title: Formulation and evaluation of ondansetron nasal delivery systems.
abstract: This study aimed to formulate and evaluate nasal delivery systems containing ondansetron hydrochloride. In the in vitro study, the permeation rate with the addition of 10% polyethylene glycol 300 (PEG 300) to aqueous solution containing 0.01% benzalkonium chloride (BC) and 10% sulfobutylether beta-cyclodextrin sodium salt (SBCD) was somewhat more rapid up to 1.5h compared to the addition of 10% PG. The permeation flux increased as the drug concentration increased regardless of the vehicles used. The addition of nicotinamide or chitosan to aqueous drug solution (40 mg/ml) with 10% PEG 300 and 0.01% BC rather decreased permeation rate and delayed lag time. Even though cyclodextrins including SBCD or dimethyl-ss-cyclodextrin failed to show permeation enhancing effects of ondansetron hydrochloride, the addition of 10% SBCD to aqueous solution containing 10% PEG 300 and 0.01% BC could be a good candidate for ondansetron nasal delivery systems because of its safety profile, stable storage in refrigerator and solubilizing effect. With the above formulation, the nasal delivery system increased AUC0-2h and Cmax by 2.1 and 1.7 times compared to those of oral delivery, respectively while there was no difference found in AUC0-2h with intravenous administration. Therefore, the nasal delivery system of ondansetron hydrochloride formulated in this study was feasible for nasal administration.
authors.affiliation: College of Pharmacy, Dongduk Women's University, Seoul 136-714, South Korea.
authors.forename: Eunsook
authors.initials: E
authors.lastname: Cho
authors.forename: Hyesun
authors.initials: H
authors.lastname: Gwak
authors.forename: Inkoo
authors.initials: I
authors.lastname: Chun
mesh_terms: D000281:Administration, Intranasal; D000284:Administration, Oral; D000818:Animals; D000932:Antiemetics / Q000008:administration & dosage* / Q000737:chemistry / Q000493:pharmacokinetics; D055598:Chemical Phenomena; D002626:Chemistry, Pharmaceutical; D002627:Chemistry, Physical; D002851:Chromatography, High Pressure Liquid; D016503:Drug Delivery Systems; D005079:Excipients; D006207:Half-Life; D066298:In Vitro Techniques; D007275:Injections, Intravenous; D009297:Nasal Mucosa; D017294:Ondansetron / Q000008:administration & dosage* / Q000737:chemistry / Q000493:pharmacokinetics; D010539:Permeability; D014677:Pharmaceutical Vehicles; D011817:Rabbits; D051381:Rats; D012995:Solubility