ABSTRACT

Present study was aimed to exploit 32 full factorial design in optimizing goat intestinal permeability of poorly permeable berberine chloride (BBC) on pre-treatment with bioenhancer piperine. For the optimization of concentration of piperine and pre-treatment time, Design-Expert software was used to predict the response % cumulative drug release (% CDR) of BBC across membrane. Effect of piperine was investigated at 3 disparate concentrations (2, 6 and 10 mg) and 3 disparate time of pre-treatment (30, 45 and 60 min). Furthermore, apparent permeability, flux and enhancement ratio were investigated. Additionally, optimized batch was screened for in-vitro anticancer activity on K562, A459 and Hela cancer cell lines. It was noticed that, with decrease in both concentration of piperine and pre-treatment time has positive influence on permeability parameters of BBC. Maximum value of 63.72±1.16 %CDR was obtained at 30 min pre-treatment time with 2 mg piperine over control 8.49±1.45 %CDR. Further, optimized batch showed extremely remarkable enhancement in in-vitro anticancer activity over control. In brief, piperine mediated inhibition of intestinal multidrug efflux pump P-glycoprotein (P-gp) might be solely accountable for permeability improvement of BBC. The limitation of poor intestinal permeability of BBC could be successfully overcome by pre-treatment with piperine. Keywords: Poorly permeable drug, Bioenhancer, Franz diffusion study, ex-vivo permeation data, goat intestinal membrane permeability, response surface analysis, in-vitro anticancer activity
Publication date: 01/10/2022

https://ijbpas.com/pdf/2022/October/MS_IJBPAS_2022_6497.pdf

Download PDF
https://doi.org/10.31032/IJBPAS/2022/11.10.6497