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首页> 外文期刊>Asian Journal of Pharmaceutical Sciences >Polyelectrolyte complex micelles by self-assembly of polypeptide-based triblock copolymer for doxorubicin delivery
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Polyelectrolyte complex micelles by self-assembly of polypeptide-based triblock copolymer for doxorubicin delivery

机译：通过自组装基于多肽的三嵌段共聚物自组装的聚电解质复合胶束

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Abstract Polyelectrolyte complex micelles were prepared by self-assembly of polypeptide-based triblock copolymer as a new drug carrier for cancer chemotherapy. The triblock copolymer, poly(l-aspartic acid)-b-poly(ethylene glycol)-b-poly(l-aspartic acid) (PLD-b-PEG-b-PLD), spontaneously self-assembled with doxorubicin (DOX) via electrostatic interactions to form spherical micelles with a particle size of 60–80?nm (triblock ionomer complexes micelles, {TBIC} micelles). These micelles exhibited a high loading capacity of 70% (w/w) at a drug/polymer ratio of 0.5 at pH 7.0. They showed pH-responsive release patterns, with higher release at acidic pH than at physiological pH. Furthermore, DOX-loaded {TBIC} micelles exerted less cytotoxicity than free {DOX} in the A-549 human lung cancer cell line. Confocal microscopy in A-549 cells indicated that DOX-loaded {TBIC} micelles were transported into lysosomes via endocytosis. These micelles possessed favorable pharmacokinetic characteristics and showed sustained {DOX} release in rats. Overall, these findings indicate that PLD-b-PEG-b-PLD polypeptide micelles are a promising approach for anti-cancer drug delivery.
机译：摘要通过自组装基于多肽的三嵌段共聚物作为癌症化疗的新药载体，制备了聚电解质复合胶束。三嵌段共聚物，聚（1-天冬氨酸）-b-聚（乙二醇）-b-聚（1-天冬氨酸）（PLD-b-PEG-b-PLD），与阿霉素（DOX）自发自组装通过静电相互作用形成粒径为60–80？nm的球形胶束（三嵌段离聚物络合物胶束， {TBIC }胶束）。这些胶束在pH 7.0的药物/聚合物比为0.5时表现出70％（w / w）的高负载能力。他们显示出pH响应释放模式，在酸性pH下的释放高于在生理pH下的释放。此外，在A-549人肺癌细胞系中，装载DOX的 {TBIC }胶束比游离 {DOX }产生的细胞毒性要小。 A-549细胞的共聚焦显微镜检查表明，装载DOX的 {TBIC }胶束通过内吞作用被转运到溶酶体中。这些胶束具有良好的药代动力学特征，并在大鼠中表现出持续的 {DOX }释放。总体而言，这些发现表明，PLD-b-PEG-b-PLD多肽胶束是一种有前途的抗癌药物递送方法。

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