Muhammad Ijaz
University of Innsbruck, Austria
Title: Characterization of inclusion complex of Acyclovir with thiolated β-Cyclodextrin as mucoadhesive vaginal drug delivery system
Biography
Biography: Muhammad Ijaz
Abstract
The objective of the present study was to synthesize and characterize Cysteamine conjugated β-Cyclodextrin (β-CD-Cys) as a novel muco-adhesive polymeric excipient for vaginal drug delivery. Increasing concentrations of cysteamine (0.25%, 0.5% and 0.75%) were covalently attached to oxidized β-CD via reductive amination. Quantification of immobilized thiol groups through Ellmans test revealed 851.84±107 µmol/g, 1040.44±132 µmol/g and 1563.72±171 µmol/g of free thiol groups attached to the polymer backbone, respectively. Viability studies of thiolated derivatives of β-CD at concentrations of 0.5% (m/v) showed no toxic effects on Caco-2 cells within 72 hours. Solubility of thiolated β-CD was furthermore 3.5-fold improved in comparison to unmodified β-CD. Thiolated derivatives of β-CD (β-CD-Cys851, β-CD-Cys1040 and β-CD-Cys1563) showed 3, 12.47 and 32.13-fold improved muco-adhesive properties on porcine intestinal mucosa and 5.84, 15.95 and 17.14-fold improved muco-adhesive properties on porcine vaginal mucosa, respectively. Inclusion complexes of antiviral drug acyclovir with thiolated β-CD resulted in increased drug solubility. According to these results, thiolated β-CD might be a promising novel tool for vaginal delivery of poorly water soluble therapeutic agents, such as acyclovir.
