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首页> 外文期刊>Materials science & engineering >Enzymatic synthesis of PEGylated lactide-diester-diol copolyesters for highly efficient targeted anticancer drug delivery
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Enzymatic synthesis of PEGylated lactide-diester-diol copolyesters for highly efficient targeted anticancer drug delivery

机译：酶合成聚乙二醇化丙交酯 - 二醇共聚酯，用于高效靶向抗癌药物递送

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摘要

PEGylated lactide-diester-diol copolymers were successfully synthesized via lipase-catalyzed copolymerization, the resultant amphiphilic PEG-poly(L-lactate-co-hexamethylene-co-adipate) (PEG-PLLHA) and PEG-poly(D,L-lactate-co-hexamethylene-co-adipate) (PEG-PDLLHA) block copolymers readily undergo self-assembly processes to form nanosized micelles in aqueous medium, which are stable under physiological conditions in the presence of serum proteins. By conjugating folic acid (FA) to enzymatic synthesized poly(hexamethylene adipate-co-hexamethylene 2,3-epoxy succinate), we could formulate FA-bearing PEG-polyester micelles for docetaxel (DTX) targeting delivery. FA-PEG-PLLHA and FA-PEG-PDLLHA micelles possess efficient cell-targeting capability toward FA receptor-positive cancer cells (e.g., CT-26), which significantly enhances their cellular uptake rates and efficacy of drug-loaded formulations toward such cells. During in vivo anticancer treatments, the FA-bearing micelles are highly capable of targeting and accumulating preferentially in tumor tissues by both active cell-targeting mechanism and passive targeting via the EPR effect. All these desirable properties enable the FA-bearing micelles to deliver DTX with 97% tumor-inhibiting efficiency through systemic delivery, which is favorable in comparison to the values of various DTX nanoparticle formulations reported in literature. Importantly, biosafety assays reveal that all DTX-loaded micelles are biocompatible and safe for in vivo antitumor treatment applications. Thus, FA-PEG-PLLHA and FA-PEG-PDLLHA micelles represent new types of promising anticancer drug nanocarriers for targeted chemotherapy.
机译：通过脂肪酶催化的共聚成功地合成Pegymated丙交酯 - 二醇共聚物，所得的两亲的PEG - 聚（L-乳酸共聚六甲基 - 共同己二酸）（PEG-PLLHA）和PEG-Poly（D，L-乳酸） -Co-六亚甲基 - 共己二酸酯（PEG-PDLLHA）嵌段共聚物容易经历自组装方法，以在血清蛋白存在下在生理条件下稳定地形成纳米化胶束。通过将叶酸（Fa）缀合至酶合成聚（六亚甲基己二酸酯 - 共六甲基2,3-环氧琥珀酸盐），我们可以为多西紫杉醇（DTX）靶向递送的Fa承载的PEG聚酯胶束。 FA-PEG-PLLHA和FA-PEG-PDLLHA胶束对FA受体阳性癌细胞（例如，CT-26）具有有效的细胞靶向能力，其显着提高了它们的蜂窝摄取率和药物负载制剂对这些细胞的功效。在体内抗癌治疗期间，通过活性细胞靶向机构和通过EPR效应的无源靶向，对轴承胶束能够靶向和积累肿瘤组织中的靶向和积累。所有这些所需的性能使得FA轴承胶束使得通过全身递送提供97％抑制肿瘤抑制效率的DTX，与文献中报道的各种DTX纳米粒子配方的值相比，这是有利的。重要的是，生物安全测定表明，所有DTX负载的胶束都是生物相容的，并且在体内抗肿瘤处理应用中是安全的。因此，Fa-PEG-PLLHA和FA-PEG-PDLLHA胶束代表了用于靶向化疗的新型抗癌药物纳米载体。

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