Temperature and pH dual‐sensitive polyaspartamide derivatives for antitumor drug delivery |
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| Authors: | Yingying Ma Guangyan Zhang Lingjuan Li Huan Yu Jia Liu Chaoqun Wang Yanfeng Chu Renxi Zhuo Xulin Jiang |
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| Affiliation: | 1. Department of Chemistry, Key Laboratory of Biomedical Polymers of Ministry of Education, Wuhan University, Wuhan, People's Republic of China;2. Hubei Provincial Key Laboratory of Green Materials for Light Industry & Department of Light Industry, Hubei University of Technology, Wuhan, People's Republic of China |
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| Abstract: | The pH‐sensitive tertiary amino groups were introduced to synthesize temperature and pH dual‐sensitive degradable polyaspartamide derivatives (phe/DEAE‐g‐PHPA) containing pendant aromatic structures and ionizable tertiary amino groups. The thermo/pH‐responsive behavior of phe/DEAE‐g‐PHPA polymer can be tuned by adjusting the graft copolymer composition. Due to the pH sensitivity of the phe/DEAE‐g‐PHPA‐g‐mPEG polymer with hydrophilic long PEG chain, the micelles and the anticancer drug‐loaded micelles were prepared by a quick pH‐changing method without using toxic organic solvent. The obtained polymeric micelles, paclitaxel‐loaded micelles and doxorubicin‐loaded micelles were stable under physiological conditions. Both the drug‐loaded micelles showed much faster release at pH 5 than at pH 7.4. The doxorubicin‐loaded micelles showed obvious and better anticancer activity against both HepG2 and HeLa cells than free doxorubicin. Thus these nontoxic, dual thermo‐ and pH‐sensitive phe/DEAE‐g‐PHPA‐g‐mPEG micelles may be a promising anticancer drug delivery system. © 2015 Wiley Periodicals, Inc. J. Polym. Sci., Part A: Polym. Chem. 2016 , 54, 879–888 |
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| Keywords: | intelligent polymers stimulus‐responsive pH‐induced micellization poly(amino acids) polymeric nanoparticles |
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