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Development of docetaxel nanocrystals surface modified with transferrin for tumor targeting

Authors Choi JS, Park JS

Received 22 September 2016

Accepted for publication 16 November 2016

Published 16 December 2016 Volume 2017:11 Pages 17—26


Checked for plagiarism Yes

Review by Single anonymous peer review

Peer reviewer comments 2

Editor who approved publication: Dr Tuo Deng

Jin-Seok Choi, Jeong-Sook Park

College of Pharmacy, Institute of Drug Research and Development, Chungnam National University, Yuseong-gu, Daejeon, South Korea

The purpose of this study was to develop the surface modification of docetaxel nanocrystals (DTX-NCs) with apo-Transferrin human (Tf) for improving the cellular uptake and cytotoxicity of DTX. DTX-NCs were prepared by a nanoprecipitation method, and the surface modified with Tf by an adsorption method (Tf-DTX-NCs). The morphology and particle size of DTX-NCs and Tf-DTX-NCs were characterized using a field emission scanning electron microscope and zetasizer. An in vitro drug release study was performed in phosphate-buffered saline containing 0.5% (w/v) Tween 80 for 24 hours. Cellular uptake was studied at 0.5, 1, and 2 hours. A cytotoxicity study was performed using the A549 (human lung cancer) cell line after 24-, 48-, and 72-hour treatments. The mean sizes were 295±97 and 398±102 nm for DTX-NCs and Tf-DTX-NCs, respectively. Tf-DTX-NCs and DTX-NCs exhibited rapid drug release, whereas DTX (pure) was slowly released. Tf-DTX-NCs showed higher cellular uptake than DTX-NCs in confocal microscopic and quantitative studies. Moreover, at DTX concentration of 100 µg/mL, Tf-DTX-NCs (82.6%±0.8%) showed higher cytotoxicity than DTX-NCs (77.4%±4.1%) and DTX (pure; 20.1%±4.6%) for 72-hour treatment. In conclusion, Tf-DTX-NCs significantly improved the cellular uptake and cytotoxicity of DTX in the A549 cell line.

Keywords: docetaxel, nanocrystals, surface modification, apo-Transferrin human

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