Penlac
Ciclopirox delivery into the human nail plate.

Hui X, Wester RC, Barbadillo S, Lee C, Patel B, Wortzmman M, Gans EH, Maibach HI.

Department of Dermatology, University of California-San Francisco, 90 Medical Center Way, Surge 110, Box 0989, San Francisco, CA 94143, USA. xhui itsa.ucsf.edu

The human nail penetration of the antifungal ciclopirox was determined for marketed gel containing 0.77% of ciclopirox, an experimental gel containing 2% of ciclopirox, and a marketed lacquer containing 8% of ciclopirox. After 14 days dosing, unabsorbed drug remaining on the surface, drug within the infection-prone area, and the amount that had penetrated through the nail were determined. Ciclopirox delivery into and through the nail was significantly greater from the marketed gel, than from either the experimental gel or the nail lacquer (p < 0.05). In addition, the surface nail contained more unabsorbed drug from the lacquer. Further, the drug penetrating into and through the nail was also greater from the marketed gel, leading to a higher Calculated Efficacy Coefficient for the marketed gel, than from the marketed lacquer or the experimental gel. The formulation plays an important role in the enhancement of ciclopirox permeation into and through the human nail plate, and the concentration of ciclopirox in the formulation was not a factor in determining penetration. Copyright 2004 Wiley-Liss, Inc. and the American Pharmacists Association

Online source: www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=15349963&dopt=Abstract ciclopirox Penlac



Penlac
A randomized comparison of nail surface remanence of three nail lacquers, containing amorolfine 5%, ciclopirox 8% or tioconazole 28%, in healthy volunteers.

Sidou F, Soto P.

Galderma R&D, Sophia Antipolis, France. farzaneh.sidou galderma.com

This randomized, investigator-masked study compared the remanence on the nail surface of commercially available antimycotic nail lacquers containing amorolfine, ciclopirox and tioconazole. The lacquers, to which a coloring agent was added, were applied randomly to the left and right thumbnails and great toenails of 10 healthy volunteers. Volunteers were asked to wash their hands under standardized conditions at 30, 60 and 90 min after product application and to take at least one shower during the study. Photographs were taken immediately after drug application and at 30, 60 and 90 min, i.e., immediately after each hand washing, and then at 8 and 24 h. Photographs of treated toenails were taken at 0, 8 and 24 h. Photographic image analysis allowed automatic calculation of the proportion of nail surface remaining covered by the different nail lacquers over time and after washing. In addition, clinical visual assessment was made to determine the degree of the nail surface covered by the nail lacquers over time. It was demonstrated that at 24 h after product application, remanence of amorolfine nail lacquer on the thumbnails was significantly higher than that of ciclopirox (p < 0.05) and that of tioconazole on the thumb- and toenails at each time point up to 8 h after product application (all p < 0.05). Clinical observation showed that 30 min after application, the tioconazole nail lacquer had still had not completely dried. Amorolfine nail lacquer was shown to be more resistant than ciclopirox and tioconazole nail lacquers to chemical trauma from soaps and to mechanical aggressions from the immediate nail environment.

Online source: www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=15573688&dopt=Abstract ciclopirox Penlac



Penlac
Pharmacoeconomic analysis of sequential treatment pathways in the treatment of onychomycosis.

Frankum LE, Nightengale B, Russo CL, Sarnes M.

Applied Health Outcomes, Palm Harbor, Florida, USA. lfrankum applied-outcomes.com

This study examines the budgetary effect of using ciclopirox, itraconazole (pulse treatment), terbinafine, or itraconazole (continuous treatment) as first-, second-, or third-line therapy in the treatment of toenail onychomycosis by determining which therapeutic sequence is most cost effective. Using a disease treatment pathway model, alternative agents were compared based on cost per clinical response. The results from this sequential treatment analysis demonstrated that ciclopirox followed by itraconazole pulse and then terbinafine provides the lowest-cost approach to the treatment of onychomycosis (dollar 757.89 per clinical response), followed by the sequence of ciclopirox, terbinafine, and itraconazole pulse (dollar 796.13 per clinical response). This study provides a framework for formulary decision makers to evaluate a sequential treatment pathway that resembles actual practice.

Online source: www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=15682633&dopt=Abstract ciclopirox Penlac



Penlac
A multicenter, open-label study to assess the safety and efficacy of ciclopirox topical suspension 0.77% in the treatment of diaper dermatitis due to Candida albicans.

Gallup E, Plott T; Ciclopirox TS Investigators.

Medical Strategies Inc., Mission, KS 66202, USA. bethg nchqa.org

Ciclopirox is a broad-spectrum antifungal, antibacterial, and anti-inflammatory agent. This open-label study investigated the safety and efficacy of ciclopirox topical suspension 0.77% in the treatment of diaper dermatitis due to Candida albicans (C. albicans). Forty-four male and female subjects aged 6 to 29 months were included in the study. Study medication was applied topically to the affected diaper area twice daily for 1 week. Subjects were clinically evaluated at baseline and days 3, 7, and 14 (7 days post-treatment). Safety and efficacy variables included adverse events, mycological culture studies, KOH tests, Severity Scores, and Global Evaluation of Clinical Response. All adverse events were mild to moderate and considered not related to the study medication. Treatment provided statistically significant improvement (P < .05) for both the rate of mycological cure and reduction of Severity Score at each time point compared with baseline. Ciclopirox was safe and effective in the treatment of diaper dermatitis due to C. albicans.

Online source: www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=15696982&dopt=Abstract ciclopirox Penlac



Penlac
In vitro transungual permeation of ciclopirox from a hydroxypropyl chitosan-based, water-soluble nail lacquer.

Monti D, Saccomani L, Chetoni P, Burgalassi S, Saettone MF, Mailland F.

Department of Bioorganic Chemistry and Biopharmaceutics, University of Pisa, Pisa, Italy. montid farm.unipi.it

Commercial antimycotic nail lacquers are commonly based on water-insoluble resins. The present study was aimed at evaluating a novel, experimental nail lacquer (P-3051, Polichem SA, Lugano, Switzerland) based on the water-soluble film-forming agent hydroxypropyl chitosan (HPCH). The in vitro permeation of ciclopirox (CPX) from P-3051 and from a commercial, water-insoluble lacquer based on a vinyl resin (Penlac, Aventis Pharma), was investigated using thin membranes obtained from bovine hooves, an accepted model for human nails. Similar CPX permeation fluxes at steady state through the membranes, but significantly different lag times were observed for P-3051 and Penlac, when these were tested as dry films. The formulations thus appeared to influence only the time required by CPX to saturate the membrane, and not the final drug concentration gradient in the membrane. Permeation experiments performed on the same membranes and on hairless mouse skin with P-3051 and with a similar, HPCH-free vehicle (ERV), both tested in liquid form, disproved the possibility that HPCH might act as a permeation enhancer for CPX in either substrate. The possible reasons for the greater efficiency of the HPCH vehicle in terms of CPX transfer from the vehicle itself to the keratin membrane are discussed. This effect might be tentatively attributed to a particular affinity of HPCH for the membrane, resulting in intimate contact and strong adhesion of the HPCH lacquer to the keratin substrate.

Online source: www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=15704853&dopt=Abstract ciclopirox Penlac