Enhancement of catechin skin permeation via a newly fabricated mPEG-PCL-graft-2-hydroxycellulose membrane

• Published in: Journal of membrane science 2011-04, Vol.371 (1-2), p.134-140
• Main Authors: Chen, Chao-Hsuan, Hsieh, Ming-Fa, Ho, Yi-Nung, Huang, Chun-Ming, Lee, Jui-Sheng, Yang, Chan-Yi, Chang, Yung
• Format: Article
• Language: English
• Subjects: artificial membranes; Bioavailability; Catechin; Cellulose; Chemistry; Colloidal state and disperse state; Exact sciences and technology; gastrointestinal system; General and physical chemistry; green tea; liver; Membranes; oral administration; Penetration enhancer; polymers; rats; solvents; Transdermal delivery
• ISSN: 0376-7388; 1873-3123
• DOI: 10.1016/j.memsci.2011.01.029

► Green tea catechins are known to have medicinal anti-inflammatory and antioxidative functions. ► Orally administrated catechins are metabolized in body, leading to low bioavailability. ► This paper presents in vitro and in vivo permeation of catechins through the skin. ► Catechin-loaded cellulose membrane grafted with PEG-PCL shows increased bioavailability. ► The amphiphilic PEG-PCL can modify the permeation flux of cellulose membrane for catechins. Green tea extracts largely consist of anti-oxidative/anti-inflammatory catechins such as (−)-epigallocatechin gallate. Orally administered catechins are metabolized in the gastrointestinal tract and liver, subsequently incurring low bioavailability. This study attempts to improve the bioavailability of catechin by using mPEG-PCL-graft-2-hydroxycellulose (mPEG-PCL-g-HEC) porous membrane as a penetration matrix for skin delivery of catechins. The green tea-extracted catechin was obtained based on the partition difference in two phases of solvents. In vitro permeation tests using a Franz diffusion cell system indicated that the mPEG-PCL-g-HEC membrane with a loading content of the catechins of 1.5mg/cm2 significantly enhanced the permeation of the catechins up to 0.84mg/mL in the receptor of Franz cell for a period of 48h, whereas the permeated catechins through HEC membrane was only 0.04mg/mL. Moreover, a comparative experiment of the oral and transdermal administrations was conducted to measure the delivered catechins in plasma in Wistar rats. In the oral administration where free catechin was given, the catechin AUC was 34.22±1.51μgh/mL and Cmax was 22.7±1.29μg/mL, respectively. Conversely, in the transdermal administration using catechins-loaded E50C36-g-HEC membranes, the catechin AUC of 356.24±3.24μgh/mL and Cmax of 19.03±0.75μg/mL was obtained. Furthermore, a higher catechin AUC of E50C36-g-HEC membrane than that of E50-C84-g-HEC membrane presented a role of the permeation enhancer to the amphiphilic polymer grafted to the cellulosic material. Therefore, this study showed the potential use of amphiphilic polymer mPEG-PCL in controlling the delivery of catechins via skin.