Formulation development and in vitro assessment of smedds for oral delivery of antiviral drugs

Abstract

Aim: The aim of the present study was to develop SMEDSS (liquid and solid) based formulations for poorly water-soluble antiviral drugs EFZ and RIL. newlineMaterials and Methods: Preformulation study along with drug excipients compatibility study was conducted for EFZ and RIL. HPLC method was adopted for the determination of EFZ and RIL. A preliminary study including solubility study and SMEDDS components compatibility study was performed. Various tools of QbD and DoE were employed for the optimization of the design. Liquid SMEDDS was converted into Solid SMEDDS by spray drying and adsorption method respectively for EFZ and RIL. Exhaustive characterization of L-SMEDDS was done by TEM, particle size and zeta potential. Solid SMEDDS were characterized by DSC, XRD, and SEM. In vitro cell permeation study was conducted on Caco-2 cell lines. newline newlineResults and Discussion: Results of drug excipients compatibility study revealed the compatibility of drugs with proposed excipients. The HPLC calibration curves of EFZ and RIL showed perfect linearity with R2 value 0.999. QbD and REM tools have helped to screen significant independent factors. The highest solubility of EFZ and RIL was found in Cremophore (134.45) and in Labrasol (72.63), respectively. DSC and XRD characterization of both Solid SMEDSS revealed the conversion of crystalline form into amorphous form. Results of short term stability study exhibited stable characteristics of SMEDDS. In vitro cell line permeation study proved almost 4-5 times solubility increment of drug. newline newlineConclusion: In a nutshell, it can be concluded that SMEDDS design is a promising approach for solubility enhancement of poorly water-soluble drugs. newline newline newline