Docetaxel-loaded multilayer nanoparticles with nanodroplets for cancer therapy

Abstract

A mixture of docetaxel (DTX) and Solutol^® HS 15 (Solutol) transiently formed nanodroplets when it was suspended in an aqueous medium. However, nanodroplets that comprised DTX and Solutol showed a rapid precipitation of DTX because of their unstable characteristics in the aqueous medium. The incorporation of nanodroplets that comprised DTX and Solutol through vesicle fusion and subsequent stabilization was designed to prepare multilayer nanoparticles (NPs) with a DTX-loaded Solutol nanodroplet (as template NPs) core for an efficient delivery of DTX as a chemotherapeutic drug. As a result, the DTX-loaded Solutol nanodroplets (~11.7 nm) were observed to have an increased average diameter (from 11.7 nm to 156.1 nm) and a good stability of the hydrated NPs without precipitation of DTX by vesicle fusion and multilayered structure, respectively. Also, a long circulation of the multilayer NPs was observed, and this was due to the presence of Pluronic F-68 on the surface of the multilayer NPs. This led to an improved antitumor efficacy based on the enhanced permeation and retention effect. Therefore, this study indicated that the multilayer NPs have a considerable potential as a drug delivery system with an enhanced therapeutic efficacy by blood circulation and with low side effects.

Keywords:

• multilayer nanoparticles
• Solutol
• Pluronic F-68
• docetaxel
• cancer therapy

Acknowledgments

This work was supported by the National Research Foundation of Korea grants funded by the Korean government (20110027932 and 2013063969), R&D program funded by the Ministry of Knowledge Economy (A004600537), and Cancer Control, Ministry of Health and Welfare (1420390).

Disclosure

The authors report no conflicts of interest in this work.