sectional study was conducted to assess knowledge and attitudes regarding corticosteroid use among healthcare providers (HCPs) in the United Arab Emirates using a validated questionnaire. Knowledge, attitudes, and fear items were described as frequency and percentages. Then, a total score was calculated; multilinear regression was used to see the effect of demographics on these scores.

Results

Among 129 HCPs, 100 had previously prescribed corticosteroids (77.5%), with intranasal spray being the most dispensed dosage form (89.0%). Respiratory diseases were the most reported indication for corticosteroid dispensing (93.0%). HCPs preferred corticosteroids for their ability to quickly relief of patients' symptoms (67.0%). About 60.0% identified increased appetite as a patient-reported side effect. The assessment of the HCPs' knowledge showed a median score of 10 out of 11 (IQR = 9–11). The median fear score was six out of 10 (IQR = 4–10), but they were significantly and conversely related to each other.

Conclusion

This study revealed that while HCPs in the UAE possess substantial knowledge regarding corticosteroid use, their concerns, particularly around side effects, indicate a need for further education. Addressing these concerns through targeted educational programs could enhance the safe and effective utilization of corticosteroids, ultimately improving patient care outcomes.

背景解决与皮质类固醇相关的知识和顾虑对于加强患者护理、促进最佳利用以及最大限度地减少其潜在副作用至关重要。方法在阿拉伯联合酋长国开展了一项横断面研究,使用经过验证的问卷评估医疗保健提供者(HCPs)对皮质类固醇使用的知识和态度。以频率和百分比来描述知识、态度和恐惧项目。结果 在 129 名医护人员中,有 100 人曾开过皮质类固醇处方(77.5%),其中鼻内喷雾剂是最常用的处方剂型(89.0%)。据报告,呼吸系统疾病是皮质类固醇配药最多的适应症(93.0%)。高级保健人员更喜欢皮质类固醇,因为它能迅速缓解患者的症状(67.0%)。约 60.0% 的医生认为食欲增加是患者报告的副作用之一。对保健医生知识的评估显示,在满分 11 分中,中位数为 10 分(IQR = 9-11)。结论这项研究表明,虽然阿联酋的保健医生掌握了大量有关皮质类固醇使用的知识,但他们所担心的问题,尤其是副作用,表明需要进一步的教育。通过有针对性的教育计划来解决这些问题,可以提高皮质类固醇的安全有效使用,最终改善患者的治疗效果。
{"title":"Healthcare providers' perspectives on corticosteroid-containing drugs: a cross-sectional study in the United Arab Emirates","authors":"Muna Barakat,&nbsp;Diana Malaeb,&nbsp;Ahmad El Ouweini,&nbsp;Salah Aburuz,&nbsp;Sham ZainAlabdin,&nbsp;Omar El Khatib,&nbsp;Bassem Sadek,&nbsp;Razan I. Nassar,&nbsp;Amal Akour","doi":"10.1186/s43094-024-00690-6","DOIUrl":"10.1186/s43094-024-00690-6","url":null,"abstract":"<div><h3>Background</h3><p>Addressing knowledge and concerns related to corticosteroid is essential to enhance patient care, promote optimal utilization, and minimize their potential side effects.</p><h3>Methods</h3><p>A cross-sectional study was conducted to assess knowledge and attitudes regarding corticosteroid use among healthcare providers (HCPs) in the United Arab Emirates using a validated questionnaire. Knowledge, attitudes, and fear items were described as frequency and percentages. Then, a total score was calculated; multilinear regression was used to see the effect of demographics on these scores.</p><h3>Results</h3><p>Among 129 HCPs<b>,</b> 100 had previously prescribed corticosteroids (77.5%), with intranasal spray being the most dispensed dosage form (89.0%). Respiratory diseases were the most reported indication for corticosteroid dispensing (93.0%). HCPs preferred corticosteroids for their ability to quickly relief of patients' symptoms (67.0%). About 60.0% identified increased appetite as a patient-reported side effect. The assessment of the HCPs' knowledge showed a median score of 10 out of 11 (IQR = 9–11). The median fear score was six out of 10 (IQR = 4–10), but they were significantly and conversely related to each other.</p><h3>Conclusion</h3><p>This study revealed that while HCPs in the UAE possess substantial knowledge regarding corticosteroid use, their concerns, particularly around side effects, indicate a need for further education. Addressing these concerns through targeted educational programs could enhance the safe and effective utilization of corticosteroids, ultimately improving patient care outcomes.</p></div>","PeriodicalId":577,"journal":{"name":"Future Journal of Pharmaceutical Sciences","volume":"10 1","pages":""},"PeriodicalIF":3.4,"publicationDate":"2024-09-02","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://fjps.springeropen.com/counter/pdf/10.1186/s43094-024-00690-6","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142123082","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Synergistic effect of waste-derived β-tricalcium phosphate microbeads loaded in hydroxyapatite-keratin-polyvinyl alcohol composite matrix in drug release for osteosarcoma treatment 羟基磷灰石-角蛋白-聚乙烯醇复合基质中负载的废物衍生β磷酸三钙微珠在骨肉瘤治疗中的药物释放协同效应
IF 3.4 Q2 PHARMACOLOGY & PHARMACY Pub Date : 2024-08-28 DOI: 10.1186/s43094-024-00681-7
Himanshi Diwan, Siddhartha Dan, Mahesh Kumar Sah

Background

Sustained drug delivery system (DDS) for clinically relevant osteosarcoma medications is a promising strategy for treatment. β-tricalcium phosphate (β-TCP) microbeads loaded with doxorubicin hydrochloride (DOX) and cis-diamminedichloroplatin (CDDP) anticancer drugs in a matrix of hydroxyapatite-keratin-polyvinyl alcohol composite matrix scaffolds (HAp-K-PVA) was developed as promising DDS. HAp, β-TCP, and K utilized for the development of DDS were resourced from avian eggshells and human hairs, respectively, and duly characterized before application.

Methods

The β-TCP/alginate microbeads were fabricated using droplet extrusion and ionotropic gelation, and integrated into secondary drug carrier HAp-K-PVA composite matrix, via freeze gelation. The physicochemical and thermal characterization of developed microbeads and matrix scaffolds was performed.

Results

When DOX and CDDP were co-loaded in DDS, a synergistic impact was observed after 30 days of continuous release, in contrast to the immediate outburst as seen with individual DOX and CDDP releases. Besides, the drug release from the microbeads only, the release with the HAp-K-PVA composite matrix scaffolds was observed slower. The controlled release, antibacterial effectiveness against the test pathogens and cell viability with osteoblast-like osteosarcoma (UTOS) cells indicated the therapeutic potential for the treatment of osteosarcoma in situ. The cell viability was observed for 24 h, which showed nearly 90% after 24 h for HAp-K-PVA composite matrix scaffolds, decreased for all the scaffold groups after 72 h, indicating the enhancement due to combined synergistic effect of the co-loaded drugs.

Conclusion

This study established a promising foundation for novel and sustainable biomaterials for osteosarcoma treatment. Further advancement holds the potential to enhance patient clinical outcomes and foster advancements in the field of regenerative medicine.

