Docetaxel-loaded mixed micelles composed of Solutol HS15 and Pluronic F127 or folate-conjugated F127: preparation, optimization and in vitro comparative characterization

doi:10.5246/jcps.2015.02.011

Abstract

Abstract:

In this study, two kinds of docetaxel (DTX)-loaded mixed micelles, composed of Solutol HS15 (HS15)/Pluronic F127 (F127) or folate-conjugated F127, (SF-DTX and FSF-DTX), were prepared by the thin-film hydration method and evaluated in vitro. Both SF-DTX and FSF-DTX were spherical with diameter close to 23 nm. They had high encapsulating efficiency (99.05% and 90.28% for SF-DTX and FSF-DTX, respectively) and sustained-release property. SF and FSF were able to enhance the cellular accumulation of DTX in KBv cells and reduce ATP content in A-549 cells. They also were able to reverse multidrug resistance (MDR). In vitro cytotoxicity and cellular accumulation of DTX suggested an active targeting of FSF-DTX. It could be concluded from the results that the novel F127/HS15 system could serve as a potential nanocarrier with the ability of overcoming MDR, and folate-conjugated F127/HS15 might achieve active targeting at the same time.

Key words: Solutol HS 15, Pluronic F127, Mixed micelle, Folate-conjugation, Multidrug resistance

CLC Number:

R943

Supporting:

Wenting Wu, Zhiyu Guan. Docetaxel-loaded mixed micelles composed of Solutol HS15 and Pluronic F127 or folate-conjugated F127: preparation, optimization and in vitro comparative characterization[J]. Journal of Chinese Pharmaceutical Sciences, 2015, 24(2): 95-103.

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