Abstract
The treatment of onychomycosis is a challenging task because of unique barrier properties of the nail plate which hampers the passage of antifungal drugs in a concentration required to eradicate the deeply seated causative fungi in the nail bed. In present investigation, application of hydroxypropyl-β-cyclodextrin (HP-β-CD) was established as an effective and nail friendly transungual drug permeation enhancer especially for poorly water soluble drugs using terbinafine hydrochloride as a poorly soluble drug. HP-β-CD significantly improves hydration of nail plates and increases solubility of terbinafine hydrochloride in the aqueous environment available therein, which leads to uninterrupted drug permeation through water filled pores of hydrogel-like structure of hydrated nail plates. A nail lacquer formulation was designed with an objective to deliver the drug in an effective concentration across nail plates, using HP-β-CD as a permeation enhancer. The formulations containing HP-β-CD showed higher flux than the control formulation in in vitro drug permeation study. The formulation containing 10% w/v of HP-β-CD showed maximum flux of 4.586 ± 0.08 μg/mL/cm2 as compared to the control flux of 0.868 ± 0.06 μg/mL/cm2. This finding supports application of HP-β-CD as an effective permeation enhancer for transungual delivery of terbinafine hydrochloride and possibly other poorly water soluble drugs where HP-β-CD can act as a solubilizer.
Highlights
Onychomycosis is the most common nail fungal disease, which causes discoloration, thickening, hardening, and crumbling of the infected nails [1].The delivery and maintenance of an effective concentration of antimycotic drugs higher than their minimum inhibitory concentration (MIC) across nail plate are a major challenge faced in the treatment of onychomycosis
To eliminate its systemic toxicity, topical route of drug administration could be used in place of oral route
Triethyl citrate was received as a free sample from Morflex, Inc., North Carolina, USA, and HP-β-CD was obtained from Signet Chemical Corporation Pvt
Summary
The delivery and maintenance of an effective concentration of antimycotic drugs higher than their minimum inhibitory concentration (MIC) across nail plate are a major challenge faced in the treatment of onychomycosis. The conventional drug therapy involves daily administration of antifungal drugs through oral and topical routes. The inherent problem with transungual formulations is their poor drug permeability through nail plate and, the drug flux is mostly lower than its MIC [5, 6]. Nail lacquer formulations have, emerged as an effective topical drug delivery system for treating nail fungal diseases [1, 7]. As antifungal drugs are mostly water insoluble and show poor transungual permeability, their delivery across the nail plate in adequate concentration from nail lacquer formulation is not possible
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