背景用于临床相关骨肉瘤药物的持续给药系统(DDS)是一种前景广阔的治疗策略。在羟基磷灰石-角蛋白-聚乙烯醇复合基质支架(HAp-K-PVA)中载入盐酸多柔比星(DOX)和顺式二氨基二氯铂(CDDP)抗癌药物的β-磷酸三钙(β-TCP)微珠被开发为前景广阔的 DDS。开发 DDS 所用的 HAp、β-TCP 和 K 分别取自禽类蛋壳和人类毛发,并在应用前进行了适当的表征。结果将 DOX 和 CDDP 共同载入 DDS 后,在持续释放 30 天后观察到了协同效应,这与单独释放 DOX 和 CDDP 时的立即爆发形成了鲜明对比。此外,仅从微珠中释放药物时,HAp-K-PVA 复合基质支架的释放速度较慢。药物的可控释放、对测试病原体的抗菌效果以及成骨细胞样骨肉瘤(UTOS)细胞的存活率都表明了这种材料在原位治疗骨肉瘤方面的治疗潜力。在 24 小时内观察到的细胞存活率显示,HAp-K-PVA 复合基质支架的细胞存活率接近 90%,72 小时后所有支架组的细胞存活率均有所下降,这表明共负载药物的联合协同效应增强了细胞存活率。该研究为新型可持续生物材料治疗骨肉瘤奠定了良好的基础,其进一步发展有望提高患者的临床疗效,促进再生医学领域的进步。
{"title":"Synergistic effect of waste-derived β-tricalcium phosphate microbeads loaded in hydroxyapatite-keratin-polyvinyl alcohol composite matrix in drug release for osteosarcoma treatment","authors":"Himanshi Diwan,&nbsp;Siddhartha Dan,&nbsp;Mahesh Kumar Sah","doi":"10.1186/s43094-024-00681-7","DOIUrl":"10.1186/s43094-024-00681-7","url":null,"abstract":"<div><h3>Background</h3><p>Sustained drug delivery system (DDS) for clinically relevant osteosarcoma medications is a promising strategy for treatment. β-tricalcium phosphate (β-TCP) microbeads loaded with doxorubicin hydrochloride (DOX) and cis-diamminedichloroplatin (CDDP) anticancer drugs in a matrix of hydroxyapatite-keratin-polyvinyl alcohol composite matrix scaffolds (HAp-K-PVA) was developed as promising DDS. HAp, β-TCP, and K utilized for the development of DDS were resourced from avian eggshells and human hairs, respectively, and duly characterized before application.</p><h3>Methods</h3><p>The β-TCP/alginate microbeads were fabricated using droplet extrusion and ionotropic gelation, and integrated into secondary drug carrier HAp-K-PVA composite matrix, via freeze gelation. The physicochemical and thermal characterization of developed microbeads and matrix scaffolds was performed.</p><h3>Results</h3><p>When DOX and CDDP were co-loaded in DDS, a synergistic impact was observed after 30 days of continuous release, in contrast to the immediate outburst as seen with individual DOX and CDDP releases. Besides, the drug release from the microbeads only, the release with the HAp-K-PVA composite matrix scaffolds was observed slower. The controlled release, antibacterial effectiveness against the test pathogens and cell viability with osteoblast-like osteosarcoma (UTOS) cells indicated the therapeutic potential for the treatment of osteosarcoma in situ. The cell viability was observed for 24 h, which showed nearly 90% after 24 h for HAp-K-PVA composite matrix scaffolds, decreased for all the scaffold groups after 72 h, indicating the enhancement due to combined synergistic effect of the co-loaded drugs.</p><h3>Conclusion</h3><p>This study established a promising foundation for novel and sustainable biomaterials for osteosarcoma treatment. Further advancement holds the potential to enhance patient clinical outcomes and foster advancements in the field of regenerative medicine.</p></div>","PeriodicalId":577,"journal":{"name":"Future Journal of Pharmaceutical Sciences","volume":"10 1","pages":""},"PeriodicalIF":3.4,"publicationDate":"2024-08-28","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://fjps.springeropen.com/counter/pdf/10.1186/s43094-024-00681-7","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142084557","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
A critical analytical aspect on analytical protocols in the pharmaceutical analysis of H1N1 antiviral agent and its active metabolite 甲型 H1N1 流感病毒抗病毒剂及其活性代谢物药物分析中的关键分析方法
IF 3.4 Q2 PHARMACOLOGY & PHARMACY Pub Date : 2024-08-28 DOI: 10.1186/s43094-024-00666-6
Suraj R. Chaudhari, Vaibhavi K. Salunkhe, Shubham D. Tabade, Pragati K. Bhonde, Sarthak G. Kulkarni, Dnyaneshwar H. Maykar, Saurabh B. Ganorkar, Sanjay J,  Surana, Atul A. Shirkhedkar

Background

Oseltamivir (OSM) was the first active oral therapeutic inhibitor approved by the Food and Drug Administration in 1999 for the clinical management of the influenza virus. It is an ester-type prodrug of OSM carboxylate in the market under the trade name Tamiflu™ capsules, i.e., oseltamivir phosphate. Because of the ubiquitous application to alleviate influenza virus (flu virus) symptoms, it is imperative to develop systematic analytical protocols for quality control laboratories, bioequivalence, and pharmacokinetic analysis.

Main body of the abstract

This review provides complete state-of-the-art analytical protocols for quantifying OSM, as published in scientific journals and official compendia. Several studies use LC–MS/MS and HPLC/UV. Additionally, there are reports on UPLC, HPTLC, capillary electrophoresis, FTIR, voltammetry, potentiometry, spectrophotometric, and spectrofluorometry protocols for the drug. Many analytical protocols have also been documented to analyze OSM from environmental water, surface water, sewage discharge, the Neya River and treated sewage effluent and surface water.

Conclusion

The present review concludes with significant remarks on the methodology used to analyze OSM. Despite the therapeutic applicability of the drug, there are a limited number of comprehensive documents on analytical protocols for determining its concentration in various matrices. This lack of information is elusive, as the applicability and effectiveness of these protocols are crucial for ensuring the quality, efficacy, and safety of OSM.

