Journal
CHINESE CHEMICAL LETTERS
Volume 30, Issue 12, Pages 2027-2031Publisher
ELSEVIER SCIENCE INC
DOI: 10.1016/j.cclet.2019.04.052
Keywords
Polyethylene glycol; Doxorubicin; Prodrug; Schiff-base reaction; pH-Responsiveness
Categories
Funding
- National Natural Science Foundation of China [21374066]
- Major Program of the Natural Science Project of Jiangsu Higher Education Institutions [15KJA150007]
- Natural Science Foundation of Jiangsu Province [BK20171212]
- Priority Academic Program Development (PAPD) of Jiangsu Higher Education Institutions
- Soochow-Waterloo University Joint Project for Nanotechnology from Suzhou Industrial Park
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PEGylated prodrug, covalent attaching polyethylene glycol (PEG) polymer chains to therapeutic drugs, is one of the most promising techniques to improve the water-solubility, stability, and therapeutic effect of drugs. In this study, three PEGylated acid-sensitive prodrugs DOX-PEG-DOX with different molecular weights, were prepared via Schiff-base reaction between aldehyde-modified PEG and the amino groups of doxorubicin (DOX). This kind of amphiphilic polymeric prodrug could be self-assemble into nanoparticles in aqueous solution. The average particle size and morphologies of the prodrug nanoparticles under different pH conditions were observed by dynamic light scattering (DLS) and transmission electron microscopy (TEM), respectively. It turned out that the nanoparticles could be kept stable in the physiological environment, but degraded in acidic medium. Subsequently, we also investigated in vitro drug release behavior and found that the prodrug had acid-sensitive property. The cytotoxicity and intracellular uptake assays revealed that the prodrugs could rapidly internalized by HeLa or FlepG2 cells to release DOX and effectively inhibited the proliferation of the tumor cells, which have the potential for use in cancer therapy. (C) 2019 Chinese Chemical Society and Institute of Materia Medica, Chinese Academy of Medical Sciences. Published by Elsevier B.V. All rights reserved.
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