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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 prepare surfactant-modified rifampicin (RFP) liposomes for liposome hydration performance, drug loading, drug release rate and pulmonary membrane permeability. Methods: The liposomes of rifampicin were prepared by thin-film ultrasonic method. The effects of lauric acid monoethanolamide (LMEA), laurel ncronol and polysorbate on the morphology, particle size distribution, encapsulation efficiency , Stability and drug release rate. Results: The LMEA-RFP liposomes had a diameter of 25-64 nm and an entrapment efficiency of 85.3%. The cumulative transmission rate of the lung membrane reached 61.84% at 8 h. The apparent membrane permeability coefficient KP was 42.9 and the LD50 was 610 mg · kg -1. Conclusion: LMEA modified rifampicin liposome drug load increased, with good stability, low toxicity.