利拉萘酯固体脂质纳米粒的构建及表征  

Preparation and Characterization of Liranaftate Solid Lipid Nanoparticles

作　　者：张海龙[1] 刘海乐[1] 兰天[1] 丁劲松[1] 

机构地区：[1]中南大学药学院,湖南长沙410013

出　　处：《中国医药工业杂志》2012年第5期351-355,共5页Chinese Journal of Pharmaceuticals

摘　　要：以单硬脂酸甘油酯和胆固醇为脂质材料,采用乳化溶剂扩散法制备利拉萘酯固体脂质纳米粒,并采用正交设计优化处方。结果表明,所得优化制品平均粒径为(145.3±6.1)nm,包封率为(75.8±0.7)%,载药量为(4.82±0.03)%,DSC分析提示药物可能以无定形状态存在于载体中。稳定性初步研究显示制品在4℃条件放置30 d可维持稳定。体外透皮试验表明,利拉萘酯固体脂质纳米粒凝胶的皮肤滞留比约为市售乳膏(Zefnart)的100倍。Solid lipid nanoparticles（SLN） loaded with liranaftate were prepared by emulsion solvent diffusion method with glyceryl monostearate and cholesterin as matrix material.The formulation was optimized through orthogonal design.The mean particle size of the liranaftate SLN was（145.3±6.1）nm with the entrapment efficiency of（75.8±0.7）% and drug loading of（4.82±0.03）%.The results of differential scanning calorimetry（DSC） showed that liranaftate was entrapped in the SLN as amorphous form.The results of preliminary stability test showed that the liranaftate SLN stored at 4 ℃ for 30 d could maintain stable.The results of in vitro transdermal test showed that the skin deposition ratio of liranaftate SLN gel was about 100 times of the commercial cream（Zefnart）.

关 键 词：利拉萘酯 固体脂质纳米粒 乳化溶剂扩散法 制备 

分 类 号：R944.9[医药卫生—药剂学]