in vitro biological evaluation of folate-functionalized block copolymer micelles for selective anti-cancer drug delivery

Macromolecular Bioscience
Mariano LicciardiAndrew L Lewis

Abstract

The main objective of this study was to evaluate the ability of folic acid-functionalized diblock copolymer micelles to improve the delivery and uptake of two poorly water-soluble anti-tumor drugs, tamoxifen and paclitaxel, to cancer cells through folate receptor targeting. The diblock copolymer used in this study comprised a hydrophilic poly[2-(methacryloyloxy)ethyl phosphorylcholine] (MPC) block, carrying at the chain end the folate targeting moiety, and a pH-sensitive hydrophobic poly[2-(diisopropylamino)ethyl methacrylate] (DPA) block (FA-MPC-DPA). The drug-loading capacities of tamoxifen- and paclitaxel-loaded micelles were determined by high performance liquid chromatography and the micelle dimensions were determined by dynamic light scattering and transmission electron microscopy. Cell viability studies were carried out on human chronic myelogenous leukaemia (K-562) and colon carcinoma cell lines (Caco-2) in order to demonstrate that drug-loaded FA-MPC-DPA micelles exhibited higher cytotoxicities toward cancer cells than unfunctionalized MPC-DPA micelles. Uptake studies confirmed that folate-conjugated micelles led to increased drug uptake within cancer cells, demonstrating the expected selectivity toward these tumor cells.

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Citations

Aug 10, 2010·Journal of Ovarian Research·Murali M YallapuSubhash C Chauhan
Jul 12, 2014·Journal of Drug Targeting·Masamichi NakayamaTeruo Okano
May 9, 2012·Journal of Biomedical Materials Research. Part a·Huaihong ZhangBaiwang Sun
Apr 7, 2017·ACS Applied Materials & Interfaces·Anna Li VolsiGaetano Giammona
Jun 21, 2017·European Journal of Pharmaceutical Sciences : Official Journal of the European Federation for Pharmaceutical Sciences·Abdul Khaliq Elzhry ElyafiJonathan P Salvage
Aug 19, 2009·Macromolecular Bioscience·Tiancheng LuXiabin Jing
Dec 15, 2019·Polymers·Gaetano Giammona, Emanuela Fabiola Craparo
Dec 15, 2020·Journal of Chromatography. a·Javier González-SálamoJavier Hernández-Borges
Aug 18, 2020·Computational and Structural Biotechnology Journal·Ling-Yan ZhouZhi-Yao He
Nov 6, 2021·Journal of Molecular Recognition : JMR·Manjeet Harijan, Meenakshi Singh

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