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Pharmaceutics 2018, 10(4), 217; https://doi.org/10.3390/pharmaceutics10040217

A Tailored Thermosensitive PLGA-PEG-PLGA/Emulsomes Composite for Enhanced Oxcarbazepine Brain Delivery via the Nasal Route

1
Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Ain Shams University, Monazzamet Elwehda Elafrikeya Street, Abbaseyya, Cairo 11566, Egypt
2
Department of Pharmaceutical Technology, Faculty of Pharmacy and Biotechnology, German University in Cairo, Al-Tagmoaa Alkhames, Cairo 11835, Egypt
3
School of Pharmacy, University of Camerino, Via S. Agostino 1, 62032 Camerino (MC), Italy
4
IDentity, 19 Cavendish Crescent North, The Park, Nottingham NG7 1BA, UK
5
Department of Biomolecular Sciences, School of Pharmacy, University of Urbino, Piazza del Rinascimento 6, 61029 Urbino (PU), Italy
*
Author to whom correspondence should be addressed.
Received: 10 October 2018 / Revised: 28 October 2018 / Accepted: 1 November 2018 / Published: 5 November 2018
(This article belongs to the Special Issue Transmucosal Absorption Enhancers in the Drug Delivery Field)
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Abstract

The use of nanocarrier delivery systems for direct nose to brain drug delivery shows promise for achieving increased brain drug levels as compared to simple solution systems. An example of such nanocarriers is emulsomes formed from lipid cores surrounded and stabilised by a corona of phospholipids (PC) and a coating of Tween 80, which combines the properties of both liposomes and emulsions. Oxcarbazepine (OX), an antiepileptic drug, was entrapped in emulsomes and then localized in a poly(lactic acid-co-glycolic acid)-poly(ethylene glycol)-poly(lactic acid-co-glycolic acid) (PLGA-PEG-PLGA) triblock copolymer thermogel. The incorporation of OX emulsomes in thermogels retarded drug release and increased its residence time (MRT) in rats. The OX-emulsome and the OX-emulsome-thermogel formulations showed in vitro sustained drug release of 81.1 and 53.5%, respectively, over a period of 24 h. The pharmacokinetic studies in rats showed transport of OX to the systemic circulation after nasal administration with a higher uptake in the brain tissue in case of OX-emulsomes and highest MRT for OX-emulsomal-thermogels as compared to the IN OX-emulsomes, OX-solution and Trileptal® suspension. Histopathological examination of nasal tissues showed a mild vascular congestion and moderate inflammatory changes around congested vessels compared to saline control, but lower toxic effect than that reported in case of the drug solution. View Full-Text
Keywords: nose to brain delivery; antiepileptic drug; drug delivery; block copolymers; thermogel system nose to brain delivery; antiepileptic drug; drug delivery; block copolymers; thermogel system
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This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited (CC BY 4.0).

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El-Zaafarany, G.M.; Soliman, M.E.; Mansour, S.; Cespi, M.; Palmieri, G.F.; Illum, L.; Casettari, L.; Awad, G.A.S. A Tailored Thermosensitive PLGA-PEG-PLGA/Emulsomes Composite for Enhanced Oxcarbazepine Brain Delivery via the Nasal Route. Pharmaceutics 2018, 10, 217.

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