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一种新型阴道给药系统:含阿巴卡韦的抗艾滋病毒生物黏附膜。

A novel vaginal drug delivery system: anti-HIV bioadhesive film containing abacavir.

作者信息

Ghosal Kajal, Ranjan Alok, Bhowmik Benoy Brata

机构信息

Dr. B.C. Roy College of Pharmacy and Allied Health Science, Bidhan Nagar, Durgapur, 713206, West Bengal, India,

出版信息

J Mater Sci Mater Med. 2014 Jul;25(7):1679-89. doi: 10.1007/s10856-014-5204-6. Epub 2014 Apr 4.

Abstract

Women are very much susceptible for acquired immunodeficiency syndrome (AIDS) and other sexually transmitted diseases (STDs), mainly due to unprotected heterosexual vaginal intercourse and for some other social and economical disadvantages. Our aim was to formulate and optimize vaginal film of abacavir, a potent nucleoside reverse transcriptase inhibitor, for the treatment of AIDS and HIV. Abacavir films were prepared by solvent evaporation method using sodium alginate (Na-alginate) as the main polymer, Hydroxypropyl Methylcellulose E 15 (HPMC E 15) as the copolymer and glycerol as a humectant. Abacavir sulphate (ABC) was used here as a drug. Films were optimized for various physicochemical parameters such as tensile strength, % elongation at break, swelling capacity, drug content (mg/cm(2)), thickness, folding endurance, bioadhesion, pH, moisture content and SEM. Drug polymer interaction was studied by FTIR Spectra. The drug release study was accomplished in dissolution apparatus. In vivo study was also carried out. This newly formed film was one kind of sustain release type and can be considered as a novel drug carrier system for the treatment of AIDS and other STDs. It was suitable for local as well as systemic effect. The films showed good physicochemical property with good aesthetic appeal.

摘要

女性非常容易感染获得性免疫缺陷综合征(艾滋病)和其他性传播疾病(性病),主要原因是无保护的异性阴道性交以及一些其他社会和经济方面的不利因素。我们的目标是制备并优化阿巴卡韦(一种有效的核苷类逆转录酶抑制剂)阴道膜,用于治疗艾滋病和艾滋病毒。阿巴卡韦膜采用溶剂蒸发法制备,以海藻酸钠(Na - 海藻酸盐)作为主要聚合物,羟丙基甲基纤维素E 15(HPMC E 15)作为共聚物,甘油作为保湿剂。硫酸阿巴卡韦(ABC)在此用作药物。对膜进行了多种物理化学参数的优化,如拉伸强度、断裂伸长率、溶胀能力、药物含量(mg/cm²)、厚度、耐折度、生物黏附性、pH值、水分含量和扫描电子显微镜(SEM)。通过傅里叶变换红外光谱(FTIR)研究药物与聚合物的相互作用。药物释放研究在溶出装置中完成。还进行了体内研究。这种新形成的膜是一种缓释型,可被视为治疗艾滋病和其他性病的新型药物载体系统。它适用于局部和全身作用。这些膜具有良好的物理化学性质和美观性。

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