背景奥司他韦(OSM)是美国食品和药物管理局于 1999 年批准用于临床治疗流感病毒的第一种活性口服治疗抑制剂。它是 OSM 羧酸酯类原药,在市场上的商品名为特敏福™胶囊,即磷酸奥司他韦。由于 OSM 可用于缓解流感病毒(流感病毒)症状,因此必须为质量控制实验室、生物等效性和药动学分析制定系统的分析方案。一些研究使用了 LC-MS/MS 和 HPLC/UV。此外,还有关于 UPLC、HPTLC、毛细管电泳、傅立叶变换红外光谱、伏安法、电位法、分光光度法和分光荧光法等药物分析方案的报告。本综述最后对用于分析 OSM 的方法作了重要评论。尽管该药物可用于治疗,但有关确定其在各种基质中浓度的分析规程的综合文献数量有限。这种信息的缺乏令人难以捉摸,因为这些规程的适用性和有效性对于确保 OSM 的质量、疗效和安全性至关重要。
{"title":"A critical analytical aspect on analytical protocols in the pharmaceutical analysis of H1N1 antiviral agent and its active metabolite","authors":"Suraj R. Chaudhari,&nbsp;Vaibhavi K. Salunkhe,&nbsp;Shubham D. Tabade,&nbsp;Pragati K. Bhonde,&nbsp;Sarthak G. Kulkarni,&nbsp;Dnyaneshwar H. Maykar,&nbsp;Saurabh B. Ganorkar,&nbsp;Sanjay J,&nbsp; Surana,&nbsp;Atul A. Shirkhedkar","doi":"10.1186/s43094-024-00666-6","DOIUrl":"10.1186/s43094-024-00666-6","url":null,"abstract":"<div><h3>Background</h3><p>Oseltamivir (OSM) was the first active oral therapeutic inhibitor approved by the Food and Drug Administration in 1999 for the clinical management of the influenza virus. It is an ester-type prodrug of OSM carboxylate in the market under the trade name Tamiflu™ capsules, i.e., oseltamivir phosphate. Because of the ubiquitous application to alleviate influenza virus (flu virus) symptoms, it is imperative to develop systematic analytical protocols for quality control laboratories, bioequivalence, and pharmacokinetic analysis.</p><h3>Main body of the abstract</h3><p>This review provides complete state-of-the-art analytical protocols for quantifying OSM, as published in scientific journals and official compendia. Several studies use LC–MS/MS and HPLC/UV. Additionally, there are reports on UPLC, HPTLC, capillary electrophoresis, FTIR, voltammetry, potentiometry, spectrophotometric, and spectrofluorometry protocols for the drug. Many analytical protocols have also been documented to analyze OSM from environmental water, surface water, sewage discharge, the Neya River and treated sewage effluent and surface water.</p><h3>Conclusion</h3><p>The present review concludes with significant remarks on the methodology used to analyze OSM. Despite the therapeutic applicability of the drug, there are a limited number of comprehensive documents on analytical protocols for determining its concentration in various matrices. This lack of information is elusive, as the applicability and effectiveness of these protocols are crucial for ensuring the quality, efficacy, and safety of OSM.</p></div>","PeriodicalId":577,"journal":{"name":"Future Journal of Pharmaceutical Sciences","volume":"10 1","pages":""},"PeriodicalIF":3.4,"publicationDate":"2024-08-28","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://fjps.springeropen.com/counter/pdf/10.1186/s43094-024-00666-6","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142091156","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Identification and characterization of phytochemicals in methanolic extract of roots of Datura fastuosa using various techniques 采用多种技术鉴定曼陀罗根甲醇提取物中的植物化学物质并确定其特征
IF 3.4 Q2 PHARMACOLOGY & PHARMACY Pub Date : 2024-08-27 DOI: 10.1186/s43094-024-00682-6
Girma Mengesha Melese, Tewodros Brihanu Aychiluhim, Abdurrahman Mengesha Yessuf, Matthewos Eshete

Background

Plant extracts have attracted significant interest among researchers due to their potential bioactivity and crucial contribution to the production of pharmaceutical compounds. In this study, the primary objective was to extract, analyze and characterize the bioactive compounds found in the methanol root extract of Datura fastuosa (D. fastuosa). This was achieved using various analytical techniques such as gas chromatography/mass spectrometry (GC–MS), ultra-violet visible spectrophotometry, Fourier-transform infrared (FT-IR), nuclear magnetic radiation spectrometry (NMR) and DPPH free radical scavenging activity assay.

Results

GC–MS analysis of the methanol root crude extract identified 49 compounds. Three compounds were isolated via column chromatography; one was pure, with a sharp melting point and clean IR spectrum, while the other two showed broad melting points and IR interferences. Comprehensive investigation of the pure extract revealed a UV profile with two distinct bands (300–800 nm) and confirmed functional groups (alcohol, alkanes, alkenes, carbonyl, methylene, and methyl) through FT-IR analysis. The 1HNMR (proton nuclear magnetic resonance spectroscopy) signal confirmed the presence of forty-nine non-equivalent protons, 13CNMR (Carbon-13 nuclear magnetic resonance spectroscopy) signal confirmed the presence of 32 non-equivalent carbons and DEPT-135 (distortionless enhancement by polarization transfer-135) signal confirmed the presence of 24 carbons (17 for odd and 7 for even) which are protons containing carbons in the compound. Combining the above mentioned analyses with data obtained from the GC/MS analysis of National Institute of Standards and Technology (NIST) library, the isolated pure compound exhibited a structural similarity to 1-(7-(3-hydroxyphenyl)-1,1,4a,5,6,9,10a,10b-octamethyl-1,2,3,4,4a,4b,6a,7,8,9,10,10a,10b,11,12,12a-hexadecahydrochrysen-2-yl)propan-1-one, with a chemical formula of C35H50O2.

Conclusions

The presence of various notable compounds, including phenolics, flavonoids, alkaloids, steroids etc., within the methanol root extract of D. fastuosa signifies its pharmacological potential. The methanol crude extract demonstrated antioxidant potential compared to standard ascorbic acid, exhibiting DPPH scavenging activity. Previous research has demonstrated the bioactivity of some of these compounds, further elucidating the plant’s medicinal properties. These findings not only suggest opportunities for developing synthetic drugs but also underscore its direct therapeutic potential in addressing diverse ailments.

