Host?guest inclusion complex of albendazole and itaconyl-β-cyclodextrin: Preparation and characterization in solution and solid state

GARCÍA, A.; LAMAS, M. C.; LEONARDI, D.

Rosario

Congreso; RICIFA 2016; 2016

RICIFA

Several alternatives are applicable to enhance the solubility of poorly soluble drugs in order to arrive at the pharmacological target in sufficient amounts, and thereby producing its therapeutic activity. The formulation of inclusion complexes with cyclodextrins or its derivatives is one of the most promising approaches. The aim of this work was to evaluate the suitability of itaconyl-β-cyclodextrin to develop oral dosage forms including albendazole, as poorly soluble model drug. It was selected a substituent presenting acidic groups with the purpose of improving the guest?host affinity. Itaconyl-β-cyclodextrin was synthesized in aqueous media, under mild conditions. The β-cyclodextrin derivative and the inclusion complex were characterized in solution and solid state by phase solubility studies, SEM, XRD, DSC, ESI-MS, FT-IR and NMR spectroscopy. Phase solubility studies indicated that β-cyclodextrin and itaconyl-β-cyclodextrin formed 1:1 inclusion complexes with albendazole, and the stability constants were 68 M−1 and 602 M−1, respectively. Additionally, RMN and ESI-MS analysis, confirmed the inclusion complex formation in solution. Water solubility and dissolution rate of albendazole were significantly increased in the inclusion complex. These studies indicated that inclusion complex with the itaconyl-β-cyclodextrin improved remarkably the physicochemical properties of albendazole, being a suitable excipient to design oral dosage forms.