| 摘要: |
| 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。 |
| 关键词: 多烯紫杉醇 纳米粒子 聚乳酸羟基乙酸共聚物 体外释放 |
| DOI：10.3724/SP.J.1008.2011.0295 |
| 投稿时间：2010-12-17修订日期：2011-01-24 |
| 基金项目:国家自然科学基金青年项目(30800259). |
|
| Preparation and in vitro release of docetaxel-loaded PLGA-PEG nanoparticles |
| CHEN Ting, LU Ying, LIN Ya-ling, HUANG Jing-bin, TU Ye, SUN Zhi-guo, LIU Jun-jie, ZHONG Yan-qiang* |
| (Department of Pharmaceutics, School of Pharmacy, Second Military Medical University, Shanghai 200433, China) |
| Abstract: |
| ObjectiveTo 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．MethodsPLGA-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. ResultsThe 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％. ConclusionThe 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. |
| Key words: docetaxel nanoparticles poly(D,L-lactide-co-glycolide) in vitro release |