背景植物提取物因其潜在的生物活性和对医药化合物生产的重要贡献而引起了研究人员的极大兴趣。本研究的主要目的是提取、分析和鉴定曼陀罗(D. fastuosa)甲醇根提取物中的生物活性化合物。研究采用了多种分析技术,如气相色谱/质谱法(GC-MS)、紫外可见分光光度法、傅立叶变换红外光谱法(FT-IR)、核磁辐射光谱法(NMR)和 DPPH 自由基清除活性测定法。通过柱层析分离出三个化合物,其中一个纯度高、熔点高、红外光谱清晰,而另外两个化合物熔点较宽且存在红外干扰。对纯萃取物的综合研究显示,其紫外光谱有两条明显的波段(300-800 nm),并通过傅立叶变换红外光谱分析确认了其官能团(醇、烷、烯、羰基、亚甲基和甲基)。1HNMR(质子核磁共振波谱)信号证实了化合物中存在 49 个非等价质子,13CNMR(碳-13 核磁共振波谱)信号证实了化合物中存在 32 个非等价碳原子,DEPT-135(极化转移无畸变增强-135)信号证实了化合物中存在 24 个碳原子(奇数为 17 个,偶数为 7 个),这些碳原子都是含有质子的碳原子。1,4a,5,6,9,10a,10b-八甲基-1,2,3,4,4a,4b,6a,7,8,9,10,10a,10b,11,12,12a-十六氢胆蒽-2-基)丙-1-酮的结构相似,化学式为 C35H50O2。结论 大叶黄杨的甲醇根提取物中含有多种重要化合物,包括酚类、黄酮类、生物碱和类固醇等、Fastuosa 的甲醇根提取物中含有多种重要化合物,包括酚类、黄酮类、生物碱、类固醇等,这表明其具有药理潜力。与标准抗坏血酸相比,甲醇粗萃取物表现出抗氧化潜力,具有 DPPH 清除活性。之前的研究已经证明了其中一些化合物的生物活性,进一步阐明了该植物的药用特性。这些发现不仅为开发合成药物提供了机会,而且还强调了它在解决各种疾病方面的直接治疗潜力。
{"title":"Identification and characterization of phytochemicals in methanolic extract of roots of Datura fastuosa using various techniques","authors":"Girma Mengesha Melese,&nbsp;Tewodros Brihanu Aychiluhim,&nbsp;Abdurrahman Mengesha Yessuf,&nbsp;Matthewos Eshete","doi":"10.1186/s43094-024-00682-6","DOIUrl":"10.1186/s43094-024-00682-6","url":null,"abstract":"<div><h3>Background</h3><p>Plant extracts have attracted significant interest among researchers due to their potential bioactivity and crucial contribution to the production of pharmaceutical compounds. In this study, the primary objective was to extract, analyze and characterize the bioactive compounds found in the methanol root extract of <i>Datura fastuosa</i> (<i>D. fastuosa</i>). This was achieved using various analytical techniques such as gas chromatography/mass spectrometry (GC–MS), ultra-violet visible spectrophotometry, Fourier-transform infrared (FT-IR), nuclear magnetic radiation spectrometry (NMR) and DPPH free radical scavenging activity assay.</p><h3>Results</h3><p>GC–MS analysis of the methanol root crude extract identified 49 compounds. Three compounds were isolated via column chromatography; one was pure, with a sharp melting point and clean IR spectrum, while the other two showed broad melting points and IR interferences. Comprehensive investigation of the pure extract revealed a UV profile with two distinct bands (300–800 nm) and confirmed functional groups (alcohol, alkanes, alkenes, carbonyl, methylene, and methyl) through FT-IR analysis. The <sup>1</sup>HNMR (proton nuclear magnetic resonance spectroscopy) signal confirmed the presence of forty-nine non-equivalent protons, <sup>13</sup>CNMR (Carbon-13 nuclear magnetic resonance spectroscopy) signal confirmed the presence of 32 non-equivalent carbons and DEPT-135 (distortionless enhancement by polarization transfer-135) signal confirmed the presence of 24 carbons (17 for odd and 7 for even) which are protons containing carbons in the compound. Combining the above mentioned analyses with data obtained from the GC/MS analysis of National Institute of Standards and Technology (NIST) library, the isolated pure compound exhibited a structural similarity to 1-(7-(3-hydroxyphenyl)-1,1,4a,5,6,9,10a,10b-octamethyl-1,2,3,4,4a,4b,6a,7,8,9,10,10a,10b,11,12,12a-hexadecahydrochrysen-2-yl)propan-1-one, with a chemical formula of C<sub>35</sub>H<sub>50</sub>O<sub>2</sub>.</p><h3>Conclusions</h3><p>The presence of various notable compounds, including phenolics, flavonoids, alkaloids, steroids etc., within the methanol root extract of <i>D. fastuosa</i> signifies its pharmacological potential. The methanol crude extract demonstrated antioxidant potential compared to standard ascorbic acid, exhibiting DPPH scavenging activity. Previous research has demonstrated the bioactivity of some of these compounds, further elucidating the plant’s medicinal properties. These findings not only suggest opportunities for developing synthetic drugs but also underscore its direct therapeutic potential in addressing diverse ailments.</p></div>","PeriodicalId":577,"journal":{"name":"Future Journal of Pharmaceutical Sciences","volume":"10 1","pages":""},"PeriodicalIF":3.4,"publicationDate":"2024-08-27","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://fjps.springeropen.com/counter/pdf/10.1186/s43094-024-00682-6","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142084558","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
α-Amylase, α-glucosidase and aldose reductase inhibitory and molecular docking studies on Tinospora cordifolia (Guduchi) leaf extract 天竺葵叶提取物对α-淀粉酶、α-葡萄糖苷酶和醛糖还原酶的抑制作用及分子对接研究
IF 3.4 Q2 PHARMACOLOGY & PHARMACY Pub Date : 2024-08-23 DOI: 10.1186/s43094-024-00671-9
Hemlata Janardhan Bhosale, Shailesh Vaijeenath Mamdapure, Ramdas Balaji Panchal, Umesh Pravin Dhuldhaj

Background

Type II diabetes mellitus is posing a severe health threat throughout the globe due to its associated pathophysiological risks and high mortality rate. Carbohydrate catabolic enzymes, including α-amylase, α-glucosidase and aldose reductase, play an important role in the development of diabetes. The natural or synthetic inhibitors of these enzymes are crucial in reducing diabetes and its related complications. Tinospora cordifolia is a plant of great significance in Ayurveda due to its unique biological activities, including anti-diabetic properties. The present study aims to identify the active constituents of T. cordifolia leaves and evaluate the in vitro inhibitory potential of its ethanol extract constituents against α-amylase, α-glucosidase and aldose reductase activities.

Results

The ethanolic leaf extract of T. cordifolia inhibited the activities of α-amylase, α-glucosidase and aldose reductase in a dose-dependent manner. It was on par  with the standard inhibitors acarbose and quercetin. At 5 mg/ml, the noted % inhibition values of extract were 69.27 ± 0.17, 67.8 ± 0.26 and 62.55 ± 0.24, respectively, for α-amylase, α-glucosidase and aldose reductase. Using GC-MS analysis, neophytadiene, γ-sitosterol, phytol, phytyl palmitate, and phytyl acetate were identified as prominent constituents of the ethanolic extract. Based on molecular docking and ADME analysis, γ-sitosterol was found as the major reactive phytoconstituent, which showed the highest inhibitory potential against α-amylase, α-glucosidase and aldose reductase activities.

Conclusions

The present study identified γ-sitosterol as triplet inhibitor of α-amylase, α-glucosidase and aldose reductase and affirmed the ethno-medicinal significance of T. cordifolia leaves in the development of new anti-diabetic leads.

