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Development of nanoparticles for the Novel anticancer therapeutic agents for Acute Myeloid Leukemia 新型急性髓系白血病抗癌药物纳米颗粒的研制
Pub Date : 2023-07-31 DOI: 10.37285/ijpsn.2023.16.4.7
Ajay Bhagwat, Rohit Doke Doke, Santosh Ghule, Bipin Gandhi
Acute myeloid leukaemia is becoming more predominant in blood cancer in geriatrics people groups. In 2017, four new therapeutic candidates have been approved by the FDA: Enasidenib, CPX 351, Midostaurin, and Gemtuzumab ozogamicin; with the approval of Venetoclax and Daurismo, additional advances were achieved in 2018. Ivosidenib and gilteritinib were also accepted as single-agent therapy in persistent and recurrent AML 2018. Most of the anticancer drugs belong to Biopharmaceutical classification system-II (BSC), and BCS class-IV has poor bioavailability because of solubility issues. We will overcome this problem by preparing nanoparticles of this drug by using different nanoparticle preparation methods.
急性髓性白血病在老年人群的血癌中越来越占优势。2017年,FDA批准了四种新的候选治疗药物:Enasidenib、CPX 351、midoshuin和Gemtuzumab ozogamicin;随着Venetoclax和Daurismo的批准,2018年取得了额外的进展。Ivosidenib和gilteritinib也被接受为持续和复发性AML 2018的单药治疗。大多数抗癌药物属于生物制药分类系统ii (BSC), BCS iv类由于溶解度问题,生物利用度较差。我们将通过使用不同的纳米颗粒制备方法制备该药物的纳米颗粒来克服这一问题。
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引用次数: 0
RP-HPLC Method Development for Estimation of Diclofenac Diethylamine Topical Solution 反相高效液相色谱法测定双氯芬酸二乙胺外用溶液的含量
Pub Date : 2023-07-31 DOI: 10.37285/ijpsn.2023.16.4.4
Sejal H Dhaduk, Nilesh K Patel, Jaivik H Modh, Amitkumar J Vyas, Ajay I Patel
Objective: A simple, rapid, precise, and reproducible RP-HPLC method development and validation for estimation of Diclofenac Diethylamine in Topical Solution. Experimental condition: The method was developed using Kromasil C8 (150 mm × 4.6 mm, 5 µm) column. Mobile phase composition was Buffer: Methanol (25:75 %V/V) (Buffer-1.37 g of NaH2PO4 in 1000 ml adjust pH 2.5 ± 0.05 with OPA.), flow rate 1 ml/min and detection carried out at 254 nm at column temperature 40ºC. The injection volume was 10µl with run time of 10 minutes. Diluent used was Methanol: Water (50:50 % V/V). Results: The retention time for Diclofenac Diethylamine was found 5.26 minute. Method found linear in the range of 50-150 µg/ml (r2 = 0.9998). Percentage Recovery was 100.5-100.9 %. The RSD for Diclofenac Diethylamine are less than 2 for precision, specificity, robustness respectively. Conclusion: A simple and rapid RP-HPLC method was developed for the estimation of Diclofenac Diethylamine in pure API and Topical formulation. The method was validated as per ICH guideline and statistical data confirmed Specificity, Linearity, Accuracy, Precision and Robustness of proposed method.
目的:建立一种简便、快速、精确、重现性好的反相高效液相色谱法测定外用溶液中双氯芬酸二乙胺的含量。实验条件:色谱柱为Kromasil C8 (150 mm × 4.6 mm, 5µm)。流动相组成为Buffer:甲醇(25:75 %V/V) (Buffer-1.37 g NaH2PO4 in 1000 ml调节pH 2.5±0.05与OPA),流速1 ml/min,柱温40℃,254 nm检测。进样量为10µl,运行时间为10分钟。稀释剂为甲醇:水(50:50 % V/V);结果:双氯芬酸二乙胺的保留时间为5.26 min。方法在50 ~ 150µg/ml范围内呈线性关系(r2 = 0.9998)。回收率为100.5 ~ 100.9%。双氯芬酸二乙胺的精密度、特异性、稳健性的RSD均小于2。结论:建立了一种简便、快速的双氯芬酸二乙胺原料药和外用制剂中双氯芬酸二乙胺含量测定方法。根据ICH指南对该方法进行了验证,统计数据证实了该方法的专属性、线性度、准确度、精密度和稳健性。
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 Experimental condition: The method was developed using Kromasil C8 (150 mm × 4.6 mm, 5 µm) column. Mobile phase composition was Buffer: Methanol (25:75 %V/V) (Buffer-1.37 g of NaH2PO4 in 1000 ml adjust pH 2.5 ± 0.05 with OPA.), flow rate 1 ml/min and detection carried out at 254 nm at column temperature 40ºC. The injection volume was 10µl with run time of 10 minutes. Diluent used was Methanol: Water (50:50 % V/V).
