ENHANCEMENT OF SOLUBILITY AND BIOAVAILABILITY OF BCS CLASS-II AMBRISENTAN: IN VITRO, IN VIVO AND EX VIVO ANALYSIS

Authors

  • RAHUL RADKE Faculty of Pharmacy, Oriental University, Indore, M.P. India
  • NEETESH K. JAIN Faculty of Pharmacy, Oriental University, Indore, M.P. India

DOI:

https://doi.org/10.22159/ijap.2022v14i1.43347

Keywords:

Ambrisentan, Gelucire 50/13, Bioavailability, Solid dispersion, Kneading technique

Abstract

Objective: The aim of this investigation was to enhance the solubility and bioavailability of the BCS class II poorly water soluble drug ambrisentan by solid dispersion (SD) techniques using Gelucire 50/13 as a hydrophilic carrier.

Methods: Solid dispersion of ambrisentan was prepared by kneading method using different dug: carrier ratios. Prepared SD was characterized for solubility,  drug content, percentage yield, in vitro dissolution, ex vivo permeation and bioavailability. Solid state characterization was performed by differential scanning calorimetry (DSC), X-ray diffraction (XRD) and scanning electron microscopy (SEM).

Results: All the SDs formulation showed increase in drug solubility and dissolution, when compared with its pure form. Aqueous solubility of drug was found to be increased 8.23 fold in SD. DSC study showed that endothermic peak of drug was disappeared in spectra of SD, confirming its amorphous conversion, XRD study revealed the reduction to almost absence of specific high intensity peaks of drug which confirmed the reduction of crysatallinity of ambrisentan in SD. SEM of optimized SD formulation demonstrates the complete encapsulation and solubilization drug. In vitro dissolution study showed that optimized SD formulation (ASD4) gives the faster drug release of 101.5% in 60 min, as compare to its pure form and other SD formulations.

Conclusion: Solid dispersion  ASD4 prepared with 1:4 drug to carrier ratio showed highest drug solubility and  in vitro dissolution. The ex vivo and in vivo studies performed on optimized formulation ASD4 showed enhancement  in drug permeability and bioavailability in Gelucire 50/13 based SD formulation.

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Published

22-11-2021

How to Cite

RADKE, R., & K. JAIN, N. (2021). ENHANCEMENT OF SOLUBILITY AND BIOAVAILABILITY OF BCS CLASS-II AMBRISENTAN: IN VITRO, IN VIVO AND EX VIVO ANALYSIS. International Journal of Applied Pharmaceutics, 14(1). https://doi.org/10.22159/ijap.2022v14i1.43347

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