Effect of Resveratrol Pretreatment on Intestinal Transport and Oral Bioavailability of Carvedilol in Rats by P-gp Inhibition Shahid Mohammed Abdul Aziz1,*, Kumar Y Shravan2, Farooq Syed Umar3, Qureshi Md. Shamim4 1Research Scholar, Department of Pharmacology, Singhania University, Pacheri Bari, Jhun Jhunu, Rajasthan 2Professor, Department of Pharmaceutics, Vagdevi College of Pharmacy, Warangal, Telangana 3Research Scholar, Department of Pharmaceutics, Singhania University, Pacheri Bari, Jhun Jhunu, Rajasthan 4Anwarul Uloom College of Pharmacy, New Mallepally, Hyderabad, Telangana – 500001 *Corresponding Author E-mail: shahiduz_zama@yahoo.co.in
Online published on 30 April, 2020. Abstract The present study aimed to assess the effect of resveratrol on the intestinal transport and oral bioavailability of carvedilol in rats. The intestinal transport was evaluated by in vitro non-everted intestinal sac The present study aimed to assess the effect of resveratrol on the intestinal transport and oral bioavailability of carvedilol in rats. The intestinal transport was evaluated by in vitro non-everted intestinal sac method. The oral pharmacokinetics was evaluated by conducting oral bioavailability study. In both methods the rats were pretreated with resveratrol for 7 days. In intestinal sac method rats were sacrificed by using anesthetic ether. The intestinal segments were isolated and used for the studies. The probe drug (carvedilol) solution was placed in the isolated intestinal sac. Samples were collected at preset time points and replaced with fresh buffer. The drug content in the samples was estimated using high performance liquid chromatography method. Control experiments were also performed. A significant increase in transport of carvedilol in duodenum, jejunum and ileum was seen with resveratrol treated group when compared to control. In oral bioavailability study the pharmacokinetic parameters like area under plasma concentration time curve and peak plasma concentration of carvedilol increased significantly in resveratrol treated group from control group. These results suggest that resveratrol increased the intestinal transport and oral bioavailability due to inhibition of P-gp mediated efflux in the intestine. Further studies are recommended to prove this effect in human beings (p<0.05) difference compared to control, in the transport of carvedilol from the intestinal sacs which were pretreated with resveratrol. It suggests that resveratrol might be acting by inhibiting the transporters and enzymes which are responsible for transport/metabolism of carvedilol. From the results it can be concluded that resveratrol be acting by inhibiting p-glycoprotein as carvedilol is transported by p-glycoprotein. Further studies are recommended to prove their effects in human beings. Top Keywords Carvedilol, P-gp, Resveratrol, Bioavailability, Pharmacokinetics. Top |