摘要
目的:制备全反式维A酸(all-trans retinoic acid,ATRA)醇质体并对其稳定性及体外经皮渗透等进行考察。方法:采用注入法制备ATRA醇质体,通过正交设计优化制备工艺;同时测定其Zeta电位及粒径;以改进的Franz扩散池法,进行体外小鼠经皮渗透实验,测定药物累积渗透量及透皮速率。结果:优选处方组成为20%乙醇(w/w),4%磷脂(w/w),磷脂∶胆固醇(w/w)2∶1,磷脂∶维A酸(w/w)10∶1,检测平均粒径为237.3 nm,Zeta电位为-36.31 mV;ATRA醇质体放置1,10,20 d后,7 h累积透皮量分别为(210.6±1.7),(196.2±3.8)和(181.1±4.2)μg.cm-2,而水醇混合物累积透皮量仅为(120.4±5.4)μg.cm-2。结论:ATRA醇质体制备工艺简单可行,所得传递体粒径较小且均匀,室温放置较稳定,透皮效果较好并可以促进维A酸经皮转运。
Objective：To prepare the all-trans retinoic acid（ATRA） ethosomes,and evaluate their stability and transdermal resorption in vitro.Methods：The ethosomes were prepared by ethanol infusion method.The formula was evaluated by orthogonal experiment.The Zeta potential and size of ethosomes were measured.The penetration experiments in vitro were performed on modified Franz fusion cells.The accumulation of drug-penetration was calculated.Results：The appropriate formulation consisted of 20% ethanol（w/w）,4% phospholipids（w/w）.The ratio of phospholipids to cholesterol was 2∶1（w/w）,the ratio of phospholipids to retinoic acid was 10∶1（w/w）.The average particle size of all-trans retinoic acid ethosomes optimized formula was 237.3 nm and evenly distributed,and Zeta potential was-36.31 mV.The cumulative penetrations during 7 h of ethosomes at day 1,day 10,day 20 after preparation were（210.6±1.7）,（196.2±3.8） and（181.1±4.2） μg·cm-2,respectively.While,the cumulative penetration of ethanol solution was（120.4±5.4） μg·cm-2.Conclusion：The preparation method of all-trans retinoic acid ethosomes was simple and suitable.The particle size are relatively small and homogeneous,and can improve significantly the transdermal delivery speed of retinoic acid.
出处
《中国新药杂志》
CAS
CSCD
北大核心
2010年第13期1153-1156,共4页
Chinese Journal of New Drugs
关键词
全反式维A酸
醇质体
经皮渗透
注入法
正交设计
all-trans retinoic acid
ethosomes
transdermal resorption
ethanol infusion method
orthogonal experiment
