Transungual delivery of ketoconazole using novel lacquer formulation
ABSTRACT Onychomycosis, a common fungal infection of the nail, can have a substantial impact on quality of life. The success of topical therapy for onychomycosis depends on effective penetration, which can be enhanced using an appropriate delivery method. This study evaluated the effectiveness of a novel topical lacquer on enhancing [14C]-ketoconazole penetration by comparing nail absorption, nail distribution, and nail penetration of [(14)C]-ketoconazole dissolved in the novel lacquer versus a commercial ketoconazole cream. Using the in vitro finite dose model, the formulations were applied daily to human nail plates for 7 days. Drug absorption was measured by monitoring rate of appearance in each nail layer and the supporting bed. After the multiple day treatment, cumulative concentrations of ketoconazole formulated in novel lacquer in the deep nail layer and the nail bed were significantly greater than cumulative concentrations of commercial ketoconazole (p<0.05), as well as several orders of magnitude greater than the Minimal Inhibitory Concentration (MIC) deemed necessary to inhibit the growth of causative dermatophytic and yeast species. These results suggest that this novel ketoconazole lacquer has the potential to be an effective topical treatment for onychomycosis.
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ABSTRACT: Although considered as trifling illness, nail diseases have a reasonably high occurrence and a noteworthy impact on the patients’ quality of life. Furthermore, there is a need to improve the topical treatment for nail diseases to avoid drug interactions and to reduce side effects associated with oral therapy. Topical drug delivery to the nails has established amplified consideration lately. Strategies (such as chemical enhancers, formulation strategies, physical and mechanical methods) are being investigated in order to improve drug permeability across the nail plate. The rationale of this review is to present contemporary information on the structure of human nail along with its comparison with animal hooves. Precincts of nail permeability have been briefly discussed with respect to factors like permeant's molecular size, hydrophilicity, charge and the nature of the vehicle etc. These factors affect drug uptake and permeation through the nail. Formulations like nail lacquers which mimic cosmetic varnish and colloidal carriers along with nail substitutes that can be utilized for TU delivery have also been discussed.This article is protected by copyright. All rights reserved.International journal of cosmetic science 05/2014; 36(5). DOI:10.1111/ics.12142 · 1.45 Impact Factor
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ABSTRACT: The present therapy adopted by physicians for the treatment of fungal includes the systemic administration and topical administration of antifungal agents. A concern in these formulations involves systemic adverse effects and also less concentration of drug at the site of infection. Hence an attention has recently been focused on novel drug delivery of antifungal agents which is the most widely accepted approach.Journal of Pharmaceutical Innovation 05/2014; · 1.25 Impact Factor
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ABSTRACT: Topical therapy is at the forefront in treating nail ailments (especially onychomycosis and nail psoriasis) due to its local effects, which circumvents systemic adverse events, improves patient compliance and reduces treatment cost. However, the success of topical therapy has been hindered due to poor penetration of topical therapeutics across densely keratinized nail plate barrier. For effective topical therapy across nail plate, ungual drug permeation must be enhanced. Present review is designed to provide an insight into prime aspects of transungual drug deliveryviz. nail structure and physiology, various onychopathies, techniques of nail permeation enhancement andin vitro models for trans-nail drug permeation studies. Updated list of drug molecules studied across the nail plate and key commercial products have been furnished with sufficient depth. Patents pertinent to, and current clinical status of transungual drug delivery have also been comprehensively reviewed. This is the first systematic critique encompassing the detailed aspects of transungual drug delivery. In our opinion, transungual drug delivery is a promising avenue for researchers to develop novel formulations, augmenting pharmaceutical industries to commercialize the products for nail disorders.Journal of Drug Targeting 05/2014; 22(9):769-789. DOI:10.3109/1061186X.2014.929138 · 2.72 Impact Factor