胰岛素磷脂复合物自微乳传递系统的制备

Formulation of self-nanoemulsifying drug delivery systems for insulin-soybean lecithin complex

目的构建胰岛素磷脂复合物自微乳传递系统(ISC-SNEDDS)。方法利用冻干法制备胰岛素磷脂复合物(ISC),根据其溶解性选择油相,确定复合物中胰岛素(INS)与磷脂(SPC)的最佳质量比;利用假三相图法,通过乳化后的外观和粒径筛选最优空白自微乳处方并制备载药自微乳制剂。结果制成磷脂复合物后,胰岛素在油酸乙酯中的溶解度显著增加;自微乳的最优处方为ethyl oleate-cremophor EL-alcohol(35:32.5:32.5),以0.01mol·L-1 HCl稀释10倍后,平均粒径为30.79±1.57nm,多分散系数PDI为0.132±0.025。结论胰岛素磷脂复合物可以增加胰岛素在油酸乙酯中的溶解度,其自微乳制剂的制备方法简单,稀释后粒径均一。

OBJECTIVE To prepare a novel self-nanoemulsifying drug delivery systems（SNEDDS） of insulin.METHODS The insulin-soybean phosphatidylcholine complex（ISC） was prepared by an anhydrous co-solvent lyophilization method.The type of oil and the weight ratio of insulin and soybean lecithin were chosen according to the dissolubility of the complex.The best formulation was optimized according to the appearance and the particle size of nanoemulsions with ternary phase diagrams.RESULTS The solubility of ISC was increased in ethyl oleate.The best formulation was ethyl oleate：cremophor EL：alcohol with the weight ratio of 35：32.5：32.5.The average size of ISC-SNEDDS was 30.79 ± 1.57 nm and PDI was 0.132 ± 0.025.CONCLUSION ISC could increase the solubility of insulin in ethyl oleate,the formulation of its SNEDDS was simple.