title: Investigating the cubosomal ability for transnasal brain targeting: In vitro optimization, ex vivo permeation and in vivo biodistribution.
abstract: The aim of this study was to enhance the risperidone delivery to the brain through the transnasal route via optimization of cubosomal gel. Cubosomes were prepared using glycerol mono-oleate (GMO), Pluronic F127 (PF127) and Tween 80 (T80). The prepared formulae were characterized by testing their particle size, polydispersity index, zeta potential, entrapment efficiency, in vitro drug release and transmission electron microscopy. Central composite design was planned for the formulae optimization and the selected formula (containing PF127 with concentration 15 mg/g GMO and T80 with concentration of 20mg/L) was re-prepared in presence of gelling polymer (gellan gum or polyox). The optimal cubosomal gel (containing 0.4% w/v polyox) had been subjected to ex-vivo permeation, histopathological evaluation and in vivo biodistribution studies. It showed significantly higher transnasal permeation and better distribution to the brain, when compared to the used control (drug solution and/or suspension). Finally, the cubosomal gel could be considered as a promising carrier for brain targeting of CNS acting drugs through the transnasal route.
authors.affiliation: National Organization for Drug Control and Research (NODCAR), Cairo, Egypt.
authors.forename: Fatma Elzahraa
authors.initials: FE
authors.lastname: Abdelrahman
authors.affiliation: Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Cairo University, Cairo, Egypt; College of Pharmacy, Gulf Medical University, Ajman, United Arab Emirates. Electronic address: ibrahim.elsayed@pharma.cu.edu.eg.
authors.forename: Ibrahim
authors.initials: I
authors.lastname: Elsayed
authors.affiliation: National Organization for Drug Control and Research (NODCAR), Cairo, Egypt.
authors.forename: Mary Kamal
authors.initials: MK
authors.lastname: Gad
authors.affiliation: Egyptian Atomic Energy Authority (EAEA), Cairo, Egypt.
authors.forename: Ahmed
authors.initials: A
authors.lastname: Badr
authors.affiliation: Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Cairo University, Cairo, Egypt.
authors.forename: Magdi Ibrahim
authors.initials: MI
authors.lastname: Mohamed
mesh_terms: D000281:Administration, Intranasal / Q000379:methods; D000818:Animals; D001921:Brain / Q000378:metabolism*; D002626:Chemistry, Pharmaceutical / Q000379:methods; D004337:Drug Carriers / Q000737:chemistry; D016503:Drug Delivery Systems / Q000379:methods; D065546:Drug Liberation; D005782:Gels / Q000737:chemistry; D051379:Mice; D046529:Microscopy, Electron, Transmission / Q000379:methods; D053758:Nanoparticles / Q000008:administration & dosage* / Q000737:chemistry*; D010316:Particle Size; D010539:Permeability; D020442:Poloxamer / Q000737:chemistry; D011108:Polymers / Q000737:chemistry; D018967:Risperidone / Q000008:administration & dosage* / Q000737:chemistry*; D012756:Sheep; D014018:Tissue Distribution
chemical_list: D004337:Drug Carriers; D005782:Gels; D011108:Polymers; D020442:Poloxamer; D018967:Risperidone
keywords: Biodistribution; Cubosomes; Gel; Glyceryl mono-oleate (PubChem CID: 33,022); Permeation; Pluronic; Risperidone; Risperidone (PubChem CID: 5073); Tween