alexa Block Copolymer Based Composition of Epigallocatechin-3-gallate with Improved Oral Bioavailability as a Way to Increase its Therapeutic Activity | OMICS International | Abstract
ISSN: 2155-983X

Journal of Nanomedicine & Biotherapeutic Discovery
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Research Article

Block Copolymer Based Composition of Epigallocatechin-3-gallate with Improved Oral Bioavailability as a Way to Increase its Therapeutic Activity

Evgueni Klinski1, Alexandre Semov1, Xu Yan1, Valery Alakhov1*, Ekaterina Muyzhnek2 and Vsevolod Kiselev3

1Supratek Pharma Inc. Montreal, Quebec, Canada

2MiraxBioPharma, Moscow, Russia

3National Research Centre, “Kurchatov Institute”, Moscow, Russia

*Corresponding Author:
Valery Alakhov
Supratek Pharma Inc
Montreal, Quebec, Canada
Tel: 1-514-422-9191
Fax: 1-514-422-9410
E-mail: [email protected]

Received date: July 23, 2013; Accepted date: September 10, 2013; Published date: September 13, 2013

Citation: Klinski E, Semov A, Yan X, Alakhov V, Muyzhnek E, et al. (2013) Block Copolymer Based Composition of Epigallocatechin-3-gallate with Improved Oral Bioavailability as a Way to Increase its Therapeutic Activity. J Nanomedine Biotherapeutic Discov 3:117. doi: 10.4172/2155-983X.1000117

Copyright: © 2013 Klinski E, et al. This is an open-access article distributed under the terms of the Creative Commons Attribution License, which permits unrestricted use, distribution, and reproduction in any medium, provided the original author and source are credited.

Abstract

At the present, a high potential of epigallocatechin-3-gallate (EGCG) as a new preventive and therapeutic agent in oncology and several other indications is well established. EGCG exerts its antitumor activity through induction of cell cycle arrest and apoptosis, inhibition of tumor angiogenesis, migration, and metastasisdue to its ability to interact with multiple targets in cancer cell. Unfortunately, very low oral bioavailability of EGCG prevents its efficient development as novel medicine. In this work, we have developed a polymer based nano-formulation of EGCG that significantly improved its oral bioavailability by increasing systemic exposure of the compound by about8-fold. This formulation comprises a well-known inactive ingredient non-ionic blockcopolymer Pluronic F127 that has recently been successfully used to increase bioavailability of another promising phytonutrient, 3,3`-diindolylmethane. The pharmacokinetic parameters established in the present study revealed that AUC and Cmax of the new formulation dosed at 500 mg/kg were 578.5 ± 73.8 μg∙h/mL and 49.3 ± 2.9 μg/mL, while in the case of control EGCG administered in the equivalent dose AUC and Cmax were 72.9 ± 14.7 μg∙h/mL, and 10.7 ± 1.1 μg/mL.

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