title: Quetiapine Nanoemulsion for Intranasal Drug Delivery: Evaluation of Brain-Targeting Efficiency.
abstract: To evaluate the possibility of improved drug delivery of quetiapine fumarate (QTP), a nanoemulsion system was developed for intranasal delivery. Effects of different HLBs of Emalex LWIS 10, PEG 400 and Transcutol P, as co-surfactants, were studied on isotropic region of pseudoternary-phase diagrams of nanoemulsion system composed of capmul MCM (CPM) as oil phase, Tween 80 as surfactant and water. Phase behaviour, globule size, transmission electron microscope (TEM) photographs and brain-targeting efficiency of quetiapine nanoemulsion were investigated. In vitro dissolution study of optimised nanoemulsion formulation, with mean diameter 144 ± 0.5 nm, showed more than twofold increase in drug release as compared with pure drug. According to results of in vivo tissue distribution study in Wistar rats, intranasal administration of QTP-loaded nanoemulsion had shorter Tmaxcompared with that of intravenous administration. Higher drug transport efficiency (DTE%) and direct nose-to-brain drug transport (DTP%) was achieved by nanoemulsion. The nanoemulsion system may be a promising strategy for brain-targeted delivery of QTP.
authors.affiliation: Department of Pharmaceutics, Poona College of Pharmacy, Bharati Vidyapeeth Deemed University, Pune, 411038, Maharashtra, India.
authors.forename: Mithila
authors.initials: M
authors.lastname: Boche
authors.affiliation: Department of Pharmaceutics, Poona College of Pharmacy, Bharati Vidyapeeth Deemed University, Pune, 411038, Maharashtra, India. vbpokharkar@yahoo.co.in.
authors.forename: Varsha
authors.initials: V
authors.lastname: Pokharkar
mesh_terms: D000281:Administration, Intranasal; D000818:Animals; D001921:Brain / Q000187:drug effects*; D002626:Chemistry, Pharmaceutical / Q000379:methods; D016503:Drug Delivery Systems / Q000379:methods; D065546:Drug Liberation / Q000187:drug effects; D004655:Emulsions / Q000008:administration & dosage* / Q000737:chemistry* / Q000378:metabolism; D008297:Male; D053758:Nanoparticles / Q000008:administration & dosage* / Q000737:chemistry*; D010316:Particle Size; D011136:Polysorbates / Q000737:chemistry; D000069348:Quetiapine Fumarate / Q000008:administration & dosage* / Q000737:chemistry* / Q000378:metabolism; D051381:Rats; D017208:Rats, Wistar; D012995:Solubility; D013501:Surface-Active Agents / Q000737:chemistry; D014018:Tissue Distribution
chemical_list: D004655:Emulsions; D011136:Polysorbates; D013501:Surface-Active Agents; D000069348:Quetiapine Fumarate
keywords: co-surfactants; surfactants; targeted drug delivery; ternary-phase diagrams