Effect of polyol fatty acid esters on diclofenac permeation through rat skin.
The effects of a series of polyol fatty acid esters (sefsols) on diclofenac permeation through rat skin were investigated using in vitro and in vivo methods. Four monoesters and one diester of sefsol were selected as a vehicle components. The effects of each sefsol on in vitro diclofenac permeation were compared at a concentration of 5% sefsol in water. Monoesters of sefsol, except the glyceryl monoester, enhanced the percutaneous permeation of diclofenac. The highest enhancement was observed in propylene glycol monocaprylate. The plasma concentration of diclofenac was increased dramatically by the addition of 10% propylene glycol monocaprylate when applying the diclofenac sodium suspension to abdominal rat skin in vivo. These results suggest that the monoesters of polyol fatty acid are potential candidates to enhance the transdermal absorption of diclofenac sodium.
Takahashi
K
K
Institute of Pharmaceutical Sciences, Mukogawa Women's University School of Pharmacy, Hyogo, Japan.
Matsumoto
T
T
Kimura
T
T
Sakano
H
H
Mizuno
N
N
Yata
N
N
D000279:Administration, Cutaneous; D000818:Animals; D000893:Anti-Inflammatory Agents / Q000494:pharmacology*; D002210:Caprylates / Q000494:pharmacology*; D004008:Diclofenac / Q000097:blood / Q000493:pharmacokinetics / Q000494:pharmacology*; D066298:In Vitro Techniques; D008297:Male; D011409:Propylene Glycols / Q000494:pharmacology*; D051381:Rats; D017208:Rats, Wistar; D012869:Skin Absorption / Q000187:drug effects*
D000893:Anti-Inflammatory Agents; D002210:Caprylates; D011409:Propylene Glycols; D004008:Diclofenac