Alteration of the diffusional barrier property of the nail leads to greater terbinafine drug loading and permeation

The diffusional barrier property of biological systems varies with ultrastructural organization of the tissues and/or cells, and often plays an important role in drug delivery. The nail plate is a thick, hard and impermeable membrane which makes topical nail drug delivery challenging. The current st...

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Bibliographic Details
Published in:International journal of pharmaceutics 2009-06, Vol.375 (1), p.22-27
Main Authors: Nair, Anroop B., Sammeta, Srinivasa M., Kim, Hyun D., Chakraborty, Bireswar, Friden, Phillip M., Murthy, S. Narasimha
Format: Article
Language:English
Subjects:
Abrasion
Administration, Topical
Aged
Aged, 80 and over
Antifungal Agents - administration & dosage
Antifungal Agents - pharmacokinetics
Biological and medical sciences
Cadaver
Drug Delivery Systems
Enhancers
Female
General pharmacology
Humans
In Vitro Techniques
Iontophoresis
Male
Medical sciences
Middle Aged
Nail barrier
Nails - metabolism
Nails - ultrastructure
Naphthalenes - administration & dosage
Naphthalenes - pharmacokinetics
Permeability
Pharmaceutical technology. Pharmaceutical industry
Pharmacology. Drug treatments
Pretreatment
Terbinafine
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Summary:The diffusional barrier property of biological systems varies with ultrastructural organization of the tissues and/or cells, and often plays an important role in drug delivery. The nail plate is a thick, hard and impermeable membrane which makes topical nail drug delivery challenging. The current study investigated the effect of physical and chemical alteration of the nail on the trans-ungual drug delivery of terbinafine hydrochloride (TH) under both passive and iontophoretic conditions. Physical alterations were carried out by dorsal or ventral nail layer abrasion, while chemical alterations were performed by defatting or keratolysis or ionto-keratolysis of the nails. Terbinafine permeation into and across the nail plate following various nail treatments showed similar trends in both passive and iontophoretic delivery, although the extent of drug delivery varied with treatment. Application of iontophoresis to the abraded nails significantly improved ( P < 0.05) TH permeation and loading compared to abraded nails without iontophoresis or normal nails with iontophoresis. Drug permeation was not enhanced when the nail plate was defatted. Keratolysis moderately enhanced the permeation but not the drug load. Ionto-keratolysis enhanced TH permeation and drug load significantly ( P < 0.05) during passive and iontophoretic delivery as compared to untreated nails. Ionto-keratolysis may be more efficient in permeabilization of nail plates than long term exposure to keratolysing agents.
ISSN:0378-5173
1873-3476
DOI:10.1016/j.ijpharm.2009.03.012