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Novel Ph-Triggered Biocompatible Polymeric Micelles Based on Heparin–Α-Tocopherol Conjugate for Intracellular Delivery of Docetaxel in Breast Cancer Publisher Pubmed



Emami J1 ; Kazemi M1 ; Hasanzadeh F2 ; Minaiyan M3 ; Mirian M4 ; Lavasanifar A5
Authors
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Authors Affiliations
  1. 1. Department of Pharmaceutics, School of Pharmacy and Pharmaceutical Sciences, Isfahan University of Medical Sciences, Isfahan, Iran
  2. 2. Department of Medical Chemistry, School of Pharmacy and Pharmaceutical Sciences, Isfahan University of Medical Sciences, Isfahan, Iran
  3. 3. Department of Pharmacology, School of Pharmacy and Pharmaceutical Sciences, Isfahan University of Medical Sciences, Isfahan, Iran
  4. 4. Department of Biotechnology, School of Pharmacy and Pharmaceutical Sciences, Isfahan University of Medical Sciences, Isfahan, Iran
  5. 5. Faculty of Pharmacy and Pharmaceutical Sciences, University of Alberta, Edmonton, Canada

Source: Pharmaceutical Development and Technology Published:2020


Abstract

In this study, pH-triggered polymeric micelle comprising α-tocopherol (TOC) and heparin (HEP) was developed and loaded with docetaxel (DTX). The amphiphilic copolymer was synthesized by grafting TOC onto HEP backbone by a pH-cleavable bond. DTX-loaded micelles were characterized in terms of critical micelle concentration (CMC), particle size, zeta potential, entrapment efficiency (EE), pH-responsive behavior, and drug release. In vitro cytotoxicity of the micelles against breast cancer cells was investigated by MTT assay. The cellular uptake of coumarin-loaded micelles was also evaluated. Furthermore, the pharmacokinetics of DTX-loaded micelles was evaluated and compared with that of Taxotere®. HEP–CA–TOC copolymers showed low CMC values and high EE. At pH 7.4, the micelles remained stable in size and shape, whereas considerable changes in particle size and morphology were observed at pH 5.5. DTX-loaded micelles showed pH-dependent drug release profiles. Coumarin-loaded micelles showed higher cellular uptake than free coumarin. Therefore, the DTX-loaded micelles showed more toxicity against breast cancer cells than free DTX. A significant increase in T1/2 β, AUC0-∞ and MRT was observed in DTX-loaded micelle treated group as compared to the group treated with Taxotere®. The results suggest that the pH-sensitive HEP-modified micelles could be promising for enhanced intracellular drug delivery of DTX for cancer treatment. © 2020, © 2020 Informa UK Limited, trading as Taylor & Francis Group.
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