包裹多烯紫杉醇PLGA-PEG纳米粒的制备及体外释放度考察

Preparation and in vitro release of docetaxel-loaded PLGA-PEG nanoparticles

目的制备包裹多烯紫杉醇PLGA-PEG纳米粒(DTX-NPs)并评价其体外释放行为。方法合成高分子聚合物PLGA-PEG-COOH并表征;以其作为载体,复乳溶剂挥发法制备隐形纳米粒;动态光散射粒径仪和透射电镜测定DTX-NPs的粒径分布、zeta电位及表面形态;采用HPLC法测定DTX-NPs的包封率及载药量;以pH 7.4磷酸缓冲盐溶液(PBS)作为释放介质,考察DTX-NPs的体外释放行为。结果 DTX-NPs平均粒径为(138.8±1.01)nm,zeta电位为(-13.74±3.54)mV,包封率(99.41%±0.29%),载药量(2.47±0.02)μg/mg,24 h突释量为49%。结论 DTX-NPs制备工艺简便可控,结果稳定,且其体外释放行为具有缓释性,能够在血液中长时间滞留,具有良好的应用前景,值得进一步研究。

Objective To prepare the docetaxel（DTX）-loaded nanoparticles based on poly（D,L-lactide-co-gly-colide）-block-poly（ethylene glycol）（PLGA-b-PEG-COOH）（DTX-NPs）and to evaluate their in vitro release property.Methods PLGA-PEG was successfully synthesized and double emulsion solvent evaporation technique was used to prepare DTX-NPs.The size distribution,zeta potential,and surface morphology of the prepared DTX-NPs were characterized by dynamic light scattering（DLS） and transmission electron microscopy（TEM）;the entrapment efficiency and drug content were investigated by HPLC;and the in vitro release was examined using phosphate buffer solution as the releasing medium.Results The average diameter of DTX-NPs was（138.8±1.01） nm,the zeta potential was（-13.74±3.54） mV,the encapsulation efficiency was（99.91%±0.29%）,the drug load was（2.47±0.02） μg/mg,the 24 h drug release was 49%,and the total drug release in 120 h was 95%.Conclusion The present preparation method for DTX-NPs is reliable and simple,and the product is stable and possesses a sustained release character in vitro.It can stay in the blood for a long period and possess a bright future of application.