齐墩果酸/PLGA-TPGS纳米粒的制备及其体外释放行为研究

Preparation and in Vitro Release Study of Oleanolic Acid/PLGA-TPGS Nanoparticles

目的:制备齐墩果酸/乳酸羟基乙酸共聚物-水溶性维生素E衍生物(PLGA-TPGS)纳米粒(OPN)并考察其体外释放情况。方法:用自制的PLGA-TPGS为载体材料,采用超声乳化-溶剂挥发法制备OPN,考察其粒径、Zeta电位、载药量、包封率、体外累积释放率。结果:所制OPN的平均粒径为(202.4±1.2)nm,Zeta电位为(-21.5±2.2)mV,载药量为(27.65±2.27)%,包封率为(92.52±2.15)%,其在含1.0%十二烷基硫酸钠的磷酸盐缓冲液(pH7.4)中呈两相释放,432h时累积释放率为(93.8±2.9)%。结论:所制OPN质量稳定、可控,具有明显的体外缓释作用。

OBJECTIVE： To prepare Oleanolic acid/polylactic-co-glycolic acid-D-a-tocopherol polyethylene glycol succinate de-rivates （PLGA-TPGS） nanoparticles （OPN） and to determine its in vitro release rate. METHODS： OPN were prepared by ultrasoni-cation emulsion-solvent evaporation technique using PLGA-TPGS as carrier. Its panicle size, Zeta potential, drug-loading and en- capsulation efficiency and in vitro release rate were determined. RESULTS： The OPN was sphere-like with mean particle size of （202.4 ±1.2） nm, Zeta potential of （ -21.5 ± 2.2） mV, drug-loading amount of （27.65 ±2.27）% and encapsulation efficiency of （92.52 ± 2,15）%. The in vitro drug release profile in phosphate buffer solution of pH 7.4 containing 1.0% sodium dodecyl sulfate showed diphasic release pattern, and the accumulative release rate was （93.8 ±2.9）% at 432 h. CONCLUSION： The OPN is stable and controllable in quality, and shows obvious sustained-release in vitro.