包裹多烯紫杉醇PLGA-PEG纳米粒的制备及体外释放度考察
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国家自然科学基金青年项目(30800259).


Preparation and in vitro release of docetaxel-loaded PLGA-PEG nanoparticles
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Supported by National Natural Science Foundation for Distinguished Young Scholars (30800259).

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    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。

    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.

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  • 收稿日期:2010-12-17
  • 最后修改日期:2011-01-24
  • 录用日期:2011-03-04
  • 在线发布日期: 2011-03-17
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