Enhancement of bioavailability of griseofulvin by its complexation with beta-cyclodextrin

• Published in: Drug development and industrial pharmacy Vol. 24; no. 6; p. 583
• Main Authors: Dhanaraju, M D, Kumaran, K S, Baskaran, T, Moorthy, M S
• Format: Journal Article
• Language: English
• Published: England 01.01.1998
• Subjects: Animals; Antifungal Agents - administration & dosage; Antifungal Agents - pharmacokinetics; Antifungal Agents - toxicity; beta-Cyclodextrins; Biological Availability; Chemistry, Pharmaceutical; Cyclodextrins - administration & dosage; Cyclodextrins - toxicity; Female; Griseofulvin - administration & dosage; Griseofulvin - pharmacokinetics; Griseofulvin - toxicity; Humans; In Vitro Techniques; Male; Mice; Rabbits; Safety; Solubility; Spectrophotometry; Spectroscopy, Fourier Transform Infrared
• ISSN: 0363-9045
• DOI: 10.3109/03639049809085663

Griseofulvin is a poorly soluble antifungal antibiotic drug, the solubility of which can be enhanced by complexation with beta-cyclodextrin. The inclusion complex was prepared by coprecipitation method in various molar ratios of 1:1, 2:1, 3:1, and 1:2 of the drug and beta-cyclodextrin, respectively. The inclusion complex was characterized and evaluated by UV-VIS spectral studies and FTIR. The in vitro drug release studies indicated that the 1:2 molar ratio complex form of the drug significantly increased the dissolution rate when compared to the free form. The acute toxicity studies clearly indicated that the beta-cyclodextrin complex was nontoxic and the safety range was close to other Griseofulvin formulations. The in vivo study of the beta-cyclodextrin was carried out in both animals and human beings by administering in four different rabbits and volunteers, respectively. Pellets made with Griseofulvin-beta-cyclodextrin complex also showed a significant increase in the dissolution of the drug, revealing that beta-cyclodextrin plays an important role in the solubilization of Griseofulvin.