 Results: The retention time for Diclofenac Diethylamine was found 5.26 minute. Method found linear in the range of 50-150 µg/ml (r2 = 0.9998). Percentage Recovery was 100.5-100.9 %. The RSD for Diclofenac Diethylamine are less than 2 for precision, specificity, robustness respectively.
 Conclusion: A simple and rapid RP-HPLC method was developed for the estimation of Diclofenac Diethylamine in pure API and Topical formulation. The method was validated as per ICH guideline and statistical data confirmed Specificity, Linearity, Accuracy, Precision and Robustness of proposed method.","PeriodicalId":14382,"journal":{"name":"International Journal of Pharmaceutical Sciences and Nanotechnology","volume":"12 1","pages":"0"},"PeriodicalIF":0.0,"publicationDate":"2023-07-31","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"135357927","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Application of Nanotechnology in Malaria Research 纳米技术在疟疾研究中的应用
Pub Date : 2023-07-31 DOI: 10.37285/ijpsn.2023.16.4.1
None Bikash Medhi, Varun Gorki
Introduction In many ways, malaria is giving a challenge to researchers globally, day by day. But, the potential of nanotechnology/nanomedicine to work at the nanoscale has allowed us to target receptors/molecules of the parasite directly at a nanoscale level as well as the impetus to develop devious nanostructures that could solve the problems which previously impeded the conventional pharmacological approaches from being successful. Over the four decades, the slow but steady integration of life-sciences disciplines and nanotechnology has started transforming the way to detect and diagnose for the betterment of health1. This idea was first presented in 1974 by Professor Norio Taniguchi2, and it received the least attention concerning malaria. However, drug resistance, social demerits, and environmental concerns made malaria the exterminator and notorious disease that is known to all. The mainstay of current anti-plasmodial medication is chemotherapy, which comes with toxic severe side effects. Resistance among the parasite spp. that leads to treatment failure, insufficient knowledge of the biology and pathology of a parasite, complexity of life-cycle, dispersed locations of Plasmodium spp., and the difficulty in developing new antimalarial drugs as this development process is time-consuming and an expensive, poses a significant challenge when researchers are trying to create new antimalarial medications3. Therefore, researchers are trying to deliver drugs without toxicity and improve efficacy4 by employing nanotechnological approaches. It enhances its solubility profile, modifies the pharmacokinetic characteristics of the drug, prevents drug deterioration, and supports a continuous release of the drug at the intended site.
在许多方面,疟疾每天都给全球的研究人员带来挑战。但是,纳米技术/纳米医学在纳米尺度上工作的潜力使我们能够在纳米尺度上直接靶向寄生虫的受体/分子,同时也推动了开发迂回的纳米结构的动力,这些纳米结构可以解决以前阻碍传统药理学方法成功的问题。在过去的四十年里,生命科学学科和纳米技术缓慢而稳定的融合已经开始改变检测和诊断的方式,以改善健康。这一观点最早是由谷口典夫教授于1974年提出的,但在疟疾方面受到的关注最少。然而,耐药性、社会弊端和环境问题使疟疾成为众所周知的灭虫者和臭名昭著的疾病。目前主要的抗疟原虫药物是化疗,它有严重的副作用。疟原虫之间的耐药性导致治疗失败,对疟原虫的生物学和病理学认识不足,生命周期的复杂性,疟原虫分布的分散位置,以及开发新的抗疟药物的困难(这一开发过程耗时且昂贵),这些都给试图开发新的抗疟药物的研究人员带来了重大挑战。因此,研究人员正试图采用纳米技术方法,使药物无毒性并提高疗效。它增强其溶解度,改变药物的药代动力学特性,防止药物变质,并支持药物在预期部位的连续释放。
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引用次数: 0
Compositional and Functional Characteristics of Camel Milk: Evidence Based Review 骆驼奶的成分和功能特征:基于证据的综述
Pub Date : 2023-07-31 DOI: 10.37285/ijpsn.2023.16.4.9
Dr. Saumya Das, Avijit Mazumder, Anchit Dogra, Avinash Jha
Camel milk (CM) has been demonstrated to be effective in treating a broad range of illnesses. Camel's milk is regarded to have therapeutic properties because of its unique composition. Some people consider CM to be a precious commodity. White CM is made by combining fat and water. Several clinical studies have shown that CM effectively treats various diseases, including chronic ones. Most of the medicinal advantages of CM are included in this study. CM ingredients and qualities are similar to those found in mother's milk, making it superior to cow's milk. Insulin-like and protective proteins are found in abundance, along with lactose, which is the primary carbohydrate. It has anti-tumour qualities, and the robust immune system components assist in combatting disorders, including diabetes, autism, and diarrhoea. It has been used by Nomads and Bedouins (Arabian tribal) for millennia because of these properties.
