姜黄素PLGA-TPGS纳米粒的制备和质量评价

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,5μm),用乙腈-2%冰醋酸溶液(58∶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。

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

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 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 condi- tion was checked by RP - HPLC on KROM ASIL C18 column （4.6 mm ×250 mm, 5 μm） with acetonitrile and 2% acetic acid （58： 42） as mobile phase, and the detective wavelength was 430 nm. Results CPTN was sphere -like with mean particle size of （197.9± 6.2） nm, Zeta potential of （ -22.3 ± 1.8） mV, drugloading of （13.2±0.9） % and encapsula- tion 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 CPTN is stable and controllable in quality, in vitro release rate shows obvious sustained release.