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Molecules 2014, 19(8), 11915-11932; doi:10.3390/molecules190811915

Self-Assembled Micelles Composed of Doxorubicin Conjugated Y-Shaped PEG-Poly(glutamic acid)2 Copolymers via Hydrazone Linkers

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.
Received: 11 June 2014 / Revised: 18 July 2014 / Accepted: 21 July 2014 / Published: 11 August 2014
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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-poly(glutamate-hydrazone-doxorubicin)2 and linear copolymers of mPEG-b-poly(glutamate-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-(polypeptide)2 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
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MDPI and ACS Style

Sui, B.; Xu, H.; Jin, J.; Gou, J.; Liu, J.; Tang, X.; Zhang, Y.; Xu, J.; Zhang, H.; Jin, X. Self-Assembled Micelles Composed of Doxorubicin Conjugated Y-Shaped PEG-Poly(glutamic acid)2 Copolymers via Hydrazone Linkers. Molecules 2014, 19, 11915-11932.

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