Kerai, LV;
Hilton, S;
Maugueret, M;
Kazi, BB;
Faull, J;
Bhakta, S;
Murdan, S;
(2016)
UV-curable gels as topical nail medicines:In vivo residence, anti-fungal efficacy and influence of gel components on their properties.
International Journal of Pharmaceutics
, 514
(1)
pp. 244-254.
10.1016/j.ijpharm.2016.08.025.
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Abstract
UV-curable gels, used as nail cosmetics for their in vivo durability, were reported to be promising as topical nail medicines. Our first aim was thus to investigate whether such durability applies to drug-loaded formulations. This was found to be true. However, ethanol inclusion in the pharmaceutical formulation (to enable drug loading) reduced the in vivo residence. The second aim was therefore to determine any other effects of ethanol, and if ethanol could be avoided by the choice of monomers. Thus, three methacrylate monomers, ethyl methacrylate, isobornyl methacrylate and 2-hydroxyethyl methacrylate (HEMA) were selected, and their influence on the formulation properties were determined. Ethanol and the methacrylate monomer influenced some (but not all) of the formulation properties. The most significant was that HEMA could dissolve drug and enable the preparation of ethanol-free, drug-loaded formulations, which would benefit in vivo residence. The absence of ethanol reduced drug loading, release and ungual flux, but had no negative impact on the in vitro anti-fungal efficacy. Thus, judicious selection of gel components enabled the exclusion of ethanol. The long in vivo residence, little residual monomers, sufficient ungual permeation and in vitro anti-fungal activity of the gels indicates their potential as anti-onychomycotic topical medicines.
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