骆驼奶(CM)已被证明对治疗多种疾病有效。骆驼奶因其独特的成分而被认为具有治疗作用。有些人认为CM是一种珍贵的商品。白色CM是由脂肪和水结合而成。几项临床研究表明,CM有效治疗多种疾病,包括慢性疾病。CM的大部分药用优势都包含在本研究中。CM的成分和品质与母乳中的成分和品质相似,使其优于牛奶。胰岛素样蛋白质和保护性蛋白质丰富,还有乳糖,这是主要的碳水化合物。它具有抗肿瘤的特性,强大的免疫系统成分有助于对抗疾病,包括糖尿病、自闭症和腹泻。由于这些特性,它已经被游牧民族和贝都因人(阿拉伯部落)使用了几千年。
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引用次数: 0
A Review on Capsaicin-Methods of Extraction, Estimation and Therapeutic Effects 辣椒素的研究进展——提取方法、评价及疗效评价
Pub Date : 2023-07-31 DOI: 10.37285/ijpsn.2023.16.4.6
Sujitha Muvva, Siva Prasad M, Prachet P, Rama Rao N
The capsaicin alkaloid is the secondary metabolite present in the fruits of Capsicum annum, which belongs to the family Solanaceae. Capsaicin and dihydrocapsaicin constitute 50% of the capsaicinoids in Capsicum annum. The present article describes methods for extracting Capsaicin, like soxhlation, microwave-assisted extraction(MAE), ultrasonication, and supercritical fluid extraction. Also, different analytical methods for estimating Capsaicin are specified, including spectroscopic and chromatographic methods and hyphenated techniques, and the best approach is described. Microwave-assisted extraction of Capsaicin at a temperature of 120ºC and the solid-liquid ratio of 25mg/mL for 90 min yields 3.85% of Capsaicin, the most suitable and easy method for extracting Capsaicin. The best way for estimating Capsaicin is to use a GC-MS method with EI ionization at 70 eV and a column of 5% diphenyl, 95% dimethylpolysiloxane, 30 m x 0.25 mm, using helium as the mobile phase at a flow rate of 1.61 mL/min at a column temperature of 60ºC and injector temperature of 250ºC. Capsaicin has many pharmacological effects like anti-cancer, antidiabetic, antioxidant, antimicrobial, etc., which are also discussed in this article.
辣椒素生物碱是辣椒科植物辣椒果实中的次生代谢产物。辣椒素和二氢辣椒素占辣椒素类物质的50%。本文介绍了辣椒素的提取方法,包括草酸法、微波辅助提取法、超声波提取法和超临界流体提取法。同时,对辣椒素的分析方法进行了详细介绍,包括光谱法、色谱法和联用法,并对最佳方法进行了描述。微波辅助提取辣椒素的条件为:温度120℃,料液比25mg/mL,提取90 min,辣椒素得率为3.85%,是提取辣椒素最适宜、最简便的方法。测定辣椒素的最佳方法是采用气相色谱-质谱法,EI电离70 eV,色谱柱为5%二苯基,95%二甲基聚硅氧烷,30 m x 0.25 mm,以氦气为流动相,流速为1.61 mL/min,柱温为60℃,进样温度为250℃。辣椒素具有抗癌、抗糖尿病、抗氧化、抗菌等药理作用,本文也对其进行了讨论。
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引用次数: 0
Recent Advancement of Microneedle Technique in Diagnosis and Therapy of Diseases 微针技术在疾病诊断和治疗中的最新进展
Pub Date : 2023-07-31 DOI: 10.37285/ijpsn.2023.16.4.8
Abhishek Kanugo
The therapeutic efficacy and safety of active ingredients are limited in several dosage forms, especially for those where the skin is the prime application area. Injectable has the potential of high efficacy and bioavailability but needle phobia, painful delivery, inflammatory response, and non-compliance make them less usable. Microneedle (MN) delivery overcomes almost all the limitations by offering painless self-administration, is highly effective, economical, avoids waste generation, and has high patient compliance. The MN technique is unique and novel for delivering all therapeutic moieties, vaccines, and micro and macromolecular drugs. The MN delivery is based on the mechanism of poke and patch, coat and patch, poke and release, poke and flow. The several types of MN utilized are solid, coated, hollow, dissolving, and hydrogel-forming microneedles. The materials fabricating MNs are mainly non-degradable (metals, PVP, PVA, etc.) and degradable (natural, PLGA, PAMA, etc.). MN delivery finds significant application in diagnosing several diseases by collecting blood samples and biological fluids with minimal pain. Moreover, the tremendous significance of the MN technique is observed in vaccines, hormones, proteins, peptides, psoriasis, ocular diseases, rheumatoid arthritis, malaria, gene delivery, and cosmetics. The delivery of several kinds of injections in cancer therapy is also harrowing. MN delivery worked excellently by delivering immunotherapeutic, immune checkpoint suppressors, photothermal therapy, and photodynamic therapy and thus valuable for targeting cancer with high success and minimal toxicity.
