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Construction of amphiphilic copolymer nanoparticles based on gelatin as drug carriers for doxorubicin delivery

机译:以明胶为药物载体的两亲共聚物纳米颗粒的构建

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Novel biodegradable amphiphilic copolymer nanoparticles based on gelatin, poly(lactide) and 1,2- dipalmitoyl-sn-glycero-3-phosphoethanolamine (DPPE) (gelatin-co-PLA-DPPE) have been successfully fabricated. In order to estimate the feasibility as drug carriers, an anti-tumor model drug doxorubicin hydrochloride salt (DOX) was incorporated into polymeric nanoparticles by double emulsion or nanoprecipitation method. The nanoparticle size, size distribution and encapsulation efficiency (EE) were influenced by the feed weight ratio of the copolymer to DOX and different fabrication methods of nanoparticles. In addition, in vitro release experiments exhibited the release behavior was affected by pH of release media. The DOX-loaded nanoparticles showed that faster release at pH 5.0 than their release at pH 7.4 buffer. The DOX-loaded copolymer nanoparticles showed comparable anticancer efficacy with the free drug in vitro and in vivo. These results demonstrate a feasible application of the gelatin derivative as a promising nanocarrier for delivery of anti-tumor drugs.
机译:基于明胶,聚丙交酯和1,2-二棕榈酰-sn-甘油-3-磷酸乙醇胺(DPPE)(明胶-co-PLA-DPPE)的新型可生物降解的两亲共聚物纳米粒子已经成功制备。为了评估作为药物载体的可行性,通过双乳液或纳米沉淀法将抗肿瘤模型药物阿霉素盐酸盐(DOX)掺入聚合物纳米颗粒中。纳米颗粒的尺寸,尺寸分布和包封效率(EE)受共聚物与DOX的进料重量比以及纳米颗粒的不同制备方法的影响。此外,体外释放实验表明释放行为受释放介质pH值的影响。装有DOX的纳米颗粒显示,在pH 5.0下的释放比在pH 7.4缓冲液下的释放更快。载有DOX的共聚物纳米颗粒在体外和体内均表现出与游离药物相当的抗癌功效。这些结果证明明胶衍生物作为有希望的用于递送抗肿瘤药物的纳米载体的可行应用。

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