目的 制备小菜蛾抗菌肽(CA)聚乳酸-羟基乙酸共聚物(PLGA)纳米粒(CA-PLGA-NPs),并对其理化性质及体外释放度进行研究.方法 采用S/W/O/W复乳法结合高压均质法制备CA-PLGA-NPs,对其纳米粒的形态、粒径、多分散指数(PDI)、载药量、包封率和体外释放度进行研究.结果 CA-PLGA-NPs呈球形或类球形,粒径、PDI、载药量、包封率分别为(358.76±22.51)nm、0.168 1±0.012 2、(10.50±0.28)%、(60.92±1.58)%,突释现象不明显,2～10 d内达到释药稳定期.结论 S/W/O/W复乳法结合高压均质法制备CA-PLGA-NPs工艺可行,为小菜蛾抗菌肽给药提供了制剂学基础.

Objective To prepare the antibacterial peptides from Plutella xylostella-loaded nanoparticles based on poly(lactic-co- glycolic acid) (CA-PLGA-NPs) and evaluate its physicochemical property and in vitro release. Methods CA-PLGA-NPs were prepared by S/W/O/W double emulsion method combined with high-pressure homogenization. The morphology, particle size, polydispersion index (PDI), drug loading, encapsulation efficiency (EE), and in vitro release of the nanoparticles were studied. Results CA-PLGA-NPs were spherical or similarly spherical, and the average particle size, PDI, drug loading, and EE were (358.76 ± 22.51) nm, 0.168 1 ± 0.012 2, (10.50 ± 0.28)%, and (60.92 ± 1.58)%, respectively. And burst phenomenon was not significant. The drug delivery stable phase was 2—10 d. Conclusion S/W/O/W double emulsion method combined with high pressure homogenization method is suitable for the preparation of CA-PLGA-NPs, and provides a pharmaceutical basis for CA administration.

国家新药创制重大专项(2011ZX092J12108-04C)