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首页> 外文期刊>RSC Advances >pH-responsive flower-like micelles constructed via oxime linkage for anticancer drug delivery
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pH-responsive flower-like micelles constructed via oxime linkage for anticancer drug delivery

机译：通过肟键构建的pH响应性花状胶束，用于抗癌药物的递送

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A new type of pH-responsive flower-like micelle based on backbone-cleavable triblock copolymer polycaprolactone-oxime-poly(ethylene glycol)-oxime-polycaprolactone (PCL-OPEG-PCL) was developed for anticancer drug delivery. Firstly, PCL-OPEG-PCL was synthesized by ring-opening polymerization. The structure of PCL-OPEG-PCL was confirmed by H-1 NMR and Fourier transform infrared spectroscopy (FTIR). Benefiting from the amphiphilic character and unique molecular architecture with the hydrophilic PEG and hydrophobic PCL segments, PCL-OPEG-PCL could self-assemble into flower-like micelles in aqueous solution, which has been demonstrated by transmission electron microscopy (TEM) and dynamic light scattering (DLS). The cytotoxicity of the flower-like micelles was evaluated by MTT assay against NIH/3T3 normal cells. Doxorubicin (DOX), a model anticancer drug, was encapsulated into these flower-like micelles with high efficiency. The in vitro study showed that DOX-loaded flower-like micelles possessed high stability at physiological pH of 7.4, whereas the DOX release from the flower-like micelles was significantly accelerated at mildly acidic pH of 5.0, demonstrating the pH-responsive feature of the drug carrier with oxime linkages. DOX-loaded flower-like micelles were investigated for proliferation inhibition of Hela cells in vitro, and the DOX dose required for 50% cellular growth inhibition was found to be 1.81 mu g mL(-1). All of these results demonstrate that flower-like micelles self-assembled from PCL-OPEG-PCL triblock copolymers can be used as effective and promising drug nanocarriers.
机译：开发了一种基于骨架可裂解的三嵌段共聚物聚己内酯-肟-聚（乙二醇）-肟-聚己内酯（PCL-OPEG-PCL）的新型pH响应花状胶束，用于抗癌药物的递送。首先，通过开环聚合合成PCL-OPEG-PCL。 PCL-OPEG-PCL的结构通过H-1 NMR和傅立叶变换红外光谱（FTIR）确认。得益于亲水性PEG和疏水性PCL片段的两亲特性和独特的分子结构，PCL-OPEG-PCL可以在水溶液中自组装成花状胶束，这已通过透射电子显微镜（TEM）和动态光证明散射（DLS）。通过MTT测定法对NIH / 3T3正常细胞评价了花状胶束的细胞毒性。模型抗癌药阿霉素（DOX）被高效地封装在这些花状胶束中。体外研究表明，载有DOX的花状胶束在7.4的生理pH下具有较高的稳定性，而在中等酸性pH值为5.0时，从花状胶束释放的DOX明显加速，这证明了DOX的pH响应特性。具有肟键的药物载体。研究了负载DOX的花状胶束对Hela细胞的体外增殖抑制作用，发现抑制50％细胞生长所需的DOX剂量为1.81μg mL（-1）。所有这些结果表明，由PCL-OPEG-PCL三嵌段共聚物自组装而成的花状胶束可用作有效和有前途的药物纳米载体。

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