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一项关于使用与叶酸偶联的生物相容性聚乳酸-羟基乙酸共聚物(PLGA)微球将姜黄素靶向递送至人三阴性乳腺癌细胞的研究。

An Study for Targeted Delivery of Curcumin in Human Triple Negative Breast Carcinoma Cells Using Biocompatible PLGA Microspheres Conjugated with Folic Acid.

作者信息

Pal Kunal, Laha Dipranjan, Parida Pravat Kumar, Roy Shubham, Bardhan Souravi, Dutta Ananya, Jana Kuladip, Karmakar Parimal

机构信息

Department of Life Science and Biotechnology, Jadavpur University, Kolkata 700032, India.

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

出版信息

J Nanosci Nanotechnol. 2019 Jul 1;19(7):3720-3733. doi: 10.1166/jnn.2019.16292.

DOI:10.1166/jnn.2019.16292
PMID:30764928
Abstract

Among the different types of polymeric vehicles, (PLGA) is biodegradable and has emerged as promising tool for the delivery of cancer therapeutics. The salient features of PLGA micro carriers include prolonged circulation time, increased tumor localization and biodegradability and effectiveness of the therapeutics. We have synthesized PLGA microspheres where curcumin can be loaded and thereby increases its bioavailability. The cytotoxicity of curcumin (PLGA@CCM) microspheres was evaluated on triple negative breast cancer (TNBC) cell lines. They were found to induce apoptosis by perturbing the mitochondrial membrane potential. PLGA@CCM@FA induces apoptosis in human triple negative breast cancer cells by up-regulating Cleaved caspase-3 and down regutes p-AKT. The study in BALB/C mice model exhibited more tumor regression in case of PLGA@CCM@FA microspheres. Our results suggests that these microspheres can be an effective vehicle for delivery of hydrophobic drugs to the folate over expressed cancer cells.

摘要

在不同类型的聚合物载体中,聚乳酸-羟基乙酸共聚物(PLGA)是可生物降解的,并且已成为递送癌症治疗药物的一种有前景的工具。PLGA微载体的显著特点包括延长循环时间、增加肿瘤定位以及治疗药物的生物降解性和有效性。我们已经合成了可以负载姜黄素的PLGA微球,从而提高其生物利用度。对姜黄素(PLGA@CCM)微球在三阴性乳腺癌(TNBC)细胞系上的细胞毒性进行了评估。发现它们通过扰乱线粒体膜电位来诱导细胞凋亡。PLGA@CCM@FA通过上调裂解的半胱天冬酶-3和下调p-AKT来诱导人三阴性乳腺癌细胞凋亡。在BALB/C小鼠模型中的研究表明,PLGA@CCM@FA微球的情况下肿瘤消退更为明显。我们的结果表明,这些微球可以成为将疏水性药物递送至叶酸过表达癌细胞的有效载体。

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