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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。
Glycerol monostearate and cholesterol as the lipid material, the use of emulsification solvent diffusion method to prepare liraglutide solid lipid nanoparticles, and orthogonal design optimization prescription. The results showed that the average particle diameter of the optimized product was (145.3 ± 6.1) nm, the entrapment efficiency was (75.8 ± 0.7)% and the drug loading was (4.82 ± 0.03)%. DSC analysis indicated that the drug might exist in the amorphous state Carrier. Preliminary studies of stability showed that the product was stable at 4 ℃ for 30 days. In vitro transdermal tests showed that the skin retention ratio of liraglutide solid lipid nanoparticle gel was about 100 times that of the commercially available cream (Zefnart).