月桂酸单乙醇酰胺修饰利福平脂质体制备及性能研究

Study on preparation of rifampicin liposomes modified by lauric acid monoethanolamide and its property

目的:制备表面活性剂修饰的利福平(RFP)脂质体,进行脂质体水化性能、载药量、释药速度和肺膜透过研究。方法:采用薄膜超声法制备利福平脂质体,考察月桂酸单乙醇酰胺(LMEA)、月桂氮芯卓酮、聚山梨醇酯对利福平脂质体形态、粒径分布、包封率、稳定性和释药速度的影响。结果:LMEA-RFP脂质体粒径25～64nm;包封率为85.3%;8h肺膜累积透过率可达61.84%,表观透膜系数KP=42.9,LD50为610mg·kg-1。结论:LMEA修饰的利福平脂质体载药量增加,具有稳定性好、毒性低的特点。

OBJECTIVE To preparation rifampiein liposomes modified with surfactants to improve solubility, loding capicity, release rate, and pulmonary drug delivery. METHODS The film method was used to prepare rifampicin liposomes of various RFP liposomes morphology by LMEA, Tween 80 and azone, the properties were studied, including morphology, entrapment effi ciency,stability and drug release rate. RESULTS The particle size of RFP-LMEA liposomes was between 25-64 nm, The encapsulation efficiency reached 85.3 %. In 8 h, the rate of trans-membrane of rifampicin liposomes was 61.84%. LD50 of rifampicin LMEA-liposomes by ip was 610mg·kg^1. CONCLUSION RFP-LMEA liposomes increase the drug loading and have good stability and low toxicity.