替莫唑胺脂质体制剂治疗胶质瘤的研制

S. Velivela, N. B. Pati, B. R. Babu
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引用次数: 1

摘要

替莫唑胺是一种抗癌药物;将其包封在脂质体内静脉应用。为了避免副作用和使药物靶向于特定部位,我们配制了替莫唑胺脂质体制剂。以药物和大豆磷脂酰胆碱为载体,采用旋转蒸发器干燥薄膜水化技术制备了该脂质体。对所制备的脂质体的大小、形状、包封率、体外释药和物理稳定性进行了表征。经评价的批次具有良好的理化特性。tmz6包封率最高,为40.19%,体外释放度为64.94%。结果表明,优选tmz6为优化配方,优化后的配方在应用Korsmeyer-Pepps模型研究药物释放机理时,符合零级释放动力学和超case II转运。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
Formulation development of Temozolomide liposomal formulation in the treatment of Glioma
Temozolomide is an anti-cancer drug; it was encapsulated in liposomal intravenous application. To avoid the side effects and to target the drug to the specific site, we have formulated liposomal formulation of Temozolomide. The liposomal were prepared by dried thin film hydration technique using rotary evaporator with drug and Soya phosphatidyl choline as carrier. The prepared liposomes were characterized for size, shape, % entrapment efficiency, in-vitro drug release and physical stability. The evaluated batches showed good physicochemical characteristics. The maximum encapsulation efficiency of Temozolomide was achieved with formulation TMZ 6 with 40.19% and the in-vitro drug release is 64.94%. Based on the results it can be concluded that TMZ 6 was selected as optimized formulation and the optimized formulation Optimized formulation follows zero order release kinetics and follow super case II transport when it applied to Korsmeyer-Pepps model for mechanism of drug release.
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