Abstract

The present study investigates the effect of the length of the hydrophobic poly(D,L-lactide) block on the self-assembly behavior of amphiphilic poly(D,L-lactide)-b-poly(ethylene glycol) (P(D,L)LA-b-PEG_5k) copolymers with a large variation in molecular weight of the hydrophobic block (ranging from 5 to 100 kDa). To evaluate the cytotoxic effect of oxaliplatin-loaded P(D,L)LA-b-PEG_5k nanoparticles (OXA-NPs) prepared by the nanoprecipitation method, a half maximal inhibitory concentration (IC₅₀) study was conducted in cancer cell lines (MCF7, HCT116, and A549). The assays revealed that the IC₅₀ values for OXA-NPs in HCT116 (1.93 ± 0.08 nM) and A549 (2.84 ± 0.11 nM) were significantly lower than those of pure OXA (12.70 ± 1.14 and 29.30 ± 0.40 nM, respectively). Moreover, the results showed that normal fibroblasts treated with blank NPs exhibited no significant growth inhibition in the concentration range of 0.001–1 mg mL^–1, indicating their high biocompatibility.

中文翻译：

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用于改善奥沙利铂递送的 PEG-b-PLA 纳米颗粒的自组装行为和细胞毒性：PLA 块长度的影响

摘要

本研究探讨了疏水性聚(D,L-丙交酯)嵌段的长度对两亲性聚(D,L-丙交酯)-b-聚(乙二醇)(P( D , L)LA- b -PEG _5k ) 共聚物，疏水性嵌段的分子量变化较大（范围为 5 至 100 kDa）。为了评价纳米沉淀法制备的负载奥沙利铂的P(D,L)LA- b -PEG _5k纳米颗粒(OXA-NPs)的细胞毒作用，在癌细胞系中进行了半数抑制浓度(IC ₅₀ )研究( MCF7、HCT116 和 A549）。测定结果显示，HCT116 (1.93 ± 0.08 nM) 和 A549 (2.84 ± 0.11 nM) 中 OXA-NP 的 IC ₅₀值显着低于纯 OXA（分别为 12.70 ± 1.14 和 29.30 ± 0.40 nM）。此外，结果显示，空白纳米粒子处理的正常成纤维细胞在0.001–1 mg mL ^–1的浓度范围内没有表现出明显的生长抑制，表明其具有较高的生物相容性。