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叶酸偶联姜黄素载药生物可降解聚合物阿魏酸明胶微球用于三阴性乳腺癌的体内外研究

Folic acid conjugated curcumin loaded biopolymeric gum acacia microsphere for triple negative breast cancer therapy in invitro and invivo model.

机构信息

Department of Life Science and Biotechnology, Jadavpur University, Kolkata 700032, India; Division of Molecular Medicine and Centre for Translational Research, Bose Institute, Kolkata 700056, India.

Department of Physics, Jadavpur University, Kolkata 700032, India.

出版信息

Mater Sci Eng C Mater Biol Appl. 2019 Feb 1;95:204-216. doi: 10.1016/j.msec.2018.10.071. Epub 2018 Oct 22.

DOI:10.1016/j.msec.2018.10.071
PMID:30573243
Abstract

Among the different types of biomaterials, natural excipients gum acacia (GA) is economic and has the potential for controlled drug delivery. We have synthesized GA microspheres by co-precipitation method and characterized them by XRD, FESEM, H NMR, FTIR, UV visible spectra and DLS. Despite its potential anti-cancer activity, solubility of curcumin is very low rendering its limit in application. We have used GA microspheres where curcumin can be loaded comfortably and thereby increases its bioavailability. The cytotoxicity of curcumin encapsulated GA microspheres was evaluated on triple negative breast cancer cell lines. They were found to induce apoptosis by perturbing the mitochondrial membrane potential. Folic acid was conjugated to curcumin encapsulated GA microspheres, for delivering it specifically to the cancer cells. The in-vivo study in BALB/C mice model exhibited more tumor regression in case of folic acid targeted curcumin encapsulated GA microsphere. Our results implicates that these microspheres can be an effective therapeutic agent to folate receptors over expressing cancer cells.

摘要

在不同类型的生物材料中,天然赋形剂阿拉伯胶(GA)具有经济实惠且具有控制药物释放的潜力。我们通过共沉淀法合成了 GA 微球,并通过 XRD、FESEM、H NMR、FTIR、UV 可见光谱和 DLS 对其进行了表征。尽管姜黄素具有潜在的抗癌活性,但它的溶解度非常低,限制了其应用。我们使用 GA 微球来负载姜黄素,从而提高其生物利用度。用三阴性乳腺癌细胞系评估了包载姜黄素的 GA 微球的细胞毒性。结果发现,它们通过扰乱线粒体膜电位诱导细胞凋亡。将叶酸偶联到包载姜黄素的 GA 微球上,使其能够特异性递送到癌细胞。在 BALB/C 小鼠模型中的体内研究表明,叶酸靶向包载姜黄素的 GA 微球的肿瘤消退更多。我们的结果表明,这些微球可以成为叶酸受体过度表达的癌细胞的有效治疗剂。

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