背景II型糖尿病由于其相关的病理生理风险和高死亡率,正在对全球健康构成严重威胁。碳水化合物分解酶,包括α-淀粉酶、α-葡萄糖苷酶和醛糖还原酶,在糖尿病的发病过程中起着重要作用。这些酶的天然或合成抑制剂对减少糖尿病及其相关并发症至关重要。Tinospora cordifolia 是一种在阿育吠陀中具有重要意义的植物,因为它具有独特的生物活性,包括抗糖尿病特性。本研究旨在确定 T. cordifolia 叶子的活性成分,并评估其乙醇提取物成分对 α-淀粉酶、α-葡萄糖苷酶和醛糖还原酶活性的体外抑制潜力。它与标准抑制剂阿卡波糖和槲皮素的效果相当。在 5 毫克/毫升的浓度下,提取物对 α-淀粉酶、α-葡萄糖苷酶和醛糖还原酶的抑制率分别为 69.27 ± 0.17、67.8 ± 0.26 和 62.55 ± 0.24。通过气相色谱-质谱(GC-MS)分析,确定乙醇提取物的主要成分为新茶二烯、γ-谷甾醇、植醇、棕榈酸植脂酯和乙酸植脂酯。结论本研究发现γ-谷甾醇是α-淀粉酶、α-葡萄糖苷酶和醛糖还原酶的三重抑制剂,并肯定了T. cordifolia叶片在开发新的抗糖尿病药物方面的民族药用价值。
{"title":"α-Amylase, α-glucosidase and aldose reductase inhibitory and molecular docking studies on Tinospora cordifolia (Guduchi) leaf extract","authors":"Hemlata Janardhan Bhosale,&nbsp;Shailesh Vaijeenath Mamdapure,&nbsp;Ramdas Balaji Panchal,&nbsp;Umesh Pravin Dhuldhaj","doi":"10.1186/s43094-024-00671-9","DOIUrl":"10.1186/s43094-024-00671-9","url":null,"abstract":"<div><h3>Background</h3><p>Type II diabetes mellitus is posing a severe health threat throughout the globe due to its associated pathophysiological risks and high mortality rate. Carbohydrate catabolic enzymes, including α-amylase, α-glucosidase and aldose reductase, play an important role in the development of diabetes. The natural or synthetic inhibitors of these enzymes are crucial in reducing diabetes and its related complications. <i>Tinospora</i> <i>cordifolia</i> is a plant of great significance in Ayurveda due to its unique biological activities, including anti-diabetic properties. The present study aims to identify the active constituents of <i>T</i>. <i>cordifolia</i> leaves and evaluate the in vitro inhibitory potential of its ethanol extract constituents against α-amylase, α-glucosidase and aldose reductase activities.</p><h3>Results</h3><p>The ethanolic leaf extract of <i>T</i>. <i>cordifolia</i> inhibited the activities of α-amylase, α-glucosidase and aldose reductase in a dose-dependent manner. It was on par  with the standard inhibitors acarbose and quercetin. At 5 mg/ml, the noted % inhibition values of extract were 69.27 ± 0.17, 67.8 ± 0.26 and 62.55 ± 0.24, respectively, for α-amylase, α-glucosidase and aldose reductase. Using GC-MS analysis, neophytadiene, γ-sitosterol, phytol, phytyl palmitate, and phytyl acetate were identified as prominent constituents of the ethanolic extract. Based on molecular docking and ADME analysis, γ-sitosterol was found as the major reactive phytoconstituent, which showed the highest inhibitory potential against α-amylase, α-glucosidase and aldose reductase activities.</p><h3>Conclusions</h3><p>The present study identified γ-sitosterol as triplet inhibitor of α-amylase, α-glucosidase and aldose reductase and affirmed the ethno-medicinal significance of <i>T</i>. <i>cordifolia</i> leaves in the development of new anti-diabetic leads.</p></div>","PeriodicalId":577,"journal":{"name":"Future Journal of Pharmaceutical Sciences","volume":"10 1","pages":""},"PeriodicalIF":3.4,"publicationDate":"2024-08-23","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://fjps.springeropen.com/counter/pdf/10.1186/s43094-024-00671-9","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142045156","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Antioxidants as adjuvant therapy in the treatment of community-acquired pneumonia 抗氧化剂作为治疗社区获得性肺炎的辅助疗法
IF 3.4 Q2 PHARMACOLOGY & PHARMACY Pub Date : 2024-08-22 DOI: 10.1186/s43094-024-00674-6
Fatma Makram Youssef, Eman Mohamed Elmokadem, Amir Eskander Hanna Samy, Hayam Ateyya

Background

Community-acquired pneumonia remains a major health concern, characterized by significant morbidity and mortality. The underlying pathophysiology of community-acquired pneumonia involves substantial oxidative stress and inflammation, which contribute to lung tissue damage and impaired immune function.

Main body

Variations in oxidative metabolism contribute to the inflammatory cascade which triggers pneumonia to commence and evolve, whereas oxidative stress as well as inflammatory processes is strongly related. Understanding the underlying immunological dysregulation and unbalanced redox that heighten vulnerability to a variety of illnesses has improved over the past several decades attributable to research. One of the key strategies for addressing oxidative stress is to lower the reactive oxygen species creation in the mitochondrion which is one of the main sites of their generation by using antioxidants, where they prevent oxidants from transferring electrons to other molecules. Consequently, antioxidants either directly or indirectly reduce the risk of damage and preserve the redox equilibrium. Therefore, antioxidants, due to their ability to neutralize reactive oxygen species and modulate inflammatory processes, have been explored as potential adjuvant therapies to enhance the treatment outcomes of community-acquired pneumonia. Where recent research has explored the potential of antioxidants as adjuvant therapy in the treatment of community-acquired pneumonia, aiming to mitigate these detrimental effects. Antioxidants such as N-acetylcystein, vitamin C, vitamin E, astaxanthin, and zinc have shown promising results in both preclinical and clinical studies.

Conclusion

Outcomes of several in vitro as well as in vivo antioxidant studies have demonstrated the antioxidants' promising potential as an adjunct pneumonia therapy. For an assessment of its effectiveness in this therapeutic context, more research involving humans will be required.

背景社区获得性肺炎仍然是一个主要的健康问题,发病率和死亡率都很高。社区获得性肺炎的基本病理生理学涉及大量的氧化应激和炎症,这导致了肺组织损伤和免疫功能受损。过去几十年来,由于研究的深入,人们对导致各种疾病易发的潜在免疫失调和氧化还原失衡有了更深入的了解。解决氧化应激问题的关键策略之一是通过使用抗氧化剂来降低线粒体中活性氧的产生,线粒体是产生活性氧的主要场所之一。因此,抗氧化剂可以直接或间接地降低损害风险并保持氧化还原平衡。因此,抗氧化剂因其中和活性氧和调节炎症过程的能力,已被视为潜在的辅助疗法,以提高社区获得性肺炎的治疗效果。最近的研究探索了抗氧化剂作为辅助疗法治疗社区获得性肺炎的潜力,旨在减轻这些不利影响。N-乙酰胞嘧啶、维生素 C、维生素 E、虾青素和锌等抗氧化剂在临床前和临床研究中均显示出良好的效果。要评估抗氧化剂的治疗效果,还需要进行更多的人体研究。
{"title":"Antioxidants as adjuvant therapy in the treatment of community-acquired pneumonia","authors":"Fatma Makram Youssef,&nbsp;Eman Mohamed Elmokadem,&nbsp;Amir Eskander Hanna Samy,&nbsp;Hayam Ateyya","doi":"10.1186/s43094-024-00674-6","DOIUrl":"10.1186/s43094-024-00674-6","url":null,"abstract":"<div><h3>Background</h3><p>Community-acquired pneumonia remains a major health concern, characterized by significant morbidity and mortality. The underlying pathophysiology of community-acquired pneumonia involves substantial oxidative stress and inflammation, which contribute to lung tissue damage and impaired immune function.</p><h3>Main body</h3><p>Variations in oxidative metabolism contribute to the inflammatory cascade which triggers pneumonia to commence and evolve, whereas oxidative stress as well as inflammatory processes is strongly related. Understanding the underlying immunological dysregulation and unbalanced redox that heighten vulnerability to a variety of illnesses has improved over the past several decades attributable to research. One of the key strategies for addressing oxidative stress is to lower the reactive oxygen species creation in the mitochondrion which is one of the main sites of their generation by using antioxidants, where they prevent oxidants from transferring electrons to other molecules. Consequently, antioxidants either directly or indirectly reduce the risk of damage and preserve the redox equilibrium. Therefore, antioxidants, due to their ability to neutralize reactive oxygen species and modulate inflammatory processes, have been explored as potential adjuvant therapies to enhance the treatment outcomes of community-acquired pneumonia. Where recent research has explored the potential of antioxidants as adjuvant therapy in the treatment of community-acquired pneumonia, aiming to mitigate these detrimental effects. Antioxidants such as N-acetylcystein, vitamin C, vitamin E, astaxanthin, and zinc have shown promising results in both preclinical and clinical studies.</p><h3>Conclusion</h3><p>Outcomes of several in vitro as well as in vivo antioxidant studies have demonstrated the antioxidants' promising potential as an adjunct pneumonia therapy. For an assessment of its effectiveness in this therapeutic context, more research involving humans will be required.</p></div>","PeriodicalId":577,"journal":{"name":"Future Journal of Pharmaceutical Sciences","volume":"10 1","pages":""},"PeriodicalIF":3.4,"publicationDate":"2024-08-22","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://fjps.springeropen.com/counter/pdf/10.1186/s43094-024-00674-6","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142041502","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Enhanced viability of Lactobacillus spp. via encapsulation in hyaluronan/PVA hybrid electrospun composites for vaginal drug delivery 通过封装在透明质酸/PVA 混合电纺复合材料中提高乳酸杆菌的活力,用于阴道给药
IF 3.4 Q2 PHARMACOLOGY & PHARMACY Pub Date : 2024-08-21 DOI: 10.1186/s43094-024-00675-5
Margaret O. Ilomuanya, Deborah A. Ogundemuren, Peace-OfonAbasi O. Bassey, Bukola A. Oseni, Adeola T. Kola-Mustapha, Dimitrios Tsamos, Tsamis Alkiviadis, Alexandros E. Tsouknidas, Andrew N. Amenaghawon