活性成分的治疗效果和安全性在几种剂型中是有限的,特别是对于那些皮肤是主要应用区域的人。注射剂具有高效率和生物利用度的潜力,但针头恐惧症、递送疼痛、炎症反应和不依从性使其不太可用。微针(MN)通过提供无痛的自我给药,克服了几乎所有的限制,是非常有效的,经济的,避免浪费的产生,并有很高的患者依从性。MN技术是一种独特而新颖的技术,可用于输送所有治疗成分、疫苗以及微分子和大分子药物。MN的输送是基于戳与贴、涂与贴、戳与释放、戳与流的机制。所使用的几种类型的锰是固体,涂层,空心,溶解和水凝胶形成微针。制造纳米粒子的材料主要是不可降解的(金属、PVP、PVA等)和可降解的(天然、PLGA、PAMA等)。通过收集血液样本和生物液体,在最小疼痛的情况下,MN递送在诊断几种疾病方面具有重要应用。此外,MN技术在疫苗、激素、蛋白质、多肽、牛皮癣、眼部疾病、类风湿关节炎、疟疾、基因传递和化妆品等领域的巨大意义也被观察到。癌症治疗中几种注射剂的使用也令人痛苦。通过免疫疗法、免疫检查点抑制剂、光热疗法和光动力疗法,MN的递送效果非常好,因此对于靶向癌症具有很高的成功率和最小的毒性。
{"title":"Recent Advancement of Microneedle Technique in Diagnosis and Therapy of Diseases","authors":"Abhishek Kanugo","doi":"10.37285/ijpsn.2023.16.4.8","DOIUrl":"https://doi.org/10.37285/ijpsn.2023.16.4.8","url":null,"abstract":"The therapeutic efficacy and safety of active ingredients are limited in several dosage forms, especially for those where the skin is the prime application area. Injectable has the potential of high efficacy and bioavailability but needle phobia, painful delivery, inflammatory response, and non-compliance make them less usable. Microneedle (MN) delivery overcomes almost all the limitations by offering painless self-administration, is highly effective, economical, avoids waste generation, and has high patient compliance. The MN technique is unique and novel for delivering all therapeutic moieties, vaccines, and micro and macromolecular drugs. The MN delivery is based on the mechanism of poke and patch, coat and patch, poke and release, poke and flow. The several types of MN utilized are solid, coated, hollow, dissolving, and hydrogel-forming microneedles. The materials fabricating MNs are mainly non-degradable (metals, PVP, PVA, etc.) and degradable (natural, PLGA, PAMA, etc.). MN delivery finds significant application in diagnosing several diseases by collecting blood samples and biological fluids with minimal pain. Moreover, the tremendous significance of the MN technique is observed in vaccines, hormones, proteins, peptides, psoriasis, ocular diseases, rheumatoid arthritis, malaria, gene delivery, and cosmetics. The delivery of several kinds of injections in cancer therapy is also harrowing. MN delivery worked excellently by delivering immunotherapeutic, immune checkpoint suppressors, photothermal therapy, and photodynamic therapy and thus valuable for targeting cancer with high success and minimal toxicity.","PeriodicalId":14382,"journal":{"name":"International Journal of Pharmaceutical Sciences and Nanotechnology","volume":"3 1","pages":"0"},"PeriodicalIF":0.0,"publicationDate":"2023-07-31","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"135357682","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Phytochemical Screening, Analgesic and Anti-Inflammatory Activity of the Ethanol Extract of the Cnidoscolus Phyllacanthus Leaves 毛刺叶乙醇提取物的植物化学筛选及镇痛抗炎活性研究
Pub Date : 2023-07-31 DOI: 10.37285/ijpsn.2023.16.4.5
None Dr. Gurdeep Singh, None Ritesh Patel, None Mukesh Kr. Singh, None Gaurav Agarwal
