尼索地平醇质体的制备及体外经皮渗透研究

Preparation and in vitro transdermal penetration of nisoldipine ethosomes

目的:制备尼索地平醇质体并考察其经皮给药渗透特性。方法:采用乙醇注入匀质法制备尼索地平醇质体,以包封率为指标,设计正交试验优化处方。采用体外经皮渗透试验,比较不同给药形式对尼索地平经皮渗透的影响。结果:按优化处方制备的醇质体外形完整,平均粒径为(123.7±41.5)nm,粒径分布均匀,平均包封率为(68.01±1.45)%。醇质体可明显提高药物的透皮速率,增渗比为11.66,促渗效果优于45%乙醇溶液和脂质体。12 h后皮肤中药物的滞留量顺序为:醇质体>45%乙醇溶液>脂质体>混悬液。结论:醇质体能有效提高尼索地平经皮吸收,是透皮给药的优良载体。

OBJECTIVE To prepare nisoldipine ethosomes and investigate its penetration characteristic. METHODS Nisol- dipine ethosomes were prepared by ethanol injection homogenization method. The formulation of ethosomes was optimized by orthogonal experiment with encapsulation efficiency as index. The effects of different dosages regimens on the transdermal pen- etration of nisoldipine were studied by in witro permeation experiments. RESULTS The nisoldipine ethosomes was prepared under the optimal formulation,its morphology was integrity, its average size and encapsulation efficiency were （123. 7 ± 41.5） nm and （68. 01 ± 1.45） %, respectively. Nisoldipine ethosomes significantly enhanced the penetration rate of nisoldipine and the enhancement ratio was 11.66, superior to 45% ethanol solution and liposomes. The subsequenee of retention amount in the skin after 12h was： ethosomes〉45%ethanol solution〉 liposomes〉 suspensions. CONCLUSION The ethosomes could be an ideal carrier for transdermal delivery of nisoldipine which was effective for transdermal penetration.