title: Formulation, characterization and pharmacokinetics of Morin hydrate niosomes prepared from various non-ionic surfactants.
abstract: Morin hydrate (MH), a bioflavonoid with antioxidant and anticancer activity as well as the ability to improve the bioavailability of other drugs on their concurrent use. Three differently optimized niosomal formulations using three different non-ionic surfactants (Span 60, Span 80 and Tween 60) were achieved by (L9 (3(4))) Taguchi orthogonal array (TOA). The analysis of TOA revealed that Tween 60 Niosomes had the highest entrapment efficiency (93.4%) compared to other optimized Niosomal formulations (71-79%). In terms of MH remaining %, Tween 60 Niosomes were found to be the most stable (89%) at 4 °C over one month compared to Span 60 (56%) and Span 80 (57%) Niosomes. The release pattern in all Niosomal formulations was found to follow the Weibull model and Tween 60 Niosomes had the highest release rate. The molecular modeling simulation explained the binding of MH to the human serum albumin (HSA) by hydrogen bonds during the in vitro release process. As for the bioavailability, the AUC0-8 showed 1.3-2.7 fold increase compared to the MH solution. Ex vivo images of the excised organs showed that MH could accumulate in brain which indicates that MH-Tween 60 Niosomes might be a possible candidate to deliver hydrophobic drugs and overcome the blood-brain barrier (BBB) penetration.
authors.affiliation: Department of Pharmaceutics, China Pharmaceutical University, 24 Tongjiaxiang, Nanjing 210009, China; Department of Pharmaceutics, Faculty of Pharmacy, University of Gezira, Wad Medani P.O. Box 20, Sudan. Electronic address: aymanwaddad@hotmail.com.
authors.forename: Ayman Y
authors.initials: AY
authors.lastname: Waddad
authors.forename: Sarra
authors.initials: S
authors.lastname: Abbad
authors.forename: Fan
authors.initials: F
authors.lastname: Yu
authors.forename: Were L L
authors.initials: WL
authors.lastname: Munyendo
authors.forename: Jing
authors.initials: J
authors.lastname: Wang
authors.forename: Huixia
authors.initials: H
authors.lastname: Lv
authors.forename: Jianping
authors.initials: J
authors.lastname: Zhou
mesh_terms: D000818:Animals; D002626:Chemistry, Pharmaceutical / Q000379:methods*; D005419:Flavonoids / Q000138:chemical synthesis* / Q000493:pharmacokinetics*; D008081:Liposomes; D008297:Male; D051379:Mice; D008807:Mice, Inbred BALB C; D011897:Random Allocation; D051381:Rats; D017208:Rats, Wistar; D013501:Surface-Active Agents / Q000138:chemical synthesis* / Q000493:pharmacokinetics*; D047309:Flavones
chemical_list: D005419:Flavonoids; D008081:Liposomes; D013501:Surface-Active Agents; C008548:morin; D047309:Flavones
keywords: Drug delivery; Molecular modeling; Morin hydrate; Niosomes; Orthogonal array; Pharmacokinetics