Cyclodextrin Based Polymeric Nanobeads

Posted by

Hydroxypropyl β-cyclodextrin (HPβCD) based polymeric nanobeads containing voriconazole (VRC) were fabricated by free radical polymerization using N, N′-methylene bisacrylamide (MBA) as a cross-linker, 2-acrylamide-2-methylpropane sulfonic acid (AMPS) as monomer and ammonium persulfate (APS) as reaction promoter. Optimized formulation (CDN5) had a particle size of 320 nm with a zeta potential of −35.5 mV and 87% EE. Scanning electron microscopy (SEM) depicted porous and non-spherical shaped beads. No evidence of chemical interaction was evident in FT-IR studies, whereas distinctive high-intensity VRC peaks were found superimposed in XRD. A stable polymeric network formation was evident in DSC studies owing to a lower breakdown in VRC loaded HPβCD in comparison to blank HPβCD. In vitro release studies showed 91 and 92% drug release for optimized formulation at pH 1.2 and 6.8, respectively, with first-order kinetics as the best-fit model and non-Fickian diffusion as the release mechanism. No evidence of toxicity was observed upon oral administration of HPβCD loaded VRC polymeric nanobeads to rabbits. Molecular docking indicates the amalgamation of the compounds highlighting the hydrophobic patching mediated by nanogel formulation. It can be concluded that the development of polymeric nanobeads can be a promising tool to enhance the solubility and efficacy of hydrophobic drugs such as VRC besides decreased toxicity and for effective management of fungal infections.

The VRC/CDN5 complex as obtained from molecular modelling. The VRC is presented as balls
and sticks, while AMPS and HPβCD are shown as molecular surfaces.

Farooq, M.; Usman, F.; Naseem, M.; Aati, H.Y.; Ahmad, H.; Manee, S.; Khalil, R.; Khan, K.u.R.; Qureshi, M.I.; Umair, M. Voriconazole Cyclodextrin Based Polymeric Nanobeads for Enhanced Solubility and Activity: In Vitro/In Vivo and Molecular Simulation Approach. Pharmaceutics 2023, 15, 389.

Leave a Reply

This site uses Akismet to reduce spam. Learn how your comment data is processed.