International Journal of Pharmaceutics 2015-04-30

Core-shell structured gel-nanocarriers for sustained drug release and enhanced antitumor effect.

Wei He, Yaqi Lv, Yaping Zhao, Chaoran Xu, Zhu Jin, Chao Qin, Lifang Yin

Index: Int. J. Pharm. 484(1-2) , 163-71, (2015)

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Abstract

The present paper attempted to develop temperature-sensitive and core-shell structured gel-nanocarriers (gel-NCs) for paclitaxel (PTX) with 12-hydroxystearic acid (12-HSA) as an organic gelator, which aims at sustaining drug release over time and thus improves the therapeutic effect. The gel-NCs were prepared by a mechanical mixing and high-pressure homogenization method. The gelation transition temperature (Tgel) of the organic phase contained in the cores of the gel-NCs was optimized by a stirring method. The gel-NCs were characterized in terms of the particle size, morphology and in vitro drug release. The in vivo studies, including the antitumor effects on H22 tumor-bearing mice, biocompatibility and toxicity in mice, were performed. Gel-NCs with approximately 170 nm were prepared successfully, and the gelation of the liquid cores at 37°C was achieved, while the amount of gelator was 3.75% (w/w). Due to the gelation of the cores, sustained drug release over time was obtained. Moreover, the PTX-loaded gel-NCs suppressed tumor growth more efficiently than the conventional nanocarriers with better in vivo biocompatibility and no toxicity to other healthy organs. In conclusion, the 12-HSA organogel-based NCs appear to be promising systems for the sustained release of active compounds for a long time and thus improve the therapeutic outcome.Copyright © 2015 Elsevier B.V. All rights reserved.