Research Papers:

Novel amphiphilic folic acid-cholesterol-chitosan micelles for paclitaxel delivery

Li-Chun Cheng _, Yan Jiang, Yu Xie, Lu-Lu Qiu, Qing Yang and Hui-Yi Lu

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Oncotarget. 2017; 8:3315-3326. https://doi.org/10.18632/oncotarget.13757

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Li-Chun Cheng1, Yan Jiang1, Yu Xie1, Lu-Lu Qiu1, Qing Yang2, Hui-Yi Lu1

1Department of Pharmacy, The Second Affiliated Hospital of Dalian Medical University, Liaoning, Dalian 116027, China

2Department of Anesthesia, Critical Care and Pain Medicine, Massachusetts General Hospital, Boston, MA 02144, USA

Correspondence to:

Hui-Yi Lu, email: [email protected]

Qing Yang, email: [email protected]

Keywords: paclitaxel, folate acid, cholesterol, chitosan, micelle

Received: May 23, 2016     Accepted: November 21, 2016     Published: December 01, 2016


In order to decrease the toxicity of paclitaxel (PTX) and increase the efficiency, we developed an amphiphilic PTX injection system using a biodegradable and biocompatible polymer synthesized by folic acid, cholesterol, and chitosan (FACC). This FACC-based polymer had a low critical concentration (64.13μg/ml) and could self-assemble in aqueous condition to form nanoscale micelles. The particle sizes of FACC-PTX micelles were 253.2±0.56 nm, the encapsulation efficiency and loading capacity of these FACC-PTX micelles were 65.1±0.23% and 9.1±0.16%, respectively. The cumulative release rate was about 85% at pH 5.0 which was higher than that at pH 7.4 (76%). This pH-dependent release behavior was highly suggesting that PTX release from FACC-PTX micelles might be higher in a weak acidic tumor microenvironment and lower toxic for normal cells. The anti-cancer effectiveness of FACC-PTX micelles was investigated by in vitro cytotoxicity and targeting study. The results revealed that FACC micelles have non-toxic on cells as evidenced by high cell viability found (86% to 100%) in the cells cultured with various concentrations of FACC micelles (1 to 500 μg/ml). Targeting study indicated that the cytotoxic efficacy of FACC-PTX micelles was significantly higher than that with Taxol® in the Hela cells (folate receptor-positive cells). These findings indicated that the anticancer efficiency of PTX can be enhanced by adding some cancer cell positive receptor into drug carrier and the FACC micelle was a potential tumor targeting carrier for PXT delivery.

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