IMPROVING THE ANTIFUNGAL EFFICACY OF GRISEOFULVIN BY SOY LECITHIN NANOEMULSION

Author: Okpana Emeka Chimezie
Department: Pharmaceutical Microbiology and Biotechnology
Affiliation: Nnamdi Azikiwe University Awka

Griseofulvin, a fungistatic agent with poor aqueous solubility and bioavailability was formulated as a nanoemulsion usinga simple homogenization technique, and Soya bean oil, soya lecithin and distilled water. High concentration of the drug in the lipid was achieved by optimization. The nanoemulsion was then characterized by determining the particle size, electrical conductivity, pH and antifungal activity. In vitro antifungal activity was determined by the agar well diffusion assay against two strains each of Candida albicans, Aspergillusniger, and Trichophytonrubrum. In vivo antifungal activity was determined with only A. niger by establishing systemic mycosis in male white Wister albino rats, and subsequently administering orally 10 mg/kg of the commercial drug (as a suspension) and 0.77 mg/kg (the in vitro bioequivalent dose as the commercial suspension) of the nanoemulsion and then determining the percentage parasitemia by microbial count. Effect of the nanoemulsion on the haematopoietic system was determined by using an auto hematological analyzer and was compared to that of the commercial suspension at the same dose. The effect of the nanoemulsion and commercial suspension on the liver was evaluated by determining the aspartate aminotransferase (AST), alanine aminotransferase (ALT), alkaline phosphatase (ALP) and histopathological changes. Stability study of the nanoemulsion was also performed. The optimized formular had an oil to surfactant ration of 7:3. The drug concentration of the nanoemulsion was 0.48 μg/ml. The characteristics of the nanoemulsion 24 h after formulation included an average drop size of 150.3 ±2.23nm, pH of 6.30 ± 0.00, conductivity of 84.00 ms/cm ± 0.58 and viscosity of 0.89 cP ± 5.05. All these characteristics were not significantly different after 90 days of shelf storage. The in vitro antifungal activity showed that the nanoemulsion wasmore active against all three organisms at a much lower dose (0.48 μg/ml) than the commercial preparation (5 mg/ml). In vivo antifungal activity showed that the nanoemulsion produced a significantly reduced parasitemia (from day 3 of treatment) compared to the commercial suspension. The nanoemulsion improved the hematopoietic system of the micecompared to the commercial suspension; except for the WBC counts which showed no significant difference. The nanoemulsion produced a lesser toxic effect on the liver compared to the commercial suspension. Griseofulvinnanoemulsion is a potential new formulation of griseofulvin with higher activity and lower toxicity than the available commercial suspension.

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