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

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

International journal of pharmaceutics (2015-03-01)
Wei He, Yaqi Lv, Yaping Zhao, Chaoran Xu, Zhu Jin, Chao Qin, Lifang Yin
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.

MATERIALS
Product Number
Brand
Product Description

USP
Trehalose, United States Pharmacopeia (USP) Reference Standard
Supelco
Trehalose, Pharmaceutical Secondary Standard; Certified Reference Material
Paclitaxel semi-synthetic for peak identification, European Pharmacopoeia (EP) Reference Standard
Sigma-Aldrich
12-Hydroxyoctadecanoic acid, 99%
Sigma-Aldrich
Paclitaxel, from semisynthetic, ≥98%
Sigma-Aldrich
Paclitaxel, from Taxus yannanensis, powder
Sigma-Aldrich
Paclitaxel, from Taxus brevifolia, ≥95% (HPLC), powder
Paclitaxel, European Pharmacopoeia (EP) Reference Standard
Paclitaxel semi-synthetic for system suitability, European Pharmacopoeia (EP) Reference Standard
Paclitaxel natural for peak identification, European Pharmacopoeia (EP) Reference Standard