title: Identifying lipidic emulsomes for improved oxcarbazepine brain targeting: In vitro and rat in vivo studies.
abstract: Lipid-based nanovectors offer effective carriers for brain delivery by improving drug potency and reducing off-target effects. Emulsomes are nano-triglyceride (TG) carriers formed of lipid cores supported by at least one phospholipid (PC) sheath. Due to their surface active properties, PC forms bilayers at the aqueous interface, thereby enabling encapsulated drug to benefit from better bioavailability and stability. Emulsomes of oxcarbazepine (OX) were prepared, aimed to offer nanocarriers for nasal delivery for brain targeting. Different TG cores (Compritol(®), tripalmitin, tristearin and triolein) and soya phosphatidylcholine in different amounts and ratios were used for emulsomal preparation. Particles were modulated to generate nanocarriers with suitable size, charge, encapsulation efficiency and prolonged release. Cytotoxicity and pharmacokinetic studies were also implemented. Nano-spherical OX-emulsomes with maximal encapsulation of 96.75% were generated. Stability studies showed changes within 30.6% and 11.2% in the size and EE% after 3 months. MTT assay proved a decrease in drug toxicity by its encapsulation in emulsomes. Incorporation of OX into emulsomes resulted in stable nanoformulations. Tailoring emulsomes properties by modulating the surface charge and particle size produced a stable system for the lipophilic drug with a prolonged release profile and mean residence time and proved direct nose-to-brain transport in rats.
authors.affiliation: Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Ain Shams University, Monazzamet Elwehda Elafrikeya Street, P.O.B. 11566, Abbaseyya, Cairo, Egypt. Electronic address: Ghada@pharma.asu.edu.eg.
authors.forename: Ghada M
authors.initials: GM
authors.lastname: El-Zaafarany
authors.affiliation: Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Ain Shams University, Monazzamet Elwehda Elafrikeya Street, P.O.B. 11566, Abbaseyya, Cairo, Egypt. Electronic address: mahmoud.e.soliman@pharma.asu.edu.eg.
authors.forename: Mahmoud E
authors.initials: ME
authors.lastname: Soliman
authors.affiliation: Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Ain Shams University, Monazzamet Elwehda Elafrikeya Street, P.O.B. 11566, Abbaseyya, Cairo, Egypt. Electronic address: samar.mansour@guc.edu.eg.
authors.forename: Samar
authors.initials: S
authors.lastname: Mansour
authors.affiliation: Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Ain Shams University, Monazzamet Elwehda Elafrikeya Street, P.O.B. 11566, Abbaseyya, Cairo, Egypt. Electronic address: gawad@pharma.asu.edu.eg.
authors.forename: Gehanne A S
authors.initials: GA
authors.lastname: Awad
mesh_terms: D000281:Administration, Intranasal; D000818:Animals; D000927:Anticonvulsants / Q000008:administration & dosage* / Q000097:blood / Q000737:chemistry / Q000493:pharmacokinetics; D001921:Brain / Q000378:metabolism*; D002220:Carbamazepine / Q000008:administration & dosage / Q000031:analogs & derivatives* / Q000097:blood / Q000737:chemistry / Q000493:pharmacokinetics; D045744:Cell Line, Tumor; D002470:Cell Survival / Q000187:drug effects; D004337:Drug Carriers / Q000008:administration & dosage* / Q000737:chemistry / Q000493:pharmacokinetics; D065546:Drug Liberation; D006801:Humans; D008055:Lipids / Q000737:chemistry*; D008297:Male; D053758:Nanoparticles / Q000008:administration & dosage* / Q000737:chemistry; D009297:Nasal Mucosa; D000078330:Oxcarbazepine; D010316:Particle Size; D017208:Rats, Wistar; D013499:Surface Properties
chemical_list: D000927:Anticonvulsants; D004337:Drug Carriers; D008055:Lipids; D002220:Carbamazepine; D000078330:Oxcarbazepine
keywords: Direct nose-to-brain delivery; Drug targeting efficiency; Emulsomes; Intranasal; Oxcarbazepine