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首页> 外文期刊>Biomaterials >Preparation and characterization of poly(lactic acid)-poly(ethylene glycol)-poly(lactic acid) (PLA-PEG-PLA) microspheres for controlled release of paclitaxel.
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Preparation and characterization of poly(lactic acid)-poly(ethylene glycol)-poly(lactic acid) (PLA-PEG-PLA) microspheres for controlled release of paclitaxel.

机译：紫杉醇控释用聚乳酸-聚乙二醇-聚乳酸（PLA-PEG-PLA）微球的制备与表征。

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摘要

Microspheres of a new kind of copolymer, poly(lactic acid)-poly(ethylene glycol)-poly(lactic acid) (PLA-PEG-PLA), are proposed in the present work for clinical administration of an antineoplastic drug paclitaxel with hypothesis that incorporation of a hydrophilic PEG segment within the hydrophobic PLA might facilitate the paclitaxel release. Paclitaxel-loaded PLA-PEG-PLA microspheres of various compositions were prepared by the solvent extraction/evaporation method. Characterization of the microspheres was then followed to examine the particle size and size distribution, the drug encapsulation efficiency, the colloidal stability, the surface chemistry, the surface and internal morphology, the drug physical state and its in vitro release behavior. The effects of polymer types, solvents and drug loading were investigated. It was found that in the microspheres the PEG segment was homogeneously distributed and caused porosity.Significantly faster release from PLA-PEG-PLA microspheres resulted in comparisonwith the PLGA counterpart. Incorporation of water-soluble solvent acetone in the organic solvent phase further increased the porosity of the PLA-PEG-PLA microspheres and facilitated the drug release. A total of 49.6% sustained release of paclitaxel within 1 month was achieved. Potentially, the presence of PEG on the surface of PLA-PEG-PLA microspheres could improve their biocompatibility. PLA-PEG-PLA microspheres could thus be promising for the clinical administration of highly hydrophobic antineoplastic drugs such as paclitaxel.
机译：在目前的工作中提出了一种新型共聚物微球，即聚乳酸-聚乙二醇-聚乳酸（PLA-PEG-PLA），用于抗肿瘤药物紫杉醇的临床给药，其假设是在疏水性PLA内掺入亲水性PEG片段可能促进紫杉醇的释放。通过溶剂萃取/蒸发法制备负载紫杉醇的各种组成的PLA-PEG-PLA微球。然后进行微球的表征，以检查粒径和尺寸分布，药物包封效率，胶体稳定性，表面化学，表面和内部形态，药物物理状态及其体外释放行为。研究了聚合物类型，溶剂和载药量的影响。结果发现，在微球中，PEG链段分布均匀并产生孔隙。与PLGA相比，PLA-PEG-PLA微球释放速度明显加快。在有机溶剂相中加入水溶性溶剂丙酮进一步增加了PLA-PEG-PLA微球的孔隙率，并促进了药物释放。紫杉醇在1个月内共有49.6％的持续释放。潜在地，PLA-PEG-PLA微球表面上PEG的存在可以改善其生物相容性。因此，PLA-PEG-PLA微球可能有望用于高度疏水性抗肿瘤药（例如紫杉醇）的临床给药。

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