Effect of skin pretreatment with fatty acids on percutaneous absorption and skin retention of piroxicam after its topical application.
The enhancing effect of several fatty acids from different subclasses: saturated (lauric acid), mono-unsaturated (oleic acid) and poly-unsaturated (linoleic and linolenic acids) in the percutaneous absorption of piroxicam was investigated. These fatty acids were applied on the skin membrane in three different ways: included in the vehicle, as a pretreatment or both. An increase in piroxicam flux value was found for lauric and oleic acids in the following order: skin pretreatment with 5% fatty acids followed by application of gels containing 5% fatty acids>skin pretreatment with 5% fatty acids followed application of control gel>gel containing 5% fatty acids without skin pretreatment. For linoleic and linolenic acids, the piroxicam flux in the two pretreatment experiments was almost the same, although higher than when fatty acids were included in the formulation. Skin pretreatment with 5% linolenic acid in propylene glycol followed by application of control gel or a gel containing 5% linolenic acid, showed the highest enhancing capacity. After skin pretreatment with fatty acids, the lag time values decreased nearly three times compared to those obtained when the same fatty acids were included in the formulation. The amount of piroxicam retained in the skin after pretreatment with fatty acids was found to be very similar for all fatty acids and 3-fold higher than in the experiments without skin pretreatment.
Santoyo
S
S
Centro Galénico, Departamento de Farmacia y Tecnología Farmacéutica, Facultad de Farmacia, Universidad de Navarra, Pamplona, Spain. ssantoyo@unav.es
Ygartua
P
P
D000287:Administration, Topical; D000818:Animals; D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000493:pharmacokinetics*; D005227:Fatty Acids / Q000008:administration & dosage* / Q000494:pharmacology; D005782:Gels; D008297:Male; D010539:Permeability; D010894:Piroxicam / Q000008:administration & dosage / Q000493:pharmacokinetics*; D051381:Rats; D017208:Rats, Wistar; D012867:Skin / Q000378:metabolism*; D012869:Skin Absorption
D000894:Anti-Inflammatory Agents, Non-Steroidal; D005227:Fatty Acids; D005782:Gels; D010894:Piroxicam