醚注射法制备载瑞格列奈脂质体及评价

Shabira Sagir, M. Hamiduzzaman, Irin Dewan, M. Asaduzzaman
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引用次数: 0

摘要

瑞格列奈是一种常用的治疗2型糖尿病的降糖药。然而,由于其低生物利用度和半衰期,它并不总是支持一个合适的剂量方案。本研究的目的是开发和分析瑞格列奈控释脂质体,为治疗糖尿病提供合适的剂型。采用改良醚注射法制备了载瑞格列奈脂质体。根据USP-II桨片法,脂质体在磷酸盐缓冲液(pH 7.4)中体外溶出研究8小时。根据ICH指南,在三种不同的环境条件下进行了为期14天的稳定性研究。此外,显微镜观察证实了脂质体囊泡的存在和大小。当磷脂酰胆碱与胆固醇的摩尔比为1:0.4时,最佳搅拌速率为300 RPM,包封率为73.1%。与非聚乙二醇化脂质体相比,聚乙二醇化脂质体(PEG400/1500)延长了制剂的载药量。相反,黑油的加入使脂质体的包封效率降低。大多数配方遵循零级动力学模型和超II类释放机制。脂质体体外溶出呈控释模式,8 h后最大释药量为92.64%。此外,所有脂质体制剂在冷藏温度(5±2ºC)下更稳定,其中聚乙二醇脂质体在三种不同的环境条件下最稳定超过14天。光学显微镜下的目测证实了脂质体的囊泡结构。达卡大学药学院。自然科学22(1):89-96,2023 (6)
本文章由计算机程序翻译,如有差异,请以英文原文为准。
Preparation and Evaluation of Repaglinide Loaded Liposomes by Ether Injection Method
Repaglinide is a commonly used antidiabetic drug to treat type 2 diabetes mellitus. However, it does not always support a suitable dose regimen due to its low bioavailability and half-life. The purpose of this study was to develop and analyze repaglinide loaded control release liposomes to provide suitable dosage form to treat diabetes. Repaglinide loaded liposomes were prepared by modified ether injection method. According to the USP-II paddle method, in vitro dissolution studies of liposomes were performed for 8 hours in phosphate buffer (pH 7.4). The stability study was executed according to ICH guidelines under three different environmental conditions for 14 days. Additionally, the presence and size of liposomal vesicles was confirmed by microscopic observation. The formulations containing phosphatidylcholine and cholesterol at a molar ratio of 1:0.4 revealed the highest drug entrapment efficiency of 73.1% with an optimum stirring rate of 300 RPM. The pegylated liposomes (PEG400/1500) prolonged the drug loading capacity for the formulations compared to non-pegylated liposomes. On the contrary, the addition of nigella oil caused a decrease in entrapment efficiencies of the liposomes. Most of the formulations followed zero order kinetic model and supper class II release mechanism. In vitro dissolution showed controlled release pattern of the liposomes and maximum drug release after 8 hours was 92.64%. Additionally, all the liposomal formulations were found to be more stable at refrigeration temperature (5 ± 2ºC) where pegylated liposomes were most stable over 14 days at three different environmental conditions. Visual observation under an optical microscope, the vesicular structure of liposomes was confirmed. Dhaka Univ. J. Pharm. Sci. 22(1): 89-96, 2023 (June)
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