Pub Date : 2024-09-02DOI: 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.
{"title":"Novel paradigm of therapeutic intervention for skin cancer: challenges and opportunities","authors":"Modassir Nasim, Mariya Khan, Rabea Parveen, Azka Gull, Saba Khan, 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}
Pub Date : 2024-09-02DOI: 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.
{"title":"Healthcare providers' perspectives on corticosteroid-containing drugs: a cross-sectional study in the United Arab Emirates","authors":"Muna Barakat, Diana Malaeb, Ahmad El Ouweini, Salah Aburuz, Sham ZainAlabdin, Omar El Khatib, Bassem Sadek, Razan I. Nassar, 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}
Pub Date : 2024-08-28DOI: 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.
{"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, Siddhartha Dan, 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}
Pub Date : 2024-08-28DOI: 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, Vaibhavi K. Salunkhe, Shubham D. Tabade, Pragati K. Bhonde, Sarthak G. Kulkarni, Dnyaneshwar H. Maykar, Saurabh B. Ganorkar, Sanjay J, Surana, 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}
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.
{"title":"Identification and characterization of phytochemicals in methanolic extract of roots of Datura fastuosa using various techniques","authors":"Girma Mengesha Melese, Tewodros Brihanu Aychiluhim, Abdurrahman Mengesha Yessuf, 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}
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. Tinosporacordifolia 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.
{"title":"α-Amylase, α-glucosidase and aldose reductase inhibitory and molecular docking studies on Tinospora cordifolia (Guduchi) leaf extract","authors":"Hemlata Janardhan Bhosale, Shailesh Vaijeenath Mamdapure, Ramdas Balaji Panchal, 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}
Pub Date : 2024-08-22DOI: 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.
{"title":"Antioxidants as adjuvant therapy in the treatment of community-acquired pneumonia","authors":"Fatma Makram Youssef, Eman Mohamed Elmokadem, Amir Eskander Hanna Samy, 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}
Pub Date : 2024-08-21DOI: 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.
{"title":"Enhanced viability of Lactobacillus spp. via encapsulation in hyaluronan/PVA hybrid electrospun composites for vaginal drug delivery","authors":"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","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}
Pub Date : 2024-08-20DOI: 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.
{"title":"Stability-indicating liquid chromatographic method development and validation for quantification of trifarotene in pure and topical drug product","authors":"Muhammad Usman, 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}
Pub Date : 2024-08-19DOI: 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.
{"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, Ahmed H. Elosaily, Engy Mohsen, 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}