脂质体包膜吡罗昔康的研制与表征研究

H. S. Chiong, M. N. Hakim, M. Sulaiman, Z. A. Zakaria, A. Zuraini, S. Ong, K. Yuen
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引用次数: 9

摘要

本研究的目的是为一种亲脂性非甾体抗炎药吡罗昔康开发一种新的基于脂质体的给药系统。采用原脂质体法制备该体系,并对不同制备参数(原脂质体类型、药物浓度、水化时间和采用的减粒径处理类型)进行优化。所有制备的脂质体样品广泛表征其药物包埋和大小分布使用各种体外技术。目前的研究表明,最优配方(Pro-lipoTM Duo;每克pro - lipom 12mg吡罗西康;10 h水化时间)的实际药物包封量最高(800.4 mg/g Pro-lipoTM),包封率为15.36%,令人满意。该配方还获得了均匀(多分散指数= 0.45)和小粒径(359.95nm)的脂质体样品。发现挤压技术可显著减少载药脂质体的药物包裹和大小分布。一项为期4周的储存研究表明,在冷藏和室温下,脂质体样品的药物包载和大小分布都是稳定的。电镜显示制备的脂质体样品呈球形,呈同心片状。总之,本工作成功地证明了一种简单、可重复性和实用的制备脂质体包膜吡罗昔康的方法。关键词:Proliposomes;脂质体;吡罗昔康;封装;颗粒大小;透射电子显微镜
本文章由计算机程序翻译,如有差异,请以英文原文为准。
Development and characterisation study of liposomes-encapsulated piroxicam
The objective of present work was to develop a novel liposomes-based drug delivery system for a lipophilic non-steroidal anti-inflammatory drug, piroxicam. The system was prepared using proliposomes method and optimised for different preparation parameters including type of proliposomes, concentration of drug, duration of hydration and type of particle size reduction treatment used. All prepared liposomal samples were extensively characterized for their drug-entrapment and size profile using various in-vitro techniques. Present work showed that the most optimum formulation (Pro-lipoTM Duo; 12mg piroxicam per gram Pro-lipoTM; 10 hours hydration time) produced highest amount of actual drug been entrapped in liposomes (800.4 mg/g Pro-lipoTM) with a satisfactory entrapment efficiency of 15.36%. This formulation had also produced liposomal samples with a homogenous (polydispersity index = 0.45) and small particle size (359.95nm). Extrusion technique was found to cause significant reduction in drug-entrapment and size profile of drug-loaded liposomes. A 4-weeks storage study showed that drug-entrapment and size profile of liposomal samples were stable in both refrigerated and room temperature. Electron microscopy revealed that prepared liposomal samples were spherical-shaped and showed concentric lamellae. In conclusion, present work successfully demonstrated a simple, reproducible and practical method of preparation for liposomes-encapsulated piroxicam. Keywords: Proliposomes; Liposomes; Piroxicam; Encapsulation; Particle size; Transmission electron microscopy
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