The selection of non-steroidal anti-inflammatory agents for dermal delivery.
An analysis has been conducted to show how the penetration of a selection of non-steroidal anti-inflammatory agents (NSAIDs) through the skin may be predicted. The calculations are based on physicochemical parameters that can be predicted using commercially available software. Where available the predictions compare favourably with the literature values. The bio-effectiveness of the NSAID will be a function of both its penetration through the skin and its potency. The variation in potency has also been considered. Most NSAIDs are carboxylic acids, therefore the pK(a) will be an important determinant in ionisation and hence permeation. pH partition behaviour into the skin has been considered together with the relative impact of decreased permeation but increased solubility with degree of ionisation.
Hadgraft
J
J
The Welsh School of Pharmacy, Cardiff University, Redwood Building, CF1 3XF, Cardiff, UK. jonathan.hadgraft@btinternet.com
du Plessis
J
J
Goosen
C
C
D000279:Administration, Cutaneous; D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000008:administration & dosage* / Q000737:chemistry / Q000493:pharmacokinetics; D006801:Humans; D006863:Hydrogen-Ion Concentration; D008970:Molecular Weight; D010539:Permeability; D012869:Skin Absorption; D012995:Solubility
D000894:Anti-Inflammatory Agents, Non-Steroidal