Targeted delivery of insoluble cargo (paclitaxel) by PEGylated chitosan nanoparticles grafted with Arg-Gly-Asp (RGD)

Molecular Pharmaceutics
Pi-Ping LvGuang-Hui Ma

Abstract

Poor delivery of insoluble anticancer drugs has so far precluded their clinical application. In this study, we developed a tumor-targeting delivery system for insoluble drug (paclitaxel, PTX) by PEGylated O-carboxymethyl-chitosan (CMC) nanoparticles grafted with cyclic Arg-Gly-Asp (RGD) peptide. To improve the loading efficiency (LE), we combined O/W/O double emulsion method with temperature-programmed solidification technique and controlled PTX within the matrix network as in situ nanocrystallite form. Furthermore, these CMC nanoparticles were PEGylated, which could reduce recognition by the reticuloendothelial system (RES) and prolong the circulation time in blood. In addition, further graft of cyclic RGD peptide at the terminal of PEG chain endowed these nanoparticles with higher affinity to in vitro Lewis lung carcinoma (LLC) cells and in vivo tumor tissue. These outstanding properties enabled as-designed nanodevice to exhibit a greater tumor growth inhibition effect and much lower side effects over the commercial formulation Taxol.

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Citations

Dec 12, 2013·Journal of Materials Science. Materials in Medicine·Zhonggen ShiYuanming Zhang
Jan 24, 2014·International Journal of Pharmaceutics·Ubonvan TermsarasabDae-Duk Kim
May 9, 2014·Journal of Controlled Release : Official Journal of the Controlled Release Society·Laxmi UpadhyayaRavi Prakash Tewari
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Apr 24, 2019·Advanced Pharmaceutical Bulletin·Mojtaba AbbasianRoya Salehi
Apr 21, 2016·Journal of Materials Chemistry. B, Materials for Biology and Medicine·Wei WeiGuanghui Ma
Jan 21, 2018·Journal of Materials Chemistry. B, Materials for Biology and Medicine·Hua YueGuanghui Ma
Jun 30, 2019·Current Medicinal Chemistry·Mehdi RajabiShaker A Mousa
Mar 7, 2015·Journal of Materials Chemistry. B, Materials for Biology and Medicine·Yunfei MoYuanming Zhang
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May 6, 2021·Materials Science & Engineering. C, Materials for Biological Applications·Parvin Sadat MirzaghavamiVahid Pirhajati Mahabadi
Jul 25, 2019·ACS Applied Materials & Interfaces·Yuxiang SunFei Xiong

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