Background

Vaginal dysbiosis, a change in the beneficial vaginal microbiome, leads to a significant depletion in the essential lactobacilli thus increasing the possibility of vaginal infections such as bacterial vaginosis. Probiotics have gained more attention as a means of delivering exogenous lactobacilli but one of the challenges in delivery strategies is maintaining and improving their viability. The objective of this study is to enhance the viability of Lactobacillus spp., via encapsulation in hyaluronic acid/polyvinyl alcohol hybrid electrospun nanofibers. Polyvinyl alcohol (PVA) and hyaluronic acid (HA) composite nanofibers integrated with Lactobacillus spp. were fabricated by electrospinning. The survival of Lactobacillus spp. after its immobilization in electrospun nanofibers with polyvinyl alcohol and hyaluronic acid was evaluated.

Results

Scanning electron microscopy indicated larger average diameters in PVA/HA nanofibers with Lactobacillus spp. encapsulation (0.189 ± 0.041 µm to 0.231 ± 0.061 µm between D3 and D4, and 0.177 ± 0.043 µm to 0.212 ± 0.041 µm between D5 and D6) which showed that the nanofibers had the bacterial cells successfully enclosed in them. The viability of the lactic acid bacteria enclosed in the PVA/HA nanofibers was observed to decrease by more than 2-log units.

Conclusion

The electrospun nanofiber-based delivery system is promising for the encapsulation and delivery of lactic acid bacteria to the vagina to combat recurrent vaginal infections such as bacterial vaginosis.

背景阴道菌群失调是指有益的阴道微生物群发生变化,导致必需的乳酸杆菌大量减少,从而增加了细菌性阴道病等阴道感染的可能性。益生菌作为一种提供外源性乳酸杆菌的手段受到越来越多的关注,但提供策略的挑战之一是保持和提高乳酸杆菌的活力。本研究的目的是通过将乳酸杆菌封装在透明质酸/聚乙烯醇混合电纺纳米纤维中来提高乳酸杆菌的活力。本研究采用电纺丝法制造了含有乳酸杆菌的聚乙烯醇(PVA)和透明质酸(HA)复合纳米纤维。结果扫描电子显微镜显示,乳酸杆菌包裹的 PVA/HA 纳米纤维的平均直径更大(0.189μm)。结果扫描电子显微镜显示,包覆乳酸杆菌的 PVA/HA 纳米纤维的平均直径较大(D3 和 D4 之间为 0.189 ± 0.041 µm 至 0.231 ± 0.061 µm,D5 和 D6 之间为 0.177 ± 0.043 µm 至 0.212 ± 0.041 µm),这表明纳米纤维成功地包覆了细菌细胞。结论基于电纺纳米纤维的给药系统有望封装乳酸菌并将其输送到阴道,以防治细菌性阴道病等反复发作的阴道感染。
{"title":"Enhanced viability of Lactobacillus spp. via encapsulation in hyaluronan/PVA hybrid electrospun composites for vaginal drug delivery","authors":"Margaret O. Ilomuanya,&nbsp;Deborah A. Ogundemuren,&nbsp;Peace-OfonAbasi O. Bassey,&nbsp;Bukola A. Oseni,&nbsp;Adeola T. Kola-Mustapha,&nbsp;Dimitrios Tsamos,&nbsp;Tsamis Alkiviadis,&nbsp;Alexandros E. Tsouknidas,&nbsp;Andrew N. Amenaghawon","doi":"10.1186/s43094-024-00675-5","DOIUrl":"10.1186/s43094-024-00675-5","url":null,"abstract":"<div><h3>Background</h3><p>Vaginal dysbiosis, a change in the beneficial vaginal microbiome, leads to a significant depletion in the essential lactobacilli thus increasing the possibility of vaginal infections such as bacterial vaginosis. Probiotics have gained more attention as a means of delivering exogenous lactobacilli but one of the challenges in delivery strategies is maintaining and improving their viability. The objective of this study is to enhance the viability of <i>Lactobacillus</i> spp., via encapsulation in hyaluronic acid/polyvinyl alcohol hybrid electrospun nanofibers. Polyvinyl alcohol (PVA) and hyaluronic acid (HA) composite nanofibers integrated with <i>Lactobacillus</i> spp. were fabricated by electrospinning. The survival of <i>Lactobacillus</i> spp. after its immobilization in electrospun nanofibers with polyvinyl alcohol and hyaluronic acid was evaluated.</p><h3>Results</h3><p>Scanning electron microscopy indicated larger average diameters in PVA/HA nanofibers with <i>Lactobacillus</i> spp. encapsulation (0.189 ± 0.041 µm to 0.231 ± 0.061 µm between D3 and D4, and 0.177 ± 0.043 µm to 0.212 ± 0.041 µm between D5 and D6) which showed that the nanofibers had the bacterial cells successfully enclosed in them. The viability of the lactic acid bacteria enclosed in the PVA/HA nanofibers was observed to decrease by more than 2-log units.</p><h3>Conclusion</h3><p>The electrospun nanofiber-based delivery system is promising for the encapsulation and delivery of lactic acid bacteria to the vagina to combat recurrent vaginal infections such as bacterial vaginosis.</p></div>","PeriodicalId":577,"journal":{"name":"Future Journal of Pharmaceutical Sciences","volume":"10 1","pages":""},"PeriodicalIF":3.4,"publicationDate":"2024-08-21","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://fjps.springeropen.com/counter/pdf/10.1186/s43094-024-00675-5","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142021728","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Stability-indicating liquid chromatographic method development and validation for quantification of trifarotene in pure and topical drug product 稳定指示液相色谱法的开发与验证--用于定量检测纯品和外用药物产品中的三胡萝卜素
IF 3.4 Q2 PHARMACOLOGY & PHARMACY Pub Date : 2024-08-20 DOI: 10.1186/s43094-024-00683-5
Muhammad Usman, Muhammad Bilal Shafique

Background

Trifarotene is effective for treating acne and other skin issues. To ensure its quality and meet regulatory standards, a reverse phase liquid chromatography (RP-LC) stability-indicating method was developed and validated for its quantification in pure and topical dosage forms. An isocratic elution chromatographic method was employed, using an octadecylsilyl silica gel-packed column (150 mm × 4.6 mm, 3 µm particle size). The mobile phase was a mixture of phosphate buffer and acetonitrile (40:60 v/v). Chromatographic conditions included a flow rate of 0.5 mL/min, column temperature of 40 °C, detection at 265 nm, and injection volume of 20 µL.

