Glavas-Dodov Marija, Fredro-Kumbaradzi Emilija, Goracinova Katerina, Calis Sema, Simonoska Maja, Hincal Atila A
Department of Pharmaceutical Technology, Faculty of Pharmacy, University Ss Cyril and Methodious, 1000 Skopje, Macedonia.
Acta Pharm. 2003 Dec;53(4):241-50.
Liposome gels bearing an antineoplastic agent, 5-fluorouracil, intended for topical application have been prepared and drug release properties in vitro have been evaluated. Different formulations of liposomes were prepared by the film hydration method by varying the lipid phase composition (PL 90H/cholesterol mass ratio) and hydration conditions of dry lipid film (drug/aqueous phase mass ratio). Topical liposome gels were prepared by incorporation of lyophilized liposomes into a structured vehicle (1%, m/m, chitosan gel base). Also, hydrogels containing different concentrations of 5-fluorouracil were prepared and drug release properties were investigated. The rate of drug release from liposome gels was found to be dependent on the bilayer composition and the dry lipid film hydration conditions. Also, liposomes embedded into a structured vehicle of chitosan showed significantly slower release than hydrogels. The drug release obeyed the Higuchi diffusion model, while liposomes acted as reservoir systems for continuous delivery of the encapsulated drug.
已制备了负载抗肿瘤药物5-氟尿嘧啶的脂质体凝胶用于局部应用，并对其体外药物释放特性进行了评估。通过改变脂质相组成（磷脂90H/胆固醇质量比）和干脂质膜的水化条件（药物/水相质量比），采用薄膜水化法制备了不同配方的脂质体。通过将冻干脂质体掺入结构化载体（1%，m/m，壳聚糖凝胶基质）中来制备局部脂质体凝胶。此外，还制备了含有不同浓度5-氟尿嘧啶的水凝胶，并研究了其药物释放特性。发现脂质体凝胶的药物释放速率取决于双层组成和干脂质膜的水化条件。此外，嵌入壳聚糖结构化载体中的脂质体的释放明显比水凝胶慢。药物释放符合Higuchi扩散模型，而脂质体作为储存系统用于持续递送包封的药物。
