Antifungal activity, experimental infections and nail permeation of an innovative ciclopirox nail lacquer based on a water-soluble biopolymer.
P-3051 is an innovative 8% ciclopirox nail lacquer, based on hydroxypropyl chitosan (HPCH) as a film-forming agent. The authors' aim was to investigate P-3051's in vitro antifungal activity, as well as its in vitro and in vivo nail permeation. The dilution susceptibility tests performed for Trichophyton rubrum (T. rubrum) and Candida parapsilosis (C. parapsilosis) showed that the minimum inhibitory concentrations (MICs) of P-3051, as percent of ciclopirox, was for both fungi < or = 0.0015% (equivalent to a concentration of 15.6 mg/ ml). In the biological assay of in vitro nail permeation and fungal inhibition, the authors observed that P-3051 permeated well through bovine hoof membranes and produced dose-dependent inhibitory effects on dermatophyte, yeast and mold strains. Moreover, the inhibition effects were higher than those obtained by equal amounts of the ciclopirox reference nail lacquer. P-3051 and the reference showed the same protective activity in experimental infections with strains of dermatophytes isolated from clinical samples. The amount of ciclopirox remained in cut fingernails washed six hours after in vivo application of P-3051 ranged between 18 and 35% of the applied dose. After in vitro application to cut human nails, 40-50% of the applied ciclopirox penetrated during the first six hours, independent of nails being infected or uninfected, intact or filed. In both experiments, the concentration of ciclopirox is largely higher (three to four orders of magnitude) than the MICs for nail pathogens.
Togni
Giuseppe
G
Microbiology Laboratory, IPAS Institute, Ligornetto, Switzerland.
Mailland
Federico
F
D000328:Adult; D000818:Animals; D000935:Antifungal Agents / Q000008:administration & dosage / Q000493:pharmacokinetics / Q000494:pharmacology*; D002175:Candida / Q000187:drug effects*; D002417:Cattle; D000077768:Ciclopirox; D004305:Dose-Response Relationship, Drug; D005260:Female; D006724:Hoof and Claw; D006801:Humans; D008297:Male; D008826:Microbial Sensitivity Tests; D009262:Nails / Q000378:metabolism; D010539:Permeability; D011728:Pyridones / Q000008:administration & dosage / Q000493:pharmacokinetics / Q000494:pharmacology*; D012995:Solubility; D013997:Time Factors; D014249:Trichophyton / Q000187:drug effects*
D000935:Antifungal Agents; D011728:Pyridones; D000077768:Ciclopirox