Results

The developed analytical method reports the retention time of trifarotene 11.2 min, higher theoretical plate count, asymmetric peak, and good resolution between the peaks of trifarotene, phenoxyethanol, and environmentally generated impurities.

Conclusion

The analytical method has been found to be linear, accurate, robust, specific, and selective for impurities produced during forced degradation studies. The proposed analytical method can be utilized for routine pharmaceutical analysis of trifarotene to judge its quality and safety.

背景三胡萝卜素可有效治疗痤疮和其他皮肤问题。为确保其质量并符合监管标准,本研究开发了一种反相液相色谱(RP-LC)稳定性指示方法,并对其在纯品和外用剂型中的定量进行了验证。该方法采用等度洗脱色谱法,使用十八烷基硅胶填料色谱柱(150 毫米 × 4.6 毫米,3 微米粒径)。流动相为磷酸盐缓冲液和乙腈(40:60 v/v)的混合物。结果所开发的分析方法的三胡萝卜素保留时间为 11.2 分钟,理论板数较高,峰不对称,三胡萝卜素、苯氧乙醇和环境中产生的杂质的峰之间具有良好的分辨率。所提出的分析方法可用于三胡萝卜素的常规药物分析,以判断其质量和安全性。
{"title":"Stability-indicating liquid chromatographic method development and validation for quantification of trifarotene in pure and topical drug product","authors":"Muhammad Usman,&nbsp;Muhammad Bilal Shafique","doi":"10.1186/s43094-024-00683-5","DOIUrl":"10.1186/s43094-024-00683-5","url":null,"abstract":"<div><h3>Background</h3><p>Trifarotene is effective for treating acne and other skin issues. To ensure its quality and meet regulatory standards, a reverse phase liquid chromatography (RP-LC) stability-indicating method was developed and validated for its quantification in pure and topical dosage forms. An isocratic elution chromatographic method was employed, using an octadecylsilyl silica gel-packed column (150 mm × 4.6 mm, 3 µm particle size). The mobile phase was a mixture of phosphate buffer and acetonitrile (40:60 v/v). Chromatographic conditions included a flow rate of 0.5 mL/min, column temperature of 40 °C, detection at 265 nm, and injection volume of 20 µL.</p><h3>Results</h3><p>The developed analytical method reports the retention time of trifarotene 11.2 min, higher theoretical plate count, asymmetric peak, and good resolution between the peaks of trifarotene, phenoxyethanol, and environmentally generated impurities.</p><h3>Conclusion</h3><p>The analytical method has been found to be linear, accurate, robust, specific, and selective for impurities produced during forced degradation studies. The proposed analytical method can be utilized for routine pharmaceutical analysis of trifarotene to judge its quality and safety.</p></div>","PeriodicalId":577,"journal":{"name":"Future Journal of Pharmaceutical Sciences","volume":"10 1","pages":""},"PeriodicalIF":3.4,"publicationDate":"2024-08-20","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://fjps.springeropen.com/counter/pdf/10.1186/s43094-024-00683-5","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142013469","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Chemical profile, antioxidant and anti-Alzheimer activity of leaves and flowers of Markhamia lutea cultivated in Egypt: in vitro and in silico studies 埃及栽培的马钱子叶和花的化学成分、抗氧化性和抗老年痴呆活性:体外和硅学研究
IF 3.4 Q2 PHARMACOLOGY & PHARMACY Pub Date : 2024-08-19 DOI: 10.1186/s43094-024-00679-1
Mai Magdy, Ahmed H. Elosaily, Engy Mohsen, Hala M. EL Hefnawy

Background

Nowadays Alzheimer’s disease and its treatment methods are global concerns. Patients with this disease have poor prognosis and need supportive treatment. The antioxidant activity, anti-acetylcholinesterase (anti-AChE), anti-butyryl cholinesterase (anti-BChE) and Aβ-amyloid-42 inhibition activities of the ethanolic extracts of both leaves and flowers (LEE and FEE) of Markhamia lutea were assessed. The antioxidant activity of LEE and FEE was evaluated using 2,2-diphenyl-1-picryl-hydrazyl-hydrate, oxygen radical absorbance capacity and ferrozine iron metal chelation assays. Additionally, their total flavonoids and total phenolics were determined. The phytochemicals of LEE were analysed using LC–MS/Q-TOF in both positive and negative modes. Also, molecular docking was done for phytochemicals identified in LEE.

Result

LEE exhibited higher antioxidant and anti-Alzheimer activities in all techniques due to its high flavonoids content. LEE showed better activity than donepezil in case of anti-butyryl cholinesterase than both donepezil and rivastigmine in case of Aβ-amyloid-42 inhibition. A total of 62 compounds were tentatively identified using Ultra-performance Liquid Chromatography-Electrospray Ionization-Quadrupole Time-of-Flight Mass Spectrometry (UHPLC–ESI–TOF–MS), viz. 35 flavonoids, 11 phenolic acids, 2 terpenoids, 2 phenylpropanoids derivatives, 7 polyphenols, 3 coumarins and 2 organic acids. The molecular docking of some constituents showed that isorhamnetin-O-rutinoside, sissotrin, 3,5,7-trihydroxy-4'-methoxyflavone (diosmetin), rosmarinic acid, kaempferol hexoside, kampferol-7-neohesperoside, acacetin, taxifolin and apigenin-O-hexoside exert a promising activity as anti-Alzheimer drugs.

Conclusion

The LEE of Markhamia lutea contains secondary metabolites that is promising to act as natural antioxidants, acetylcholinesterase, butyryl cholinesterase and Aβ-amyloid-42 inhibition inhibitors, which can aid in the treatment of Alzheimer’s.

