尼莫地平脂质体的制备及体外透皮研究

Preparation and Transdermal Diffusion in Vitro of Nimodipine Liposomes

目的:采用2种方法制备尼莫地平脂质体,并考察其包封率与体外透皮性。方法:用薄膜法和乙醇注入法制备尼莫地平脂质体,考察2种方法所制脂质体的粒径分布及包封率;采用Franz扩散装置对脂质体进行体外透皮试验,并与尼莫地平溶液比较。结果:薄膜法和乙醇注入法制备的脂质体平均粒径分别为(768.7±190.6)、(1 742±270)nm,平均包封率均高达97%以上。与尼莫地平溶液比较,脂质体中药物透皮缓慢,其中以薄膜法制备的脂质体在48h以后其单位面积累积透皮量显著更高。结论:2种制备方法中以薄膜法更优。

OBJECTIVE： To prepare nimodipine liposome（NL） by two methods and to investigate its entrapment effi ciency（EE） and the transdermal diffusion in vitro. METHODS： NL were prepared using thin film dispersion and ethanol injection method respectively. The particle size distribution and the EE of NL were investigated. Franz diffusion cell was used to investigate the cumulative release amount of NL and that of nimodipine solution. RESULTS： It has shown that the mean particle diameter was （768.7 ± 190.6） nm for the NL prepared by the thin film dispersion method and （1 742 ± 270） nm for that by the ethanol injection method. The average EE of NL prepared by both methods was over 97%. As compared with ni- modipine solution, NL had slow transdermal diffusion. The cumulative release amount of liposomes prepared by the thin film dispersion method was significantly higher than that by the ethanol injection method after 48 h. CONCLUSION： Thin film dispersion was better than ethanol injection method.