Objective: The present study aimed to investigate the analgesic and anti-inflammatory activity of the Cnidoscolus phyllacanthus (family Euphorbiaceae) ethanolic leaves extract in the laboratory using in vivo methods to justify its traditional use in the above-mentioned pathological conditions. Methods: Phytochemical screening was done to find the presence of various secondary metabolites of the plant. In vivo, analgesic activity was performed employing the acetic acid-induced writhing test and tail immersion test on Swiss albino mice at doses of 50, 100 and 200 mg/kg body weight. An anti-inflammatory activity test was done on Wistar rats at three doses (50, 100 and 200 mg/kg body weight) using a carrageenan-induced paw oedema test. Data were analyzed by one-way analysis of variance (ANOVA), and Dunnett's t-test was used as the significance test. P value was considered as the minimum level of significance. Results: Phytochemical screening revealed the presence of coumarin, flavonoids, monoterpenes, diterpenes and naphthoquinones in the extract. In the acetic acid-induced writhing test, the per cent inhibition of writhing response by the extract was 12.82%, 25.64% and 76.67% at 50, 100 and 200 mg/kg doses, respectively (p < 0.01) and showed an increase in pain threshold in tail immersion method. The extract significantly (p < 0.05 and p < 0.01) inhibited carrageenan-induced inflammatory response in rats in a dose-related manner. Per cent, inhibition in paw oedema was 16.39 %, 29.50 % and 52.45 % at 50, 100 and 200 mg/kg doses, respectively. Conclusion: The results obtained from the tests indicate that the plant might have one or more secondary metabolite(s) having central and peripheral analgesic and anti-inflammatory activity.
目的:本研究旨在通过体内实验研究毛刺乙醇叶提取物的镇痛和抗炎活性,以证明其在上述病理条件下的传统使用是合理的。方法:进行植物化学筛选,发现该植物存在多种次生代谢物。在体内,以50、100和200 mg/kg体重剂量的瑞士白化小鼠进行醋酸致扭体实验和尾浸实验,观察其镇痛活性。采用角叉菜胶诱导足跖水肿试验,对Wistar大鼠进行了3种剂量(50、100和200 mg/kg体重)的抗炎活性试验。数据分析采用单因素方差分析(ANOVA),显著性检验采用Dunnett’st检验。P值为最低显著性水平。结果:植物化学筛选结果显示,提取物中含有香豆素、黄酮类化合物、单萜、二萜和萘醌类化合物。在醋酸诱导扭体实验中,50、100和200 mg/kg剂量下,提取物对扭体反应的抑制率分别为12.82%、25.64%和76.67% (p <0.01),且尾浸法疼痛阈值升高。提取物显著(p <0.05和p <0.01)抑制大鼠角叉菜胶诱导的炎症反应呈剂量相关。在50、100和200 mg/kg剂量下,对足跖水肿的抑制作用分别为16.39%、29.50%和52.45%。结论:实验结果表明,该植物可能具有一种或多种具有中枢和外周镇痛和抗炎活性的次级代谢物。
{"title":"Phytochemical Screening, Analgesic and Anti-Inflammatory Activity of the Ethanol Extract of the Cnidoscolus Phyllacanthus Leaves","authors":"None Dr. Gurdeep Singh, None Ritesh Patel, None Mukesh Kr. Singh, None Gaurav Agarwal","doi":"10.37285/ijpsn.2023.16.4.5","DOIUrl":"https://doi.org/10.37285/ijpsn.2023.16.4.5","url":null,"abstract":"Objective: The present study aimed to investigate the analgesic and anti-inflammatory activity of the Cnidoscolus phyllacanthus (family Euphorbiaceae) ethanolic leaves extract in the laboratory using in vivo methods to justify its traditional use in the above-mentioned pathological conditions. Methods: Phytochemical screening was done to find the presence of various secondary metabolites of the plant. In vivo, analgesic activity was performed employing the acetic acid-induced writhing test and tail immersion test on Swiss albino mice at doses of 50, 100 and 200 mg/kg body weight. An anti-inflammatory activity test was done on Wistar rats at three doses (50, 100 and 200 mg/kg body weight) using a carrageenan-induced paw oedema test. Data were analyzed by one-way analysis of variance (ANOVA), and Dunnett's t-test was used as the significance test. P value was considered as the minimum level of significance. Results: Phytochemical screening revealed the presence of coumarin, flavonoids, monoterpenes, diterpenes and naphthoquinones in the extract. In the acetic acid-induced