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首页> 美国卫生研究院文献>Pharmaceutics >Fabrication of Core Crosslinked Polymeric Micelles as Nanocarriers for Doxorubicin Delivery: Self-Assembly In Situ Diselenide Metathesis and Redox-Responsive Drug Release
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Fabrication of Core Crosslinked Polymeric Micelles as Nanocarriers for Doxorubicin Delivery: Self-Assembly In Situ Diselenide Metathesis and Redox-Responsive Drug Release

机译：核心交联聚合物胶束的制备作为多柔比蛋白递送的纳米载体：自组装原位五硒化物复分解和氧化还原响应药物释放

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Polymeric micelles (PMs) have been used to improve the poor aqueous solubility, slow absorption and non-selective biodistribution of chemotherapeutic agents (CAs), albeit, they suffer from disassembly and premature release of payloads in the bloodstream. To alleviate the thermodynamic instability of PMs, different core crosslinking approaches were employed. Herein, we synthesized the poly(ethylene oxide)-b-poly((2-aminoethyl)diselanyl)ethyl l-aspartamide)-b-polycaprolactone (mPEG-P(LA-DSeDEA)-PCL) copolymer which self-assembled into monodispersed nanoscale, 156.57 ± 4.42 nm, core crosslinked micelles (CCMs) through visible light-induced diselenide metathesis reaction between the pendant selenocystamine moieties. The CCMs demonstrated desirable doxorubicin (DOX)-loading content (7.31%) and encapsulation efficiency (42.73%). Both blank and DOX-loaded CCMs (DOX@CCMs) established appreciable colloidal stability in the presence of bovine serum albumin (BSA). The DOX@CCMs showed redox-responsive drug releasing behavior when treated with 5 and 10 mM reduced glutathione (GSH) and 0.1% H2O2. Unlike the DOX-loaded non-crosslinked micelles (DOX@NCMs) which exhibited initial burst release, DOX@CCMs demonstrated a sustained release profile in vitro where 71.7% of the encapsulated DOX was released within 72 h. In addition, the in vitro fluorescent microscope images and flow cytometry analysis confirmed the efficient cellular internalization of DOX@CCMs. The in vitro cytotoxicity test on HaCaT, MDCK, and HeLa cell lines reiterated the cytocompatibility (≥82% cell viability) of the mPEG-P(LA-DSeDEA)-PCL copolymer and DOX@CCMs selectively inhibit the viabilities of 48.85% of HeLa cells as compared to 15.75% of HaCaT and 7.85% of MDCK cells at a maximum dose of 10 µg/mL. Overall, all these appealing attributes make CCMs desirable as nanocarriers for the delivery and controlled release of DOX in tumor cells.
机译：已经使用聚合物胶束（PMS）来改善化学治疗剂（CAS）的差的水溶性，缓慢吸收和非选择性生物分布，尽管它们患有拆卸和血液中有效载荷的过早释放。为了减轻PM的热力学不稳定性，采用不同的核心交联方法。在此，我们合成了聚（环氧乙烷）-B-聚（（2-氨基乙基）二烯基）乙基L-己二烯酰胺（MPEG-P（La-Dsedea）-pcl）共聚物，其自组装成单分散的共聚物纳米级，156.57±4.42nm，通过垂直硒胱氨酸胺部分之间的可见光诱导的五烯醇复分解反应，核交联胶束（CCMS）。 CCMS证明了无意义的多柔比星（DOX） - 载荷含量（7.31％）和封装效率（42.73％）。在牛血清白蛋白（BSA）存在下，坯料和DOX加载的CCMS（DOX @ CCMS）建立了明显的胶体稳定性。当用5和10mM降低的谷胱甘肽（GSH）和0.1％H 2 O 2处理时，DOX @ CCMS显示氧化还原响应药物释放行为。与展示初始爆发释放的DOX加载的非交联胶束（DOX @ NCMS）不同，DOX @ CCMS在体外显示持续释放曲线，其中71.7％的包封DOX在72小时内释放。此外，体外荧光显微镜图像和流式细胞术分析证实了DOX @ CCM的有效蜂窝内化。 HaCAT，MDCK和HeLa细胞系上的体外细胞毒性试验重新突出了MPEG-P（La-Dsedea）-pcl共聚物和DOX @ CCMS的细胞相容性（≥82％的细胞活力）选择性地抑制48.85％的Hela的稳定性细胞相比，占HACAT的15.75％，最大剂量为10μg/ ml的MDCK细胞的1.85％。总体而言，所有这些吸引品属性使CCM成为纳米载体中所需的纳米载体，用于在肿瘤细胞中递送和控制释放DOX。

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