In vitro release and antiinflammatory activity of topical formulations of ketoprofen.
Ketoprofen (KP) is a potent nonsteroidal anti-inflammatory drug (NSAID) widely used in clinical practice for the control of acute and chronic pain of soft tissues and skeletal muscle system. The importance of KP in the therapeutic field, has stimulated the development of topical dosage forms to improve its percutaneous absorption through the application site. Moreover they could provide relatively consistent drug levels for prolonged periods and avoid gastric irritation, typical side effect of NSAID oral administration. Since the topical formulation efficiency depends on vehicle characteristics, some different ointments, at 1% and 5% concentrations of KP, were evaluated by in vitro and in vivo studies. Among tested ointments, 1% Carbopol cream and 5% Carbopol gel showed the best fluxes of drug through regenerated cellulose membrane. The in vivo percutaneous absorption of KP, evaluated by carrageenan-induced paw edema in rats, showed a good correlation with the in vitro results about considered creams, but the gels in vivo activity was not in according to their in vitro behaviour. The extemporaneous Carbopol cream was able to produce a better edema inhibition than the commercial one, taken as a reference and widely utilized as a topical therapeutic item. About gels, the obtained results were nearly the maximum response considered possible for a topical antiinflammatory drug.
Moretti
M D
MD
Dipartimento di Scienze del Farmaco, Università degli Studi di Sassari, Italy.
Gavini
E
E
Peana
A T
AT
D000287:Administration, Topical; D000818:Animals; D000893:Anti-Inflammatory Agents / Q000008:administration & dosage* / Q000493:pharmacokinetics / Q000494:pharmacology*; D004487:Edema / Q000139:chemically induced / Q000517:prevention & control; D005782:Gels; D007660:Ketoprofen / Q000008:administration & dosage* / Q000493:pharmacokinetics / Q000494:pharmacology*; D008297:Male; D009824:Ointments; D051381:Rats; D017208:Rats, Wistar; D012869:Skin Absorption
D000893:Anti-Inflammatory Agents; D005782:Gels; D009824:Ointments; D007660:Ketoprofen