Permeation studies of indomethacin from different emulsions for nasal delivery and their possible anti-inflammatory effects.
The purpose of this research was to develop an emulsion formulation of indomethacin (IND) suitable for nasal delivery. IND was incorporated into the oil phases of oil in water (O/W) and water in oil (W/O) emulsions. For this purpose, different emulsifying agents (Tween 80, Span 80 and Brij 58) were used in two emulsion formulations. When the effects of several synthetic membranes (nylon, cellulose, cellulose nitrate) were compared with the sheep nasal mucosa, the cellulose membrane and sheep nasal mucosa showed similar permeation properties for O/W emulsion (P > 0.05). To examine the absorption characteristics of IND, the anti-inflammatory properties of intravenous solution of IND, intranasal O/W emulsions of IND (with or without enhancers) and intranasal solution of IND (IND-Sol) were investigated in rats with carrageenan-induced paw edema. When citric acid was added to the nasal emulsion, the anti-inflammatory activity was similar to that of intravenous solution (P > 0.05). Finally, it was concluded that, intranasal administration of IND emulsion with citric acid may be considered as an alternative to intravenous and per oral administrations of IND to overcome their adverse effects.
Karasulu
H Yeşim
HY
Department of Pharmaceutical Technology, Faculty of Pharmacy, University of Ege, 35100 Bornova, Izmir, Turkey. yesim.karasulu@ege.edu.tr
Sanal
Z Evren
ZE
Sözer
Sumru
S
Güneri
Tamer
T
Ertan
Gökhan
G
D000281:Administration, Intranasal; D000818:Animals; D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000008:administration & dosage* / Q000737:chemistry / Q000378:metabolism; D002351:Carrageenan; D002592:Cetomacrogol / Q000737:chemistry; D002626:Chemistry, Pharmaceutical; D019343:Citric Acid / Q000737:chemistry; D004195:Disease Models, Animal; D004339:Drug Compounding; D004487:Edema / Q000139:chemically induced / Q000517:prevention & control*; D045703:Emulsifying Agents / Q000737:chemistry; D004655:Emulsions; D006601:Hexoses / Q000737:chemistry; D007213:Indomethacin / Q000008:administration & dosage* / Q000737:chemistry / Q000378:metabolism; D007275:Injections, Intravenous; D008297:Male; D008567:Membranes, Artificial; D009297:Nasal Mucosa / Q000378:metabolism*; D010539:Permeability; D011136:Polysorbates / Q000737:chemistry; D051381:Rats; D017208:Rats, Wistar; D012756:Sheep; D013024:Soybean Oil / Q000737:chemistry*; D013997:Time Factors; D014867:Water / Q000737:chemistry*
D000894:Anti-Inflammatory Agents, Non-Steroidal; D045703:Emulsifying Agents; D004655:Emulsions; D006601:Hexoses; D008567:Membranes, Artificial; D011136:Polysorbates; D014867:Water; C018665:sorbitan monooleate; D019343:Citric Acid; D013024:Soybean Oil; D002351:Carrageenan; D002592:Cetomacrogol; D007213:Indomethacin