Cholesterol Derivative-Based Liposomes for Gemcitabine Delivery: Preparation, In Vitro, and In Vivo Characterization.

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Cholesterol Derivative-Based Liposomes for Gemcitabine Delivery: Preparation, In Vitro, and In Vivo Characterization.

Drug Dev Ind Pharm. 2017 Aug 01;:1-34

Authors: Li T, Chen L, Deng Y, Liu X, Zhao X, Cui Y, Shi J, Feng R, Song Y

Abstract
As an anti-tumor drug, gemcitabine (Gem) is commonly used for the treatment of non-small cell lung cancer and pancreatic cancer. However, there are several clinical drawbacks to using Gem, including its extremely short plasma half-life and side effects. To prolong its half-life and reduce its side effects, we synthesized a derivative of Gem using cholesterol (Chol). This derivative, called gemcitabine-cholesterol (Gem-Chol) was entrapped into liposomes by a thin-film dispersion method. The particle size of the Gem-Chol liposomes was 112.57 ± 1.25 nm, encapsulation efficiency was above 99%, and drug loading efficiency was about 50%. In vitro studies revealed that the Gem-Chol liposomes showed delayed drug release and long-term stability at 4°C for up to two months. In vivo studies also showed the superiority of the Gem-Chol liposomes, and compared with free Gem, the Gem-Chol liposomes had longer circulation time. Moreover, an anti-tumor study in H22 and S180 tumor models showed that liposomal entrapment of Gem-Chol improved the anti-tumor effect of Gem. This study reports a potential formulation of Gem for clinical application.

PMID: 28760000 [PubMed - as supplied by publisher]

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