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J Microencapsul. 2017 May;34(3):250-261. doi: 10.1080/02652048.2017.1337247. Epub 2017 Jun 15.

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

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a College of Pharmacy, Institute of Pharmaceutical Science and Technology , Hanyang University , Ansan , Gyeonggi , Republic of Korea.
b Faculty of Pharmacy , The University of Lahore , Lahore , Punjab , Pakistan.
c Riphah Institute of Pharmaceutical Sciences , Riphah International University , Islamabad , Pakistan.
d College of Pharmacy , Chungnam National University , Daejeon , Republic of Korea.


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.


Lipid nanoparticles; bioavailability; docetaxel; pharmacokinetics; sustained release

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