New Oral Delivery System to Improve Absorption of Berberine: Likely Interaction of Cationized Chitosan with PG-P Pump.

Abstract

Berberine Chloride (BC) is an isoquinolinic alkaloid that is extracted from plants of generis Berberis. During the last decade, researchers and clinicians have paid increasing attention to BC, because of its impressive hypoglycemic and blood lipids lowering properties. Several clinical studies gave proof of evidence regarding BC efficacy in humans and pharmacological mechanisms of action, related to the previously mentioned activities, have been proposed and substantially confirmed. On the other side, BC shows a very poor oral bioavailability mainly because of the interaction with P-Glycoprotein (Pg-P) pump, which extrudes BC from inside to outside of the enteric cell. This paper describes a novel oral delivery system containing a Chitosan-N-AcetylCystein salt capable to interact with Pg-P, partially inhibiting BC extruding process. Preliminary data confirming the aforementioned postulated mechanism on Caco-2 in vitro model have been herewith reported and discussed.