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Molecules 2016, 21(9), 1265; doi:10.3390/molecules21091265

New Oral Formulation and in Vitro Evaluation of Docetaxel-Loaded Nanomicelles

1
Department of Chemical Engineering, Science and Research Branch, Islamic Azad University, Tehran 1477893855, Iran
2
Chemical Injuries Research Center, Baqiyatallah University of Medical Sciences, Tehran 193955487, Iran
3
Nanotechnology Research Center, School of Pharmacy, Mashhad University of Medical Sciences, Mashhad 917751365, Iran
*
Author to whom correspondence should be addressed.
Academic Editor: Didier Astruc
Received: 23 August 2016 / Revised: 17 September 2016 / Accepted: 17 September 2016 / Published: 21 September 2016
(This article belongs to the Collection Nanomedicine)
View Full-Text   |   Download PDF [1622 KB, uploaded 21 September 2016]   |  

Abstract

Intravenous administration of Taxotere® (a commercial form of docetaxel, DTX) leads to many problems such as hypersensitivity, hemolysis, cutaneous allergy, and patient refusal due to its prolonged injection. The oral absorption of DTX is very low due to its hydrophobic nature. The purpose of this study was to prepare and carry out an in vitro evaluation of DTX-loaded nanomicelles for oral administration in order to increase the oral delivery of DTX. Studied formulations were prepared with the two surfactants Tween 20 and Tween 80 and were characterized for their particle size, zeta potential, stability, encapsulation efficiency, stability studies in gastric fluid and intestinal fluid, toxicity studies in C26 colon carcinoma cell line, and cellular uptake. The prepared nanomicelles with particle size of around 14 nm and encapsulation efficiency of 99% were stable in gastric fluid and intestinal fluid for at least 6 h and IC50 decreased significantly after 72 h exposure compared to that of Taxotere®. Nanomicelles increased the water solubility of DTX more than 1500 times (10 mg/mL in nanomicelles compared to 6 µg/mL in water). Results of this study reveal that the new formulation of DTX could be used for the oral delivery of DTX and merits further investigation. View Full-Text
Keywords: nanomicelle; docetaxel; Taxotere®; encapsulation; stability; C-26 cell line; in vivo; in vitro nanomicelle; docetaxel; Taxotere®; encapsulation; stability; C-26 cell line; in vivo; in vitro
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This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited. (CC BY 4.0).

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MDPI and ACS Style

Hekmat, A.; Attar, H.; Seyf Kordi, A.A.; Iman, M.; Jaafari, M.R. New Oral Formulation and in Vitro Evaluation of Docetaxel-Loaded Nanomicelles. Molecules 2016, 21, 1265.

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