姜黄素PLGA-TPGS纳米粒的制备和质量评价

Preparation and quality evaluation of Curcumin- loaded PLGA-TPGS Nanoparticles

关键词:  姜黄素  乳酸羟基乙酸共聚物-水溶性维生素E  纳米粒  RP-HPLC法  体外释放度

Key words:  curcumin  PLGA-TPGS  nanoparticles  RP-HPLC  in vitro release rate

摘要:

目的　制备姜黄素乳酸羟基乙酸共聚物-水溶性维生素E纳米粒（CM-PLGA-TPGS-NPs，简称CPTN）并评价其质量。　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CPTN，通过粒径、Zeta电位、载药量、包封率和体外释放度控制其质量。采用RP-HPLC法，色谱柱为KROMASIL柱（4.6 mm×250 mm，5 μm），用乙腈-2%冰醋酸溶液（58∶〖KG-*2〗42）为流动相，检测波长为430 nm。　结果　自制CPTN的平均粒径为（197.9±6.2）nm，Zeta电位为（-22.3±1.8）mV，载药量为（13.2±0.9）%和包封率为（79.3±1.6）%。体外姜黄素在含0.5%十二烷基硫酸钠的磷酸盐缓冲液（pH7.4）中呈两相释放，30 d时累积释放率为91.3%。　结论　CPTN质量稳定可控，体外试验显示具有明显的缓释作用。

Abstract:

Objective　To prepare Curcumin-loaded polylactic-co-glycolic acid-D-α- tocopherol polyethylene glycol 1000 succinate nanoparticles (CM-PLGA-TPGS-NPs, namely CPTN) and evaluate their quality.　Methods〖WTBZ〗 CPTN were prepared by ultrasonication emulsion/solvent evaporation technique using PLGA-TPGS made by ourselves, its mean size, Zeta potential, drug-loading, encapsulation efficiency and in vitro release rate of CPTN were determined. The condition was checked by RP-HPLC on KROM ASIL C18 column (4.6 mm×250 mm, 5 μm) with acetonitrile and 2% acetic acid (58∶〖KG-*2〗42) as mobile phase, and the detective wavelength was 430 nm.　Results〖WTBZ〗 CPTN was sphere-like with mean particle size of (197.9±6.2) nm, Zeta potential of (-22.3±1.8) mV, drug-loading of (13.2±0.9) % and encapsulation efficiency of (79.3±1.6) %. The in vitro drug release profile in phosphate buffer solution of pH 7.4 containing 0.5% w/v Sodium dodecyl sulfate showed diphasic release pattern, the cumulative release rate was 91.3% at 30 d. 　Conclusion〖WTBZ〗 CPTN is stable and controllable in quality, in vitro release rate shows obvious sustained release.