A Tailored Thermosensitive PLGA-PEG-PLGA/Emulsomes Composite for Enhanced Oxcarbazepine Brain Delivery via the Nasal Route
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 (...
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| Format: | Article |
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MDPI AG
2018-11-01
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| Series: | Pharmaceutics |
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| Online Access: | https://www.mdpi.com/1999-4923/10/4/217 |
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| author | Ghada M. El-Zaafarany Mahmoud E. Soliman Samar Mansour Marco Cespi Giovanni Filippo Palmieri Lisbeth Illum Luca Casettari Gehanne A. S. Awad |
| author_facet | Ghada M. El-Zaafarany Mahmoud E. Soliman Samar Mansour Marco Cespi Giovanni Filippo Palmieri Lisbeth Illum Luca Casettari Gehanne A. S. Awad |
| author_sort | Ghada M. El-Zaafarany |
| collection | DOAJ |
| description | 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-<i>co</i>-glycolic acid)-poly(ethylene glycol)-poly(lactic acid-<i>co</i>-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<sup>®</sup> 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. |
| first_indexed | 2024-04-14T00:32:51Z |
| format | Article |
| id | doaj.art-239de7b5c5024a6d93bf19be5e5d5c35 |
| institution | Directory Open Access Journal |
| issn | 1999-4923 |
| language | English |
| last_indexed | 2024-04-14T00:32:51Z |
| publishDate | 2018-11-01 |
| publisher | MDPI AG |
| record_format | Article |
| series | Pharmaceutics |
| spelling | doaj.art-239de7b5c5024a6d93bf19be5e5d5c352022-12-22T02:22:29ZengMDPI AGPharmaceutics1999-49232018-11-0110421710.3390/pharmaceutics10040217pharmaceutics10040217A Tailored Thermosensitive PLGA-PEG-PLGA/Emulsomes Composite for Enhanced Oxcarbazepine Brain Delivery via the Nasal RouteGhada M. El-Zaafarany0Mahmoud E. Soliman1Samar Mansour2Marco Cespi3Giovanni Filippo Palmieri4Lisbeth Illum5Luca Casettari6Gehanne A. S. Awad7Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Ain Shams University, Monazzamet Elwehda Elafrikeya Street, Abbaseyya, Cairo 11566, EgyptDepartment of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Ain Shams University, Monazzamet Elwehda Elafrikeya Street, Abbaseyya, Cairo 11566, EgyptDepartment of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Ain Shams University, Monazzamet Elwehda Elafrikeya Street, Abbaseyya, Cairo 11566, EgyptSchool of Pharmacy, University of Camerino, Via S. Agostino 1, 62032 Camerino (MC), ItalySchool of Pharmacy, University of Camerino, Via S. Agostino 1, 62032 Camerino (MC), ItalyIDentity, 19 Cavendish Crescent North, The Park, Nottingham NG7 1BA, UKDepartment of Biomolecular Sciences, School of Pharmacy, University of Urbino, Piazza del Rinascimento 6, 61029 Urbino (PU), ItalyDepartment of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Ain Shams University, Monazzamet Elwehda Elafrikeya Street, Abbaseyya, Cairo 11566, EgyptThe 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-<i>co</i>-glycolic acid)-poly(ethylene glycol)-poly(lactic acid-<i>co</i>-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<sup>®</sup> 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.https://www.mdpi.com/1999-4923/10/4/217nose to brain deliveryantiepileptic drugdrug deliveryblock copolymersthermogel system |
| spellingShingle | Ghada M. El-Zaafarany Mahmoud E. Soliman Samar Mansour Marco Cespi Giovanni Filippo Palmieri Lisbeth Illum Luca Casettari Gehanne A. S. Awad A Tailored Thermosensitive PLGA-PEG-PLGA/Emulsomes Composite for Enhanced Oxcarbazepine Brain Delivery via the Nasal Route Pharmaceutics nose to brain delivery antiepileptic drug drug delivery block copolymers thermogel system |
| title | A Tailored Thermosensitive PLGA-PEG-PLGA/Emulsomes Composite for Enhanced Oxcarbazepine Brain Delivery via the Nasal Route |
| