Biological activity and characteristics of triamcinolone-acetonide formulated with the self-regulating drug carriers, Transfersomes.
Novel formulations of the halogenated corticosteroid, triamcinolone-acetonide, based on ultradeformable mixed lipid vesicles, Transfersomes, are described. Their performance was tested in vivo using radioactive label measurements, to study the drug biodistribution, and murine ear edema, to determine the drug bioactivity. Sparse use of drug-loaded Transfersomes on the skin ensures an almost exclusive delivery of triamcinolone-acetonide into the organ, thus arguably increasing the treatment safety. Delivery of triamcinolone-acetonide in the skin with ultradeformable vesicles prolongs the anti-inflammatory drug action several times compared to drug usage in a conventional crème or an ointment, the robustness of biological response for the former being at least identical to the latter. The required dose of Transfersome-based triamcinolone-acetonide is also greatly reduced. The drug dose of 0.2 microg cm(-2) suppresses 75% of arachidonic acid-induced murine ear edema for at least 48 h. In contrast, a conventional formulation of triamcinolone-acetonide requires a 10-fold higher drug dosage to achieve a similar effect. In either case, increasing the applied corticosteroid amount delays the onset of anti-edema action.
Cevc
Gregor
G
Medizinische Biophysik, Klinikum r. d. I., Technische Universität München, Ismaningerstr. 22 D-81675, Munich, Germany. cevc@idea-ag.de
Blume
Gabriele
G
D000287:Administration, Topical; D000818:Animals; D000893:Anti-Inflammatory Agents / Q000008:administration & dosage / Q000494:pharmacology*; D002626:Chemistry, Pharmaceutical; D004195:Disease Models, Animal; D004337:Drug Carriers; D004427:Ear Diseases / Q000188:drug therapy; D004487:Edema / Q000188:drug therapy; D007275:Injections, Intravenous; D008081:Liposomes; D051379:Mice; D008815:Mice, Inbred Strains; D009824:Ointments; D012867:Skin / Q000187:drug effects*; D012871:Skin Diseases / Q000188:drug therapy; D013997:Time Factors; D014222:Triamcinolone Acetonide / Q000008:administration & dosage / Q000493:pharmacokinetics / Q000494:pharmacology*
D000893:Anti-Inflammatory Agents; D004337:Drug Carriers; D008081:Liposomes; D009824:Ointments; D014222:Triamcinolone Acetonide