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.
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Pharmacokinetic studies in rats showed that oxcarbazepine-loaded emulsomes slowed drug elimination and achieved a high drug concentration in the blood stream for longer time periods compared to free drug administrations.
“Pharmacokinetic studies carried out in rats showed that oxcarbazepine-loaded emulsomes slowed drug elimination, and a high drug concentration was achieved in the blood stream for a longer time periods, as compared to the free drug administrations.”
From Nanoemulsions for “Nose-to-Brain” Drug Delivery (2019) · cites this paper as [79]
Ex vivo studies using rat nasal mucosa showed no histopathological alteration induced by oxcarbazepine emulsomes.
“Ex vivo studies carried out using rat nasal mucosa to check possible changes induced by emulsomes showed no histopathological alteration.”
From Nanoemulsions for “Nose-to-Brain” Drug Delivery (2019) · cites this paper as [79]
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- Authors
- El-Zaafarany, G. M., Soliman, M. E., Mansour, S., & Awad, G. A. S.
- Affiliations
- Ain Shams University (EG)
- Corresponding author
- El-Zaafarany, Ghada M.
- Venue
- International Journal of Pharmaceutics
- Publisher
- Elsevier BV
- Published
- 2016-04
- Volume
- 503
- Issue
- 1-2
- Pages
- 127-140
- ISSN
- 0378-5173 (ISSN-L)
- OpenAlex
- W2288911386
- Cited by
- 89
- References
- 72
- Citations by year
- 2026: 5 · 2025: 10 · 2024: 15 · 2023: 11 · 2022: 18 · 2021: 11 · 2020: 6 · 2019: 5 · 2018: 5 · 2017: 3
- FWCI
- 2.48
- Type
- journal article
- Language
- en
- Open access
- closed
- Locations
- International Journal of Pharmaceutics (publishedVersion)
- PubMed (publishedVersion)
- Topics
- Life Sciences › Pharmacology, Toxicology and Pharmaceutics › Pharmaceutical Science › Advanced Drug Delivery Systems
- Physical Sciences › Materials Science › Biomaterials › Nanoparticle-Based Drug Delivery
- Life Sciences › Pharmacology, Toxicology and Pharmaceutics › Pharmaceutical Science › Advancements in Transdermal Drug Delivery
- Keywords
- emulsomes, oxcarbazepine, brain targeting, intranasal drug delivery, nose-to-brain transport, lipid-based nanocarriers, phosphatidylcholine, Compritol, triolein, encapsulation efficiency, sustained drug release, cytotoxicity, pharmacokinetics, nanocarrier stability
- MeSH terms
- Oxcarbazepine, Administration, Intranasal, Animals, Anticonvulsants, Brain, Carbamazepine, Cell Survival, Drug Carriers, Humans, Lipids, Male, Nasal Mucosa, Particle Size, Surface Properties, Rats, Wistar, Cell Line, Tumor, Nanoparticles, Drug Liberation
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