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Merck
  • Comparison of the antifungal efficacy of terbinafine hydrochloride and ciclopirox olamine containing formulations against the dermatophyte Trichophyton rubrum in an infected nail plate model.

Comparison of the antifungal efficacy of terbinafine hydrochloride and ciclopirox olamine containing formulations against the dermatophyte Trichophyton rubrum in an infected nail plate model.

Molecular pharmaceutics (2014-02-05)
Anja Täuber, Christel C Müller-Goymann
초록

Onychomycosis is a fungal infection mostly induced by dermatophytes such as Trichophyton rubrum. Due to slow nail growth, the treatment takes 3-9 months depending on the nail size and infected area. Hence, high efficacy of the active ingredient without systemic side effects is of major interest. To test the efficacy of an antifungal formulation, an appropriate in vitro model reflecting the in vivo situation as close as possible is required. In this study, a variety of antifungal formulations, i.e., commercial ones (Ciclopoli and Lamisil cream), those used in compounding pharmacies (Pentravan) as well as poloxamer 407-based systems, have been evaluated in an infected nail plate model. The active pharmaceutical ingredients (APIs) were ciclopirox olamine and terbinafine hydrochloride. The poloxamer 407-based formulations consisted of poloxamer 407, double distilled water, propylene glycol, isopropyl alcohol, medium chain triglycerides and either 1% ciclopirox olamine or 1% terbinafine hydrochloride as API, respectively. Former studies have shown high permeation rates of terbinafine hydrochloride from similar poloxamer 407-based formulations with dimethyl isosorbide instead of propylene glycol. The present contribution shows superior inhibition of T. rubrum growth from poloxamer 407-based formulations in comparison to the commercial Lamisil cream. Moreover, poloxamer 407-based formulations were equally effective as the nail lacquer Ciclopoli even though the poloxamer formulations contained only 1% of the drug instead of 8% in the marketed lacquer. Poloxamer 407-based systems containing ciclopirox olamine proved to be about as effective as similar terbinafine hydrochloride systems.

MATERIALS
Product Number
브랜드
제품 설명

Sigma-Aldrich
2-Propanol, electronic grade, 99.999% trace metals basis
Ciclopirox olamine, European Pharmacopoeia (EP) Reference Standard
Supelco
Ergosterol, Pharmaceutical Secondary Standard; Certified Reference Material
USP
Ciclopirox olamine, United States Pharmacopeia (USP) Reference Standard
Ergosterol, European Pharmacopoeia (EP) Reference Standard
Sigma-Aldrich
2-Propanol, anhydrous, 99.5%
Sigma-Aldrich
Ergosterol, ≥75%
Sigma-Aldrich
1,2-Propanediol, puriss. p.a., ACS reagent, ≥99.5% (GC)
Sigma-Aldrich
1,2-Propanediol, ACS reagent, ≥99.5%
Supelco
1,2-Propanediol, analytical standard
Sigma-Aldrich
1,2-Propanediol, meets analytical specification of Ph. Eur., BP, USP, ≥99.5%
Sigma-Aldrich
1,2-Propanediol, ReagentPlus®, 99%
Sigma-Aldrich
Urea, BioUltra, 99% (T)
Supelco
Urea, 8 M (after reconstitution with 16 mL high purity water)
Sigma-Aldrich
Urea, ACS reagent, 99.0-100.5%
USP
Urea, United States Pharmacopeia (USP) Reference Standard
Sigma-Aldrich
Urea, BioXtra, pH 7.5-9.5 (20 °C, 5 M in H2O)
Sigma-Aldrich
Urea, suitable for electrophoresis
Sigma-Aldrich
Urea, meets USP testing specifications
Sigma-Aldrich
Urea, puriss. p.a., ACS reagent, reag. Ph. Eur., ≥99%
Sigma-Aldrich
Urea, powder, BioReagent, suitable for cell culture
Sigma-Aldrich
Urea, puriss., meets analytical specification of Ph. Eur., BP, USP, 99.0-100.5%, 99.0-101.0% (calc. on dry substance)
Sigma-Aldrich
Urea, ReagentPlus®, ≥99.5%, pellets
Supelco
Monobasic Potassium Phosphate, Pharmaceutical Secondary Standard; Certified Reference Material
Sigma-Aldrich
2-Propanol, BioReagent, ≥99.5%
Sigma-Aldrich
2-Propanol, puriss. p.a., ACS reagent, ≥99.8% (GC)
Sigma-Aldrich
2-Propanol, suitable for HPLC, 99.9%
Sigma-Aldrich
2-Propanol, ACS reagent, ≥99.5%
Sigma-Aldrich
Isopropyl alcohol, meets USP testing specifications
Sigma-Aldrich
2-Propanol, BioUltra, ≥99.5% (GC)