[Affinity of Luliconazole for Human Nail Derived Keratin].
Med Mycol J
; 58(4): J113-J119, 2017.
Article
em Ja
| MEDLINE
| ID: mdl-29187718
ABSTRACT
Affinity of Luliconazole (LLCZ), an antifungal drug used for topical treatment of onychomycosis in Japan, to nail keratin was demonstrated. Efinaconazole (EFCZ) was used as a reference drug. Drugs at fixed concentrations were added to 4 ml of buffer solution containing 40 mg of nail keratin powder prepared from healthy volunteers or from tinea unguium patients. The mixtures were shaken at 37â, and adsorption and desorption rates of the drug in nail keratin were measured. Theoretical analysis using the Freundlich adsorption isotherm was applied to eliminate effects of testing conditions on the results. Results showed that compared with EFCZ, LLCZ exhibited high adsorption rates and low desorption rates in nail keratins. These results were verified by Freundlich analysis, in which adsorption coefficient (KadsF) and desorption coefficient (KadsF) of LLCZ were 5-7 times and about 2 times higher than EFCZ, respectively. In addition, antifungal activity against Trichophyton rubrum of the desorbed LLCZ samples was determined using disk diffusion assay. In conclusion, LLCZ is considered to possess high affinity to nail keratin. LLCZ, therefore, can be retained in the nail as a reservoir and continuously desorbed at the infection site to exhibit antifungal activity against pathogenic fungi. The pharmacokinetics of LLCZ in the nail is believed to differ from that of EFCZ. As adsorption and desorption rates of the two drugs in nail keratin tended to be different between healthy volunteers and patients, further detailed study is needed.
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Texto completo:
1
Coleções:
01-internacional
Base de dados:
MEDLINE
Assunto principal:
Onicomicose
/
Imidazóis
/
Queratinas
/
Unhas
Limite:
Humans
Idioma:
Ja
Revista:
Med Mycol J
Assunto da revista:
MICROBIOLOGIA
Ano de publicação:
2017
Tipo de documento:
Article