Self-Assembled Micelles Composed of Doxorubicin Conjugated Y-Shaped PEG-Polyglutamic acid2 Copolymers via Hydrazone LinkersReport as inadecuate




Self-Assembled Micelles Composed of Doxorubicin Conjugated Y-Shaped PEG-Polyglutamic acid2 Copolymers via Hydrazone Linkers - Download this document for free, or read online. Document in PDF available to download.

1

Department of Pharmaceutics, College of Pharmacy Sciences, Jilin University, Changchun 130021, Jilin, China

2

Department of Pharmaceutics, Shenyang Pharmaceutical University, Shenyang 110016, China

3

School of Life Science and Biopharmaceutics, Shenyang Pharmaceutical University, Shenyang 110016, Liaoning, China





*

Authors to whom correspondence should be addressed.



Abstract In this work, micelles composed of doxorubicin-conjugated Y-shaped copolymers YMs linked via an acid-labile linker were constructed. Y-shaped copolymers of mPEG-b-polyglutamate-hydrazone-doxorubicin2 and linear copolymers of mPEG-b-polyglutamate-hydrazone-doxorubicin were synthesized and characterized. Particle size, size distribution, morphology, drug loading content DLC and drug release of the micelles were determined. Alterations in size and DLC of the micelles could be achieved by varying the hydrophobic block lengths. Moreover, at fixed DLCs, YMs showed a smaller diameter than micelles composed of linear copolymers LMs. Also, all prepared micelles showed sustained release behaviors under physiological conditions over 72 h. DOX loaded in YMs was released more completely, with 30% more drug released in acid. The anti-tumor efficacy of the micelles against HeLa cells was evaluated by MTT assays, and YMs exhibited stronger cytotoxic effects than LMs in a dose- and time-dependent manner. Cellular uptake studied by CLSM indicated that YMs and LMs were readily taken up by HeLa cells. According to the results of this study, doxorubicin-conjugated Y-shaped PEG-polypeptide2 copolymers showed advantages over linear copolymers, like assembling into smaller nanoparticles, faster drug release in acid, which may correspond to higher cellular uptake and enhanced extracellular-intracellular drug release, indicating their potential in constructing nano-sized drug delivery systems. View Full-Text

Keywords: miktoarm-star copolymer; conjugate; doxorubicin; pH-responsive drug release; drug delivery miktoarm-star copolymer; conjugate; doxorubicin; pH-responsive drug release; drug delivery





Author: Bowen Sui 1, Hui Xu 2,* , Jian Jin 1, Jingxin Gou 2, Jingshuo Liu 1, Xing Tang 2, Yu Zhang 2, Jinghua Xu 3, Hongfeng Zhang 3 and Xiangqun Jin 1,*

Source: http://mdpi.com/



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