Super absorbent chitosan-based hydrogel sponges as carriers for caspofungin antifungal drug

Abstract

Novel chitosan copolymers (CS-g-SBMA) grafted with [2-(methacryloyloxy)ethyl]dimethyl-(3-sulfopropyl)ammonium hydroxide (SBMA) in various molar ratio 1.5:1, 5:1, 11.5:1 and 20:1, were synthesized in the present study. SBMA was selected as zwitterion molecule showing promising antibacterial properties. Grafted chitosan derivatives were fully characterized for their successful synthesis by NMR and FT-IR, for their crystallinity by XRD showing reduced crystallinity compared to CS alone. Furthermore, swelling studies were conducted with the grafted derivatives showing extensive swelling capacity (maximum degree of swelling up to 1800%) and water absorption was studied with differential scanning calorimetry and equilibrium water adsorption/desorption isotherms were analyzed. Caspofungin, a novel antifungal drug, was used to prepare a double-acting system, with both antibacterial and antifungal properties, proper for topical use. Drug loaded hydrogels were prepared with 10, 20 and 30 wt% drug content and the loaded hydrogels were fully characterized while antimicrobial studies showed enhanced properties. Caspofungin in vitro release showed an initial burst effect followed by a diffusion process while data analysis verified the initial burst release followed by a quasi Fickian diffusion-driven sustained release. Enhance antimicrobial properties was also observed in caspofungin-loaded hydrogels showing the successful fulfill of our scope; an amphiphilic system having great potential for the development of patches with inherent antimicrobial properties and prolonged antifungal properties.

Keywords: Antibacterial properties; Caspofungin acetate; Chitosan derivatives; Drug release; Hydrogels; Zwitterionic monomer.