文献类型：期刊文献

英文题名：PEGylated-PLGA Nanoparticles Coated with pH-Responsive Tannic Acid-Fe(III) Complexes for Reduced Premature Doxorubicin Release and Enhanced Targeting in Breast Cancer

作者：Hu, Fabiao[1];Zhang, Ruihuan[1];Guo, Wei[1];Yan, Ting[1];He, Xiujuan[2];Hu, Fengzhi[2];Ren, Fuzheng[2];Ma, Xingyuan[1];Lei, Jiandu[3];Zheng, Wenyun[2]

机构：[1]East China Univ Sci & Technol, State Key Lab Bioreactor Engn, Shanghai 200237, Peoples R China;[2]East China Univ Sci & Technol, Sch Pharm, Shanghai Key Lab New Drug Design, Shanghai 200237, Peoples R China;[3]Beijing Forestry Univ, Beijing Key Lab Lignocellulos Chem, Beijing 100083, Peoples R China

年份：2021

卷号：18

期号：6

起止页码：2161

外文期刊名：MOLECULAR PHARMACEUTICS

收录：;WOS:【SCI-EXPANDED(收录号:WOS:000661309800004)】；

基金：This study was supported by the National Key Research and Development Project of China (2018YFA0902804), the National Natural Science Foundation (31670944, 81673345), and the Science and Technology Innovation Action Plan of Shanghai (17431904600). All animal procedures were performed in accordance with Chinese legislation on the Use and Care of Research Animals (Document No. 55, 2001) and the Guidelines for Care and Use of Laboratory Animals of East China University of Science and Technology University and experiments were approved by the Animal Ethics Committee of East China University of Science and Technology.

语种：英文

外文关键词：TPLGA NPs; premature release effect inhibition; chemotherapy drug delivery; tumor tissue targeting

摘要：Biodegradable poly(lactic-co-glycolic acid) nanoparticles (PLGA NPs) have been widely used as delivery vehicles for chemotherapy drugs. However, premature drug release in PLGA NPs can damage healthy tissue and cause serious adverse effects during systemic administration. Here, we report a tannic acid-Fe(III) (Fe-III-TA) complex-modified PLGA nanoparticle platform (DOX-TPLGA NPs) for the tumor-targeted delivery of doxorubicin (DOX). A PEGylated-PLGA inner core and Fe-III-TA complex outer shell were simultaneously introduced to reduce premature drug release in blood circulation and increase pH-triggered drug release in tumor tissue. Compared to the unmodified NPs, the initial burst rate of DOX-TPLGA NPs was significantly reduced by nearly 2-fold at pH 7.4. Moreover, the cumulative drug release rate at pH 5.0 was 40% greater than that at pH 7.4 due to the pH-response of the FeIII-TA complex. Cellular studies revealed that the TPLGA NPs had enhanced drug uptake and superior cytotoxicity of breast cancer cells in comparison to free DOX. Additionally, the DOX-TPLGA NPs efficiently accumulated in the tumor site of 4T1-bearing nude mice due to the enhanced permeability and retention (EPR) effect and reached a tumor inhibition rate of 85.53 +/- 8.77% (1.31-fold versus DOX-PLGA NPs and 3.12-fold versus free DOX). Consequently, the novel TPLGA NPs represent a promising delivery platform to enhance the safety and efficacy of chemotherapy drugs.