Block Copolymer Based Composition of Epigallocatechin-3-gallate with Improved Oral Bioavailability as a Way to Increase its Therapeutic ActivityEvgueni Klinski1, Alexandre Semov1, Xu Yan1, Valery Alakhov1*, Ekaterina Muyzhnek2 and Vsevolod Kiselev3
- *Corresponding Author:
- Valery Alakhov
Supratek Pharma Inc
Montreal, Quebec, Canada
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.
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 μgÃ¢ÂÂh/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 μgÃ¢ÂÂh/mL, and 10.7 ± 1.1 μg/mL.