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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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