Novel 4-Arm PolyEthylene Glycol-Block-PolyAnhydride-Esters Amphiphilic Copolymer Micelles Loading Curcumin: Preparation, Characterization, and In Vitro EvaluationReport as inadecuate




Novel 4-Arm PolyEthylene Glycol-Block-PolyAnhydride-Esters Amphiphilic Copolymer Micelles Loading Curcumin: Preparation, Characterization, and In Vitro Evaluation - Download this document for free, or read online. Document in PDF available to download.

BioMed Research InternationalVolume 2013 2013, Article ID 507103, 11 pages

Research Article

School of Pharmacy, Shanghai Jiao Tong University, Shanghai 200240, China

School of Pharmacy, Hubei University of Science and Technology, Xianning 437100, China

Received 8 April 2013; Accepted 2 June 2013

Academic Editor: Ajit S. Narang

Copyright © 2013 Li Lv et al. This is an open access article distributed under the Creative Commons Attribution License, which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.

Abstract

A novel 4-arm polyethylene glycol-block-polyanhydride-esters amphiphilic copolymer 4-arm PEG-b-PAE was synthesized by esterization of 4-arm polyethylene glycol and polyanhydride-esters which was obtained by melt polycondensation of α-, ω-acetic anhydride terminated polyL-lactic acid. The obtained 4-arm PEG-b-PAE was characterized by

H-NMR and gel permeation chromatography. The critical micelle concentration of 4-arm PEG-b-PAE was 2.38 μg-mL. The curcumin-loaded 4-arm PEG-b-PAE micelles were prepared by a solid dispersion method and the drug loading content and encapsulation efficiency of the micelles were 7.0% and 85.2%, respectively. The curcumin-loaded micelles were spherical with a hydrodynamic diameter of 151.9 nm. Curcumin was encapsulated within 4-arm PEG-b-PAE micelles amorphously and released from the micelles, faster in pH 5.0 than pH 7.4, presenting one biphasic drug release pattern with rapid release at the initial stage and slow release later. The hemolysis rate of the curcumin-loaded 4-arm PEG-b-PAE micelles was 3.18%, which was below 5%. The IC50 value of the curcumin-loaded micelles against Hela cells was 10.21 μg-mL, lower than the one of free curcumin 25.90 μg-mL. The cellular uptake of the curcumin-loaded micelles in Hela cell increased in a time-dependent manner. The curcumin-loaded micelles could induce G2-M phase cell cycle arrest and apoptosis of Hela cells.





Author: Li Lv, Yuanyuan Shen, Min Li, Xiaofen Xu, Mingna Li, Shengrong Guo, and Shengtang Huang

Source: https://www.hindawi.com/



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