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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

Paclitaxel semi-synthetic for peak identification, European Pharmacopoeia (EP) Reference Standard
Pricing and availability is not currently available.
Sigma-Aldrich
12-Hydroxyoctadecanoic acid, 99%
Pricing and availability is not currently available.
Supelco
Trehalose, Pharmaceutical Secondary Standard; Certified Reference Material
Pricing and availability is not currently available.
USP
Trehalose, United States Pharmacopeia (USP) Reference Standard
Pricing and availability is not currently available.
Sigma-Aldrich
Paclitaxel, from Taxus brevifolia, ≥95% (HPLC), powder
Pricing and availability is not currently available.
Sigma-Aldrich
Paclitaxel, from semisynthetic, ≥98%
Pricing and availability is not currently available.
Sigma-Aldrich
Paclitaxel, from Taxus yannanensis, powder
Pricing and availability is not currently available.
Paclitaxel semi-synthetic for system suitability, European Pharmacopoeia (EP) Reference Standard
Pricing and availability is not currently available.
Paclitaxel, European Pharmacopoeia (EP) Reference Standard
Pricing and availability is not currently available.
Paclitaxel natural for peak identification, European Pharmacopoeia (EP) Reference Standard
Pricing and availability is not currently available.