Čes. slov. farm. 2010, 59(2):79-86

Identification and susceptibility evaluation of Candida yeasts due to the optimization of ciclopiroxolamine release from mucoadhesive oral tablets

E. Mašková¹, J. Mašek^1,2, J. Gajdziok^1,*, M. Rabišková¹

¹ Veterinární a farmaceutická univerzita Brno, Farmaceutická fakulta, Ústav technologie léků

² Veterinární a farmaceutická univerzita Brno, Výzkumný ústav veterinárního lékařství, Oddělení farmakologie a toxikologie

Oral candidosis represents a difficult and often recidivating complication in immunodeficient patients. Oral mucoadhesive tablets with prolonged release of a locally acting antifungal drug, e.g. ciclopiroxolamine, could contribute to their pharmacotherapy. For efficient therapy, the drug concentration present in oral cavity has to be determined, i.e. the drug content in the dosage form and its release have to be formed. The Theoretical Part of this paper aims to describe the basic characteristics of Candida yeasts and their induction of oral candidosis, to the possibilities of using standardized methods for detecting and determining their susceptibility to antifungal agents. The Experimental Part is focused on the establishment, identification and quantification of Candida species represented in 536 patients by cultivation on chromogenic agar. The microdilution and disc diffusion methods have been used for assessing the susceptibility of isolated and reference strains of yeasts to the antifungal drug - ciclopiroxolamine. The obtained results showed that 65.96% of candidosis are caused by Candida albicans, however the other tested species of Candida involve the disease only in minor part (C. tropicalis 12.76%, C. glabrata 10.64%, C. parapsilosis 10.64%). The microdilution method established the minimum inhibitory concentration for the reference strains of Candida to 2 μg/ml of ciclopiroxolamine for Candida glabrata, 1 μg/ml for Candida albicans and Candida tropicalis, and 0.5 μg/ml for Candida parapsilosis. Theoretical ciclopiroxolamine content in a tablet providing exceeding MIC for the tested species of Candida for 8-10 hours should lie, when considering all influencing factors, in the range of 25-50 mg with a release rate of 0.24 mg per hour at the minimum.

Keywords: oral candidosis; ciclopiroxolamine; microbiological establishment; pathogen susceptibility evaluation; oral mucoadhesive tablets

Received: March 22, 2009; Accepted: March 30, 2010; Published: February 1, 2010  Show citation