多烯磷脂酰胆碱脂质纳米粒冻干粉针的制备工艺

Preparation of lyophilized polyene-phosphatidylcholine lipid nanoparticles

目的筛选多烯磷脂酰胆碱脂质纳米粒(PPC-LN)的处方和工艺条件。方法采用熔融乳化-高压匀质法制备PPC-LN,以单因素试验考察影响制备PPC-LN的处方和工艺因素,通过正交设计对处方和工艺条件进行优化,同时,对冻干脂质纳米粒的理化性质进行考察。结果所得纳米粒为圆整的类球形实体粒子,平均粒径为135±12nm,包封率为97.4%±0.9%,PDI为0.169±0.004。结论熔融乳化-高压匀质法可用于PPC-LN的制备,制成的冻干品包封率高,粒径分布均匀,成型良好。

OBJECTIVE To prepare lyophilized polyene phosphatidylcholine lipid nanoparticles （PPC -LN） and investigate the main influencing factors. METHODS PPC - LN was prepared by the method of melt - emulsification - high pressure homogeniza- tion. The main factors affecting PPC - LN quality were investigated by single factor test. The formulations were optimized by the orthogonal design. The physicochemical properties of lyophilized LN were also investigated. RESULTS The results showed that the nanoparticles were spherical and well distributed. The mean particle size was 135 ± 12 run with the encapsulation efficiency of 97.4% ± 0.9% and PDI of 0. 169 ± 0. 004, respectively. CONCLUSION The melt - emulsification - high pressure homogenization for the preparation of lipid nanoparticles containing PPC was highly feasible. Lyophilized PPC - LN with high encapsulation efficiency, narrow size distribution and good form could be obtained using this method.