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We hypothesised that Hansen solubility parameters (HSPs) can be used to predict drug-nail affinities. Our aims were to: i) determine the HSPs (δD, δP, δH) of the nailplate, the hoof membrane (a model for the nailplate), and of the drugs terbinafine HCl, amorolfine HCl, ciclopirox olamine and efinaconazole, by measuring their swelling/solubility in organic liquids, ii) predict nail-drug interactions by comparing drug and nail HSPs, and iii) evaluate the accuracy of these predictions using literature reports of experimentally-determined affinities of these drugs for keratin, the main constituent of the nailplate and hoof. Many solvents caused no change in the mass of nailplates, a few solvents deswelled the nail, while others swelled the nail to varying extents. Fingernail and toenail HSPs were almost the same, while hoof HSPs were similar, except for a slightly lower δP. High nail-terbinafine HCl, nail-amorolfine HCl and nail-ciclopirox olamine affinities, and low nail-efinaconazole affinities were then predicted, and found to accurately match experimental reports of these drugs’ affinities to keratin. We therefore propose that drug and nail Hansen solubility parameters may be used to predict drug-nail interactions, and that these results can assist in the design of drugs for the treatment of nail diseases, such as onychomycosis and psoriasis. To our knowledge, this is the first report of the application of HSPs in ungual research.
We hypothesised that Hansen solubility parameters (HSPs) can be used to predict drug-nail affinities. Our aims were to: i) determine the HSPs (δD, δP, δH) of the nailplate, the hoof membrane (a model for the nailplate), and of the drugs terbinafine HCl, amorolfine HCl, ciclopirox olamine and efinaconazole, by measuring their swelling/solubility in organic liquids, ii) predict nail-drug interactions by comparing drug and nail HSPs, and iii) evaluate the accuracy of these predictions using literature reports of experimentally-determined affinities of these drugs for keratin, the main constituent of the nailplate and hoof. Many solvents caused no change in the mass of nailplates, a few solvents deswelled the nail, while others swelled the nail to varying extents. Fingernail and toenail HSPs were almost the same, while hoof HSPs were similar, except for a slightly lower δP. High nail-terbinafine HCl, nail-amorolfine HCl and nail-ciclopirox olamine affinities, and low nail-efinaconazole affinities were then predicted, and found to accurately match experimental reports of these drugs’ affinities to keratin. We therefore propose that drug and nail Hansen solubility parameters may be used to predict drug-nail interactions, and that these results can assist in the design of drugs for the treatment of nail diseases, such as onychomycosis and psoriasis. To our knowledge, this is the first report of the application of HSPs in ungual research.
Application of Hansen Solubility Parameters to predict drug-nail interactions, which can assist the design of nail medicines
2016-05-01
European Journal of Pharmaceutics and Biopharmaceutics , 102 pp. 32-40. (2016)
Article (Journal)
Electronic Resource
English
solubility parameters , drug , nail , Hansen , nail-drug interaction , swelling , hoof , ungual , keratin , prediction
DDC:
690
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