苦参总生物碱脂质体凝胶的制备及释药机制研究.docVIP

苦参总生物碱脂质体凝胶的制备及释药机制研究 　　摘要：目的 优化苦参总生物碱脂质体的处方与工艺，制备苦参总生物碱脂质体凝胶并研究其释放机制。方法 运用薄膜分散法制备苦参总生物碱脂质体，以包封率和载药量为考察指标，采用酸性染料比色法测定脂质体中苦参碱含量。采用正交试验设计对处方工艺进行优化，选出最优处方制备脂质体。以泊洛沙姆-407为基质，制备苦参总生物碱脂质体凝胶。考察药物凝胶与药物脂质体凝胶的透皮速率。结果 通过优化处方与工艺所得的脂质体形态均匀，粒径范围为100～400 nm，包封率达74%，载药量达26%。所制备的脂质体凝胶呈透明状半固体。体外释放结果显示，苦参碱凝胶48 h内累积释药量为6.34 mg/cm2，苦参总生物碱脂质体凝胶48 h内累积释药量为6.97 mg/cm2，后者的累积透皮量、稳态透皮速率及48 h后在皮肤中的蓄积量均较前者显著提高。结论 优化的制备工艺稳定可行，制得的苦参总生物碱脂质体凝胶质量较好，可有效延缓药物的释放速率，提高药物在体内的蓄积量。 　　关键词：苦参总生物碱；脂质体；凝胶 　　DOI：10.3969/j.issn.1005-5304.2017.01.019 　　中图分类号：R283.5 文献标识码：A 文章编号：1005-5304（2017）01-0077-05 　　Release Mechanism and Preparation of Liposome Gel of Total Alkaloids of Sophoras Flavescentis Radix ZHU Ling-yin， ZHENG Guan-tao， ZHOU Chang-ni， SHEN Yan-li， HAN Zhi-fang， JIA Yong-yan （College of Pharmacy， Henan University of Chinese Medicine， Zhengzhou 450046， China） 　　Abstract： Objective To optimize the formulation and process of liposome gel of total alkaloids of Sophoras Flavescentis Radix； To prepare the liposome gel of total alkaloids of Sophoras Flavescentis Radix and study its release mechanism. Methods Matrine liposomes was prepared by using film dispersion method； With entrapment efficiency and medicine loading as indexes， acid dye colorimetric method was used for the determination of matrine content in liposomes. Orthogonal design was used to optimize the formulation and the optimal formulation of liposomes was selected. Poloxamer-407 was set as the substrate preparation of matrine liposome gel. The transdermal rate of medicine gel and medicine liposome gel was investigated. Results Obtained through formulation and technology optimization of liposomes formation uniform， particle size was in the range of 100 nm to 400 nm， entrapment 74%， loading 26%. Preparation of liposome gel was transparent semisolid. In vitro results showed， cumulative release dose of matrine hydrogel was 6.34 mg/cm2 within 48 h； cumulative release doses of liposome gel of total alkaloids of Sophoras Flavescentis Radix wa