writhing test, the per cent inhibition of writhing response by the extract was 12.82%, 25.64% and 76.67% at 50, 100 and 200 mg/kg doses, respectively (p < 0.01) and showed an increase in pain threshold in tail immersion method. The extract significantly (p < 0.05 and p < 0.01) inhibited carrageenan-induced inflammatory response in rats in a dose-related manner. Per cent, inhibition in paw oedema was 16.39 %, 29.50 % and 52.45 % at 50, 100 and 200 mg/kg doses, respectively. Conclusion: The results obtained from the tests indicate that the plant might have one or more secondary metabolite(s) having central and peripheral analgesic and anti-inflammatory activity.","PeriodicalId":14382,"journal":{"name":"International Journal of Pharmaceutical Sciences and Nanotechnology","volume":"8 1","pages":"0"},"PeriodicalIF":0.0,"publicationDate":"2023-07-31","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"135357923","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Investigation of In-Vitro Antidiabetic Study, Antioxidant Activity and Anthelminthic Property of Various Extracts of Bitter Cumin Seeds 苦孜然种子各种提取物体外抗糖尿病研究、抗氧化活性及驱虫性研究
Pub Date : 2023-07-31 DOI: 10.37285/ijpsn.2023.16.4.3
Vedanshu Malviya
Background Bitter cumin (Centratherum anthelminticum (L.)) is a significant restorative plant. We examined the phenolic compounds, and antioxidants, hostile to hyperglycemic and anthelmintic properties of bitter cumin extracts in different in vitro models. Methods: Bitter cumin seeds were extracted with various solvents in their rising request of extremity, which incorporates chloroform, ethyl acetate, methanol, ethanol, and distilled water. The -amylase test and glucose take-up measure by yeast were used for the assessment of the antidiabetic property. Antioxidant agent actions of bitter cumin extricate were described in different in vitro model frameworks, for example, DPPH Scavenging Effect, Ferric-Reducing Antioxidant Power, and Metal-Chelating Capacity. Phenolic content was likewise assessed and, in conclusion, the in vitro anthelmintic review was completed by utilizing Phertima posthuma. Results: The antidiabetic property of the different concentrates of bitter cumin uncovered the best action from the fluid concentrate by α-amylase action with a hindrance worth of 39.2830±0.80725%. While the investigation of glucose take-up by yeast cells was the most noteworthy, the restraint worth of the watery concentrate was the most noteworthy at 49.8100±0.62476%. The different concentrates of bitter cumin in an in-vitro study showed important properties of DPPH Ferric-Reducing Antioxidant Power and Metal-Chelating Capacity. The outcomes showed an immediate relationship between phenolic correlation substances and cell reinforcement action. The anthelmintic review uncovered that the fluid concentrate from the wide range of various concentrates was having the most incredible in-vitro action, which uncovered that the time required was 3.52±0.158 min for the loss of motility and 2.74±0.247 min for the death of the earthworms. Conclusion: The exploratory proof obtained in the laboratory model could give a reason for the conventional utilization of this seed as an antidiabetic, cell-protective, and anthelmintic. Our discoveries affirm that the customary restorative cases for this seed in the not-so-distant future certainly have the option to supplant the manufactured medications to which there is an increased occurrence of medication, increased incidence of drug interactions, and drug resistance.
