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Research Article

Sustained release docetaxel-incorporated lipid nanoparticles with improved pharmacokinetics for oral and parenteral administration

, , , , , , , , , & show all
Pages 250-261 | Received 21 Dec 2016, Accepted 29 May 2017, Published online: 15 Jun 2017
 

Abstract

The aim of this study was to develop docetaxel-incorporated lipid nanoparticles (DTX-NPs) to improve the pharmacokinetic behaviour of docetaxel (DTX) after oral and parenteral administration via sustained release. DTX-NPs were prepared by nanotemplate engineering technique with palmityl alcohol as a solid lipid and Tween-40/Span-40/Myrj S40 as a surfactants mixture. Spherical DTX-NPs below 100 nm were successfully prepared with a narrow particle size distribution, 96% of incorporation efficiency and 686 times increase in DTX solubility. DTX-NPs showed a sustained release over 24 h in phosphate-buffered saline and simulated gastric and intestinal fluids, while DTX-micelles released DTX completely within 12 h. The half-maximal inhibitory concentration (IC50) of DTX-NPs against human breast cancer MCF-7 cells was 1.9 times lower than that of DTX-micelles and DTX solution. DTX-NPs demonstrated 3.7- and 2.8-fold increase in the area under the plasma concentration–time curve compared with DTX-micelles after oral and parenteral administration, respectively.

Acknowledgements

This work was supported by the research fund of Hanyang University (HY-2012-N).

Disclosure statement

No potential conflict of interest was reported by the authors.

Additional information

Funding

This work was supported by the research fund of Hanyang University (HY-2012-N).

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