title: Preparation and in vivo evaluation of a gel-based nasal delivery system for risperidone.
abstract: The aim of this study was to prepare a nasal gel of risperidone and to investigate the pharmacokinetics and relative bioavailability of the drug in rats. Compared with oral dosing, the risperidone nasal gel exhibited very fast absorption and high bioavailability. Maximal plasma concentration (cmax) and the time to reach cmax (tmax) were 15.2 μg mL-1 and 5 min for the nasal gel, 3.6 μg mL-1 and 30 min for the oral drug suspension, respectively. Pharmacokinetic parameters such as tmax', cmax and AUC of oral and nasal routes were significantly different (p < 0.01). Relative bioavailability of the drug nasal preparation to the oral suspension was up to 1600.0 %. Further, the in vitro effect of the risperidone nasal gel on nasal mucociliary movement was also investigated using a toad palate model. The risperidone nasal formulation showed mild ciliotoxicity, but the adverse effect was temporary and reversible.
authors.forename: Fugen
authors.initials: F
authors.lastname: Gu
authors.forename: Weina
authors.initials: W
authors.lastname: Ma
authors.forename: Gendalai
authors.initials: G
authors.lastname: Meng
authors.forename: Chunzhi
authors.initials: C
authors.lastname: Wu
authors.forename: Yi
authors.initials: Y
authors.lastname: Wang
mesh_terms: D000281:Administration, Intranasal; D000818:Animals; D014150:Antipsychotic Agents / Q000008:administration & dosage* / Q000009:adverse effects / Q000097:blood / Q000493:pharmacokinetics; D001001:Anura; D001682:Biological Availability; D002923:Cilia / Q000187:drug effects / Q000378:metabolism; D065127:Dopamine D2 Receptor Antagonists / Q000008:administration & dosage* / Q000009:adverse effects / Q000097:blood / Q000493:pharmacokinetics; D004339:Drug Compounding; D016503:Drug Delivery Systems; D005782:Gels; D066298:In Vitro Techniques; D008297:Male; D009061:Mouth Mucosa / Q000187:drug effects / Q000378:metabolism; D065588:Nasal Absorption; D009297:Nasal Mucosa / Q000187:drug effects / Q000378:metabolism*; D010159:Palate; D011897:Random Allocation; D017208:Rats, Wistar; D018967:Risperidone / Q000008:administration & dosage* / Q000009:adverse effects / Q000097:blood / Q000493:pharmacokinetics; D058830:Serotonin 5-HT2 Receptor Antagonists / Q000008:administration & dosage* / Q000009:adverse effects / Q000097:blood / Q000493:pharmacokinetics
chemical_list: D014150:Antipsychotic Agents; D065127:Dopamine D2 Receptor Antagonists; D005782:Gels; D058830:Serotonin 5-HT2 Receptor Antagonists; D018967:Risperidone