Graphical Abstract

背景如今,阿尔茨海默病及其治疗方法已成为全球关注的问题。阿尔茨海默病患者预后较差,需要支持性治疗。本研究评估了马钱子叶和花乙醇提取物(LEE 和 FEE)的抗氧化活性、抗乙酰胆碱酯酶(anti-AChE)、抗丁酰胆碱酯酶(anti-BChE)和 Aβ-淀粉样蛋白-42抑制活性。使用 2,2-二苯基-1-苦基肼水合物、氧自由基吸收能力和铁嗪铁金属螯合试验评估了 LEE 和 FEE 的抗氧化活性。此外,还测定了它们的总黄酮和总酚。采用 LC-MS/Q-TOF 正、负离子模式分析了 LEE 的植物化学成分。结果 由于黄酮类化合物含量高,LEE 在所有技术中都表现出较高的抗氧化和抗老年痴呆活性。在抑制 Aβ-淀粉样蛋白-42 方面,LEE 比多奈哌齐和利巴斯的明在抑制丁酰胆碱酯酶方面表现出更好的活性。利用超高效液相色谱-电喷雾离子化-四极杆飞行时间质谱法(UHPLC-ESI-TOF-MS)初步鉴定出 62 种化合物,即 35 种黄酮类化合物、11 种酚酸类化合物、2 种萜类化合物、2 种苯丙类衍生物、7 种多酚类化合物、3 种香豆素类化合物和 2 种有机酸类化合物。部分成分的分子对接研究表明,异鼠李素-O-芸香糖苷、西索特林、3,5,7-三羟基-4'-甲氧基黄酮(diosmetin)、迷迭香酸、山柰酚六糖苷、山柰酚-7-新橙皮苷、醋酸苷、紫杉叶素和芹菜素-O-六糖苷具有抗老年痴呆药物的活性。结论马钱子鳞叶中的次生代谢物有望成为天然抗氧化剂、乙酰胆碱酯酶、丁酰胆碱酯酶和 Aβ-淀粉样蛋白-42抑制剂,有助于治疗阿尔茨海默氏症。
{"title":"Chemical profile, antioxidant and anti-Alzheimer activity of leaves and flowers of Markhamia lutea cultivated in Egypt: in vitro and in silico studies","authors":"Mai Magdy,&nbsp;Ahmed H. Elosaily,&nbsp;Engy Mohsen,&nbsp;Hala M. EL Hefnawy","doi":"10.1186/s43094-024-00679-1","DOIUrl":"10.1186/s43094-024-00679-1","url":null,"abstract":"<div><h3>Background</h3><p>Nowadays Alzheimer’s disease and its treatment methods are global concerns. Patients with this disease have poor prognosis and need supportive treatment. The antioxidant activity, anti-acetylcholinesterase (anti-AChE), anti-butyryl cholinesterase (anti-BChE) and Aβ-amyloid-42 inhibition activities of the ethanolic extracts of both leaves and flowers (LEE and FEE) of <i>Markhamia lutea</i> were assessed. The antioxidant activity of LEE and FEE was evaluated using 2,2-diphenyl-1-picryl-hydrazyl-hydrate, oxygen radical absorbance capacity and ferrozine iron metal chelation assays. Additionally, their total flavonoids and total phenolics were determined. The phytochemicals of LEE were analysed using LC–MS/Q-TOF in both positive and negative modes. Also, molecular docking was done for phytochemicals identified in LEE.</p><h3>Result</h3><p>LEE exhibited higher antioxidant and anti-Alzheimer activities in all techniques due to its high flavonoids content. LEE showed better activity than donepezil in case of anti-butyryl cholinesterase than both donepezil and rivastigmine in case of Aβ-amyloid-42 inhibition. A total of 62 compounds were tentatively identified using Ultra-performance Liquid Chromatography-Electrospray Ionization-Quadrupole Time-of-Flight Mass Spectrometry (UHPLC–ESI–TOF–MS), viz. 35 flavonoids, 11 phenolic acids, 2 terpenoids, 2 phenylpropanoids derivatives, 7 polyphenols, 3 coumarins and 2 organic acids. The molecular docking of some constituents showed that isorhamnetin-<i>O</i>-rutinoside, sissotrin, 3,5,7-trihydroxy-4'-methoxyflavone (diosmetin), rosmarinic acid, kaempferol hexoside, kampferol-7-neohesperoside, acacetin, taxifolin and apigenin-<i>O</i>-hexoside exert a promising activity as anti-Alzheimer drugs.</p><h3>Conclusion</h3><p>The LEE of <i>Markhamia lutea</i> contains secondary metabolites that is promising to act as natural antioxidants, acetylcholinesterase, butyryl cholinesterase and Aβ-amyloid-42 inhibition inhibitors, which can aid in the treatment of Alzheimer’s.</p><h3>Graphical Abstract</h3><div><figure><div><div><picture><source><img></source></picture></div></div></figure></div></div>","PeriodicalId":577,"journal":{"name":"Future Journal of Pharmaceutical Sciences","volume":"10 1","pages":""},"PeriodicalIF":3.4,"publicationDate":"2024-08-19","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://fjps.springeropen.com/counter/pdf/10.1186/s43094-024-00679-1","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142002568","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
期刊
Future Journal of Pharmaceutical Sciences
全部 Acc. Chem. Res. ACS Applied Bio Materials ACS Appl. Electron. Mater. ACS Appl. Energy Mater. ACS Appl. Mater. Interfaces ACS Appl. Nano Mater. ACS Appl. Polym. Mater. ACS BIOMATER-SCI ENG ACS Catal. ACS Cent. Sci. ACS Chem. Biol. ACS Chemical Health & Safety ACS Chem. Neurosci. ACS Comb. Sci. ACS Earth Space Chem. ACS Energy Lett. ACS Infect. Dis. ACS Macro Lett. ACS Mater. Lett. ACS Med. Chem. Lett. ACS Nano ACS Omega ACS Photonics ACS Sens. ACS Sustainable Chem. Eng. ACS Synth. Biol. Anal. Chem. BIOCHEMISTRY-US Bioconjugate Chem. BIOMACROMOLECULES Chem. Res. Toxicol. Chem. Rev. Chem. Mater. CRYST GROWTH DES ENERG FUEL Environ. Sci. Technol. Environ. Sci. Technol. Lett. Eur. J. Inorg. Chem. IND ENG CHEM RES Inorg. Chem. J. Agric. Food. Chem. J. Chem. Eng. Data J. Chem. Educ. J. Chem. Inf. Model. J. Chem. Theory Comput. J. Med. Chem. J. Nat. Prod. J PROTEOME RES J. Am. Chem. Soc. LANGMUIR MACROMOLECULES Mol. Pharmaceutics Nano Lett. Org. Lett. ORG PROCESS RES DEV ORGANOMETALLICS J. Org. Chem. J. Phys. Chem. J. Phys. Chem. A J. Phys. Chem. B J. Phys. Chem. C J. Phys. Chem. Lett. Analyst Anal. Methods Biomater. Sci. Catal. Sci. Technol. Chem. Commun. Chem. Soc. Rev. CHEM EDUC RES PRACT CRYSTENGCOMM Dalton Trans. Energy Environ. Sci. ENVIRON SCI-NANO ENVIRON SCI-PROC IMP ENVIRON SCI-WAT RES Faraday Discuss. Food Funct. Green Chem. Inorg. Chem. Front. Integr. Biol. J. Anal. At. Spectrom. J. Mater. Chem. A J. Mater. Chem. B J. Mater. Chem. C Lab Chip Mater. Chem. Front. Mater. Horiz. MEDCHEMCOMM Metallomics Mol. Biosyst. Mol. Syst. Des. Eng. Nanoscale Nanoscale Horiz. Nat. Prod. Rep. New J. Chem. Org. Biomol. Chem. Org. Chem. Front. PHOTOCH PHOTOBIO SCI PCCP Polym. Chem.
×
引用
GB/T 7714-2015
复制
MLA
复制
APA
复制
导出至
BibTeX EndNote RefMan NoteFirst NoteExpress
×
0
微信
客服QQ
Book学术公众号 扫码关注我们
反馈
×
意见反馈
请填写您的意见或建议
请填写您的手机或邮箱
×
提示
您的信息不完整,为了账户安全,请先补充。
现在去补充
×
提示
您因"违规操作"
具体请查看互助需知
我知道了
×
提示
现在去查看 取消
×
提示
确定
Book学术官方微信
Book学术文献互助
Book学术文献互助群
群 号:481959085
Book学术
文献互助 智能选刊 最新文献 互助须知 联系我们:info@booksci.cn
Book学术提供免费学术资源搜索服务,方便国内外学者检索中英文文献。致力于提供最便捷和优质的服务体验。
Copyright © 2023 Book学术 All rights reserved.
ghs 京公网安备 11010802042870号 京ICP备2023020795号-1