背景# x0D;苦孜然(Centratherum anthelminticum, L.)是一种重要的恢复性植物。我们在不同的体外模型中检测苦孜然提取物的酚类化合物、抗氧化剂、抗高血糖和驱虫药特性。 方法:& # x0D;用氯仿、乙酸乙酯、甲醇、乙醇、蒸馏水等不同溶剂对苦孜然种子进行萃取。采用-淀粉酶试验和酵母菌对葡萄糖的吸收测定来评价其抗糖尿病性能。在不同的体外模型框架下,对苦孜然提取物的抗氧化剂作用进行了研究,如清除DPPH、还原铁的抗氧化能力和金属螯合能力。对酚类物质含量进行了同样的评估,最后,利用假蜂草(Phertima posthuma)完成了体外驱虫评价。结果:& # x0D;不同苦孜然浓缩液的抗糖尿病性能表明,其α-淀粉酶抑制剂的阻碍值为39.2830±0.80725%。其中,酵母细胞对葡萄糖的摄取最为显著,水样浓缩物的抑制值为49.8100±0.62476%。在体外研究中,苦孜然的不同浓缩物显示出DPPH降铁抗氧化能力和金属螯合能力的重要特性。结果表明,酚类相关物质与细胞增强作用之间存在直接关系。对蚯蚓的研究发现,从各种浓缩物中提取的液体浓缩物具有最令人难以置信的体外作用,这表明蚯蚓失去运动所需的时间为3.52±0.158分钟,死亡所需的时间为2.74±0.247分钟。结论:& # x0D;在实验室模型中获得的探索性证据可以为这种种子作为抗糖尿病、细胞保护和驱虫药的常规利用提供理由。我们的发现证实,在不久的将来,这种种子的习惯恢复性病例肯定有替代药物的选择,因为药物的发生率增加,药物相互作用的发生率增加,耐药性增加。
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引用次数: 0
Formulation Development and Evaluation of Dry Adsorbed Nanoparticles of Curcumin and Piperine Dual Drug Loaded Nanostructured Lipid Carriers 干法吸附姜黄素和胡椒碱双药负载纳米脂质载体的配方开发与评价
Pub Date : 2023-07-31 DOI: 10.37285/ijpsn.2023.16.4.2
Rajashree Hirlekar, Srinivas Bhairy, Alfiha Momin
Purpose: The present study was aimed at preparing stable dry adsorbed nanoparticles (DANs) of curcumin (CUR) and piperine (PIP) loaded nanostructured lipid carriers (NLCs). Methods: CUR and PIP-loaded NLCs (CP NLCs) were prepared by modified hot-melt emulsification using precirol ATO5 (PRE) as solid lipid, labrafac lipophile WL1349 (LAF) as liquid lipid, and a combination of tween 80 (T80) with gelucire 50/13 (G50/13) as surfactants. The NLCs system was subjected to physical stability, particle size, zeta potential, thermal behaviour, crystallinity study and in-vitro drug release. Further, an evaporative drying technique converted the NLC system into stable DANs by adsorbing onto mannitol (Pearlitol 200SD). The DANs were characterized for redispersion properties, particle size, flow properties and in-vitro drug release. The stability studies were carried out for 30 days. Results: The optimized CP NLCs were of imperfect type and had a mean particle size of 248.5 ± 12.8 nm (size distribution of 0.216 ± 0.021), a zeta potential of -9.03 ± 0.53 mV, an entrapment efficiency (EE) of 99.80 ± 0.21% (CUR), 100.05 ± 0.07% (PIP) with a drug recovery of 99.70 ± 0.21% (CUR) and 100.36 ± 0.12% (PIP). The X-ray diffraction pattern and endothermic peaks confirmed the encapsulation of actives in lipid matrices. The in-vitro drug release showed controlled release for 24 h. The optimized DANs led to maximum redispersion and retained a particle size of 268.4 ± 23.1 nm (distribution 0.235 ± 0.037) with controlled release similar to CP NLCs. The CP NLCs DANs showed reasonable stability for 30 days. Conclusions: The developed CP NLCs DANs showed a controlled release profile, and the adsorption technique can be used to improve the stability of NLC dispersion. The DANs can be offered in patient-friendly dosage forms such as sachets, capsules, and compressed tablets.
目的:制备稳定的姜黄素(CUR)和胡椒碱(PIP)干吸附纳米颗粒(dan),负载纳米结构脂质载体(NLCs)。方法:采用改性热熔乳化的方法,以苯胺醇at5 (PRE)为固体脂质,labrafac亲脂剂WL1349 (LAF)为液体脂质,T80 (T80)和胶酰50/13 (G50/13)为表面活性剂,制备CUR和pip负载的NLCs (CP NLCs)。对NLCs系统进行了物理稳定性、粒径、zeta电位、热行为、结晶度和体外药物释放研究。此外,蒸发干燥技术通过吸附甘露醇(珍珠醇200SD)将NLC系统转化为稳定的DANs。对DANs的再分散性能、粒径、流动性能和体外释药性能进行了表征。稳定性研究进行了30天。结果:优化后的CP NLCs为不完善型,平均粒径为248.5±12.8 nm(粒径分布为0.216±0.021),zeta电位为-9.03±0.53 mV,包封效率(EE)分别为99.80±0.21% (CUR)、100.05±0.07% (PIP),药物回收率分别为99.70±0.21% (CUR)和100.36±0.12% (PIP)。x射线衍射图和吸热峰证实了活性物质在脂质基质中的包封。体外控释24 h。优化后的DANs再分散最大,粒径为268.4±23.1 nm(分布为0.235±0.037),控释与CP NLCs相似。CP NLCs DANs在30天内表现出合理的稳定性。结论:所制备的CP NLC分散体具有控释特性,吸附技术可提高NLC分散体的稳定性。DANs可以以患者友好的剂型提供,如小袋、胶囊和压缩片剂。
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引用次数: 0
Formulation Development and Characterization of Vancomycin Hydrochloride Colon-Targeted Tablets Using In-Situ Polyelectrolyte Complexation Technique 原位聚电解质络合技术制备盐酸万古霉素结肠靶向片及表征
Pub Date : 2023-05-31 DOI: 10.37285/ijpsn.2023.16.3.7
Venkateswarlu Kudupudi, Ravi Shankar Kakarparthy, Prakash Nathaniel Kumar Sarella, Venkata Ramana Murthy Kolapalli
Introduction: Vancomycin hydrochloride (VH) is an amphoteric glycopeptide antibiotic used to manage enterocolitis and pseudomembranous colitis. However, VH is prone to proteolytic degradation in the stomach, thus obscuring the drug entry into the colon. Colon-targeted drug delivery can prevent gastric degradation and localise the drug in the colon. Methodology: The applicability of in situ polyelectrolyte complexation technique using the polymers Chitosan, Karaya gum, and Hupu gum at various concentrations along with enteric coating using Eudragit S100 was studied for the preparation of colon-targeted tablets of VH. Colon-targeted tablets of VH are developed by incorporating natural polymers like chitosan, karaya gum, and hupu gum at different concentrations such that in-situ polyelectrolyte complex is formed and the formulations were then coated with Eudragit S100(6%, 8%, and 10% weight gain) to release the drug in a controlled manner in the colon. Results: Prepared formulations were subjected to in vitro, ex vivo, and in vivo evaluation studies. Out of all the prepared formulations, the formulation H2C10 prepared with 10:2 PEC and 10% Eudragit S100 coating has shown a sufficient lag time of 2 hours in 0.1N HCl, 3 hours of lag time in pH 6.8 phosphate buffer and has shown a 100.02% drug release at 22 hours in pH 7.4 phosphate buffer. Conclusion: The research results suggested that a colon-targeted drug delivery system of VH can decrease drug degradation and achieve higher concentrations in the colon to provide more therapeutic benefits.
盐酸万古霉素(VH)是一种两性糖肽抗生素,用于治疗肠结肠炎和假膜性结肠炎。然而,VH在胃中容易发生蛋白水解降解,从而使药物无法进入结肠。结肠靶向给药可以防止胃降解并将药物定位在结肠中。& # x0D;方法:研究了不同浓度的壳聚糖、卡拉亚胶、琥蒲胶的原位聚电解质络合技术与乌龙茶S100肠溶包衣在制备VH结肠靶向片中的适用性;VH结肠靶向片剂是通过加入不同浓度的天然聚合物,如壳聚糖、卡拉亚胶和胡普胶,从而形成原位聚电解质复合物,然后在配方中涂上Eudragit S100(增重6%、8%和10%),以受控的方式在结肠中释放药物。& # x0D;结果:制备的制剂进行了体外、离体和体内评价研究。在所有制备的配方中,以10:2的PEC和10%的Eudragit S100包衣制备的H2C10配方在0.1N HCl中有足够的滞后时间2小时,在pH 6.8的磷酸盐缓冲液中有3小时的滞后时间,在pH 7.4的磷酸盐缓冲液中有22小时的100.02%的药物释放。& # x0D;结论:研究结果表明,VH结肠靶向给药系统可以减少药物降解,并在结肠中达到更高的浓度,从而提供更多的治疗效果。
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International Journal of Pharmaceutical Sciences and Nanotechnology
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