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Permeation of ciclopirox across porcine hoof membrane: effect of pressure sensitive adhesives and vehicles.

Myoung Y, Choi HK.

College of Pharmacy, Chosun University, 375 Seosuk-dong, Dong-gu, Gwangju 501-759, South Korea.

The purpose of this study was to investigate the effects of various pressure sensitive adhesives (PSA) on the penetration of ciclopirox across porcine hoof membrane. In addition, the influence of various vehicles on the permeation of ciclopirox from a PSA matrix across porcine hoof membrane was evaluated using a plastic penetration chamber containing poloxamer gel at 32 degrees C. Ciclopirox in poloxamer gel was extracted, derivatized and analyzed by HPLC. Ciclopirox showed highest permeability from an acrylic adhesive with a hydroxyl functional group, and this was followed by styrene-isoprene-styrene, styrene-butadiene-styrene, silicone and polyisobutylene adhesives in order. In addition, N-methyl-2-pyrrolidone (NMP), polypropylene glycol 400 (PPG 400), dimethylsulfoxide (DMSO), Labrasol, mercaptoethanol and Transcutol showed excellent permeation enhancing effects in a styrene-isoprene-styrene adhesive. A porcine hoof membrane treated with NMP changed from the non-helical phase to the helical phase, and another treated with DMSO showed a S=O peak shift to lower wavelength.

Online source: www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=14592697&dopt=Abstract ciclopirox Penlac



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Effects of subinhibitory concentrations of ciclopirox on the adherence of Candida albicans to human buccal and vaginal epithelial cells.

Braga PC, Piatti G, Conti E, Vignali F.

Center of Respiratory Pharmacology, School of Medicine, University of Milan, Italy.

At present, only a limited number of studies of the effects of sub-inhibitory antifungal agents on the adherence of Candida to epithelial (buccal and vaginal) host cells are available. The adherence of Candida albicans to the epithelial cell surface is accepted as an important first step in persistent colonization and in the following symptomatic or asymptomatic infection of mucosal surface. Ciclopirox (ciclopiroxolamine, CAS 29342-05-0) is a substituted pyridone antimycotic drug, unrelated to the imidazole derivatives and its topical application ensures maximum local bioavailability. The present study was done to investigate the effects of sub-inhibitory concentrations of ciclopirox on the adherence of Candida albicans to human buccal and vaginal epithelial cells. The findings on the adherence of different strains of Candida indicate that the drug caused a significant reduction in the mean number of Candida adhering to both buccal and vaginal cells. This reduction was maximal at concentration of 1/2 MIC and still significant at 1/4, 1/8, 1/16 MIC, but with progressive return to mean control values at 1/32 MIC. Ciclopirox acts on fungi by inhibiting the intracellular uptake of essential substrates and ions and this probably acts on the Candida ability to express its adherence mechanisms.

Online source: www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=1492854&dopt=Abstract ciclopirox Penlac



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Managing simple chronic paronychia and onycholysis with ciclopirox 0.77% and an irritant-avoidance regimen.

Daniel CR 3rd, Daniel MP, Daniel J, Sullivan S, Bell FE.

University of Mississippi Medical Center, Jackson, USA. crd322 aol.com

Dermatologists and other physicians frequently encounter simple chronic paronychia and onycholysis. In addition to strict avoidance of contact irritants, a broad-spectrum topical antifungal agent has been recommended. We conducted an examination of treatment with this type of agent and an assessment of the efficacy of ciclopirox 0.77% topical suspension in combination with a strict irritant-avoidance regimen. Early results of a pilot study (N = 44) using ciclopirox 0.77% topical suspension in patients diagnosed with simple chronic paronychia and/or onycholysis show excellent therapeutic outcomes of a combined regimen of a broad-spectrum topical antifungal agent such as ciclopirox and contact-irritant avoidance in this patient population.

Online source: www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=14964637&dopt=Abstract ciclopirox Penlac



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HPLC method for pharmacokinetic studies on ciclopirox olamine in rabbits after intravenous and intravaginal administrations.

Coppi G, Silingardi S.

Centro Ricerche, Poli Industria Chimica, Rozzano, Italy.

This paper reports a HPLC method to detect unchanged and glucuronide derivatives of ciclopirox olamine (a substituted 2-pyridone antimycotic) and gives pharmacokinetics in rabbits after i.v. and intravaginal administration. The HPLC method utilizes a RP 18 reverse phase column, a mobile phase of water and acetonitrile (60/40), a flux of 1 ml/min and wavelength of 304 nm. For the determination of free ciclopirox the plasma drug is methylated with dimethyl sulphate, extracted with n-exane, purified on Adsorbex CN and injected into the column. For the determination of total (free and glucuronide derivatives) ciclopirox the plasma is previously hydrolized with beta-glucuronidase before the application of the above procedure. In rabbits the drug is administered at 15 mg/kg for both routes; the t1/2 elim is 2.1 hours, the total clearance/F is 0.73 1.h-1 and the distribution volume/F is 2.2 1. Ciclopirox olamine, after intravaginal administration, shows low absorption (about 2%) and is mainly transformed into glucuronide derivatives.

Online source: www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=1524626&dopt=Abstract ciclopirox Penlac



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Efficacy of different concentrations of ciclopirox shampoo for the treatment of seborrheic dermatitis of the scalp: results of a randomized, double-blind, vehicle-controlled trial.

Altmeyer P, Hoffmann K; Loprox Shampoo Dosing Concentration Study Group.

Department of Dermatology, Ruhr-University Bochum, St. Josef-Hospital, Bochum, Germany. p.altmeyer derma.de

BACKGROUND: Seborrheic dermatitis is a common inflammatory skin disorder affecting 1-3% of the population. It is thought to be linked to dandruff via a common etiology, yeasts of the genus Malassezia. Ciclopirox is a broad-spectrum, hydroxypyridone-derived, synthetic antifungal agent with anti-inflammatory properties. METHODS: A total of 203 patients were enrolled in this vehicle-controlled, double-blind, randomized study designed to compare vehicle with three different concentrations of ciclopirox shampoo: 0.1%, 0.3% and 1%, with each applied twice a week. The main efficacy parameters were based on 6-point ordinal scales describing the disease's signs and symptoms (scaling, inflammation and itching), global status of disease, and global change in disease. RESULTS: A tendency towards improvement of the sum score from baseline was found in all ciclopirox treatment groups. The most pronounced improvement was found in the ciclopirox 1% group, which changed from a baseline sum score of 8.3 to 4.4 at the end of the 4-week study period (P-value vs. vehicle 0.0372). In addition, the therapeutic index showed increasing efficacy with the use of increased concentrations of ciclopirox. CONCLUSIONS: The study supports the use of 1% ciclopirox shampoo in the treatment of seborrheic dermatitis of the scalp. Furthermore, ciclopirox shampoo at each concentration was found to be safe and well tolerated.

Online source: www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=15271194&dopt=Abstract ciclopirox Penlac