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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

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【作者】 顾晓华王轩安磊蒋妮高萌梅林田燕

【Author】 GU Xiao-hua(Dept. of Pharmacy,The First Affiliated Hospital of Dalian Medical University,Liaoning Dalian 116011,China) WANG Xuan,AN Lei,GAO Meng,MEI Lin,TIAN Yan(Dalian Medical University,Liaoning Dalian 116044,China) JIANG Ni(Dept. of Pharmacy,Dalian Children Hospital,Liaoning Dalian 116001,China)

【机构】 大连医科大学附属第一医院药剂科大连医科大学大连儿童医院药剂科

【摘要】 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。

【Abstract】 OBJECTIVE:To prepare Oleanolic acid/polylactic-co-glycolic acid-D-α-tocopherol polyethylene glycol succinate derivates(PLGA-TPGS) nanoparticles(OPN) and to determine its in vitro release rate. METHODS:OPN were prepared by ultrasonication emulsion-solvent evaporation technique using PLGA-TPGS as carrier. Its particle size,Zeta potential,drug-loading and encapsulation 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.

【基金】 辽宁省教育厅2010年度资助课题(L2010129)
  • 【分类号】R943
  • 【被引频次】13
  • 【下载频次】432
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