Preparation and evaluation of naringin-loaded polycaprolactone microspheres based oral suspension using Box-Behnken design

Abstract

The objective of the current investigation was to study the outcome of the concentration of polycaprolactone (PCL), the concentration of polyvinyl alcohol (PVA) and the concentration of hydroxypropyl methylcellulose (HPMC) on the average particle size of microspheres and the drug entrapment efficiency of naringin-loaded polycaprolactone microspheres based oral suspension. Naringin-loaded polycaprolactone microspheres based oral suspension were prepared by solvent evaporation method. Further, in this work optimization of the formulation was done using a three factors, three levels Box-Behnken design (BBD). Drug-loaded microsphere suspension was prepared by employing solvent evaporation technique. Fourier transform infrared spectroscopy (FT-IR) and differential scanning calorimetry (DSC) analysis was carried out to determine any incompatibility between the naringin and other components used in the formulations. Polymer alone (PVA concentration) or interaction effects of polymers (PCL-HPMC, PCL-PVA, HPMC-PVA, and PCL in higher order) have a substantial influence on particle size of microspheres. Amount of PVA and HPMC have a significant effect on entrapment efficiency of microspheres. The optimal conditions of PCL concertation were 7.7% w/v; HPMC concentration was 3.2% w/v and PVA concentration was 0.081% w/v. The optimized suspension showed particle size of 24μm with drug entrapment efficiency 96%. As a result, due to uniform distribution of microspheres, drug entrapment efficiency was achieved in optimized suspension.