Enhancement of bioavailability of griseofulvin by its complexation with beta-cyclodextrin.
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.
Dhanaraju
M D
MD
Department of Pharmaceutics, C. L. Baid Metha College of Pharmacy, Madras, India.
Kumaran
K S
KS
Baskaran
T
T
Moorthy
M S
MS
D000818:Animals; D000935:Antifungal Agents / Q000008:administration & dosage* / Q000493:pharmacokinetics* / Q000633:toxicity; D001682:Biological Availability; D002626:Chemistry, Pharmaceutical; D003505:Cyclodextrins / Q000008:administration & dosage* / Q000633:toxicity; D005260:Female; D006118:Griseofulvin / Q000008:administration & dosage* / Q000493:pharmacokinetics* / Q000633:toxicity; D006801:Humans; D066298:In Vitro Techniques; D008297:Male; D051379:Mice; D011817:Rabbits; D012449:Safety; D012995:Solubility; D013053:Spectrophotometry; D017550:Spectroscopy, Fourier Transform Infrared; D047392:beta-Cyclodextrins
D000935:Antifungal Agents; D003505:Cyclodextrins; D047392:beta-Cyclodextrins; D006118:Griseofulvin; C031215:betadex