DEVELOPMENT AND EVALUATION OF SBA-15 MESOPOROUS SILICA NANOPARTICLES FOR BIOAVAILABILITY ENHANCEMENT OF RITONAVIR

Abstract

Ritonavir (RTV) loaded SBA-15 mesoporous nanocarriers were prepared for improved drug dissolution and bioavailability of this HIV protease inhibitor drug categorized as BCS-class-II; indicate low solubility and high permeability. The SBA-15NPs and RTV loaded SBA-15NPs were characterized by different analytical techniques like UV spectrophotometry, differential scanning calorimetry, thermogravimetric analysis, FT-IR, N2- adsorption-desorption technique, scanning electron microscopy (SEM), transmission electron microscopy (TEM) and powder-XRD. Thermogravimetric analysis shows adsorption of ritonavir in SBA-15NPs was about 53%. Differential scanning calorimetry (DSC) and X-ray powder diffraction pattern confirm that, after RTV loading, no crystalline drug was present outside the carrier and structural arrangement of SBA-15NPs carrier was as it is. The N2 adsorption-desorption technique was used to study the specific surface area, pore size and pore volume of plain SBA-15NPs and the RTV loaded SBA-15NPs. In drug loaded SBA-15NPs surface area and pore volume was decreased compared to plain SBA-15NPs indicating the RTV was entrapped inside the mesopores. The RTV loaded SBA-15NPs shows remarkable improvement in dissolution profile of RTV in comparison to the pure drug. In the pharmacokinetic study, the maximum peak plasma concentrations and AUC0-1 value of R-SBA-15NPs were found 2.32-fold and 1.75-fold higher respectively as compared to pure RTV. The results showed that SBA-15NPs enhance dissolution rate and improvement in bioavailability in comparison to the pure RTV.