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Improved Bioavailability of Curcumin in Gliadin-Protected Gold Quantum Cluster for Targeted Delivery

机译:姜黄素在麦醇溶蛋白保护的金量子簇中用于靶向递送的提高的生物利用度

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This study deals with the synthesis of a gliadin-stabilized gold quantum cluster (AuQC) for the encapsulation of curcumin (CUR) and its targeted delivery to the cancer cell. CUR is an anticancer drug containing a hydrophobic polyphenol derived from the rhizome of Curcuma longa. The utilization of CUR in cancer treatment is limited because of suboptimal pharmacokinetics and poor bioavailability at the tumor site. In order to improve the bioavailability of CUR, we have encapsulated it into AuQCs stabilized by a proline-rich protein gliadin because proline-rich protein has the ability to bind a hydrophobic drug CUR. The encapsulation of CUR into the hydrophobic cavity of the protein was confirmed by various spectroscopic techniques. Compared to CUR alone, the encapsulated CUR was stable against degradation and showed higher pH stability up to pH 8.5. The encapsulation efficiency of CUR in AuQCs was calculated as 98%, which was much higher than the other reported methods. In vitro drug release experiment exhibited a controlled and pH-dependent CUR release over a period of 60 h. The encapsulated CUR-QCs exhibited less toxicity in the normal cell line (L929) and high toxicity in breast cancer (MDA-MB239). Thus, it can be used as a potential material for anticancer therapy and bioimaging.
机译:这项研究涉及麦醇溶蛋白稳定的金量子簇(AuQC)的合成,用于姜黄素(CUR)的封装及其向癌细胞的靶向递送。 CUR是一种抗癌药,含有一种源自姜黄根茎的疏水性多酚。由于药物动力学欠佳且肿瘤部位的生物利用度较差,因此限制了CUR在癌症治疗中的应用。为了提高CUR的生物利用度,我们将其封装到由富含脯氨酸的蛋白麦醇溶蛋白稳定的AuQC中,因为富含脯氨酸的蛋白具有结合疏水性药物CUR的能力。通过各种光谱技术证实了CUR在蛋白质的疏水腔中的包封。与单独的CUR相比,包封的CUR对降解是稳定的,并且在高达pH 8.5的条件下显示出更高的pH稳定性。据计算,AuQC中CUR的封装效率为98%,远高于其他报道的方法。体外药物释放实验显示60小时内可控且依赖pH的CUR释放。封装的CUR-QC在正常细胞系(L929)中表现出较小的毒性,而在乳腺癌(MDA-MB239)中表现出较高的毒性。因此,它可用作抗癌治疗和生物成像的潜在材料。

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