A therapeutic dose of primaquine can be delivered across excised human skin from simple transdermal patches.
This work investigated the permeation of primaquine across full-thickness excised human skin from two acrylate transdermal adhesives. Primaquine base was formulated with National Starch 387-2516 and 387-2287 to provide aluminium foil-backed 1-cm diameter patches, each loaded with 10 mg drug. Other patches were prepared that included Migliol 840 as a potential penetration enhancer. The patches were applied to cadaver skin in Franz-type diffusion cells and the permeation of primaquine determined over a 24-h period. Relatively high fluxes were found, the highest being from those formulations lacking the Migliol 840: 5.68+/-0.30x10(-2) mg cm(-2) h(-1) from 387-2516; 4.94+/-0.20x10(-2) mg cm(-2) h(-1) from 387-2287. It was determined that a simple patch with a diameter of approximately 13 cm(2) could deliver a therapeutic in vivo dose, with possibilities for the treatment and prophylaxis of Plasmodium vivax, P. ovale and P. falciparum forms of malaria. The presence of Migliol 840 failed to produce the anticipated enhancing effect: flux rates that were approximately halved. These results could to a certain extent be rationalised in terms of thermodynamic activity.
Jeans
C W
CW
Welsh School of Pharmacy, Cardiff University, Cardiff, UK.
Heard
C M
CM
D000269:Adhesives; D000279:Administration, Cutaneous; D000962:Antimalarials / Q000008:administration & dosage*; D002626:Chemistry, Pharmaceutical; D002851:Chromatography, High Pressure Liquid; D005260:Female; D006207:Half-Life; D006801:Humans; D008297:Male; D011319:Primaquine / Q000008:administration & dosage* / Q000493:pharmacokinetics; D012869:Skin Absorption
D000269:Adhesives; D000962:Antimalarials; D011319:Primaquine