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目的:制备丹参素脂质体并考察其体外释放度。方法:采用逆相蒸发法制备丹参素脂质体,以包封率为指标,通过正交试验考察大豆卵磷脂浓度、大豆卵磷脂与丹参素药脂比和水相p H值。透射电镜观察所制备脂质体的形态和粒径,利用HPLC测定丹参素含量,透析法比较丹参素脂质体和游离丹参素的体外释放度。结果:最佳制备工艺:磷脂浓度为40 mg·ml-1,药脂比为1∶10,水相p H为6.6。制备的丹参素脂质体为圆整球形,平均粒径(174±36)nm,平均包封率38.9%。丹参素浓度范围在2.0~20.0 mg·L-1的线性关系良好(r=0.998 4),丹参素脂质体的体外释放度比游离丹参素慢,能达到24 h缓释。结论:采用逆相蒸发法制备的丹参素脂质体粒径大小均匀,具有一定的缓释效果。
Objective: To prepare Danshensu liposome and investigate its in vitro release. METHODS: Danshensu liposome was prepared by reversed phase evaporation method. The entrapment efficiency was used as an index to determine the lecithin concentration, the ratio of soy lecithin to Danshensu, and the p H value of the aqueous phase. The morphology and particle size of the prepared liposomes were observed by transmission electron microscope. The content of danshensu was determined by HPLC. The in vitro release of danshensu liposome and free danshensu was compared by dialysis. RESULTS: The best preparation technology: the concentration of phospholipid was 40 mg·ml-1, the ratio of drug to lipid was 1:10, and the water phase p H was 6.6. The prepared Danshensu liposome was round and spherical, with an average particle size of (174±36) nm and an average entrapment efficiency of 38.9%. The concentration of danshensu in the range of 2.0~20.0 mg·L-1 showed a good linear relationship (r=0.998 4). The in vitro release of danshensu liposome was slower than that of free danshensu and could achieve 24 h sustained release. Conclusion: Danshensu liposomes prepared by reversed phase evaporation method have uniform particle size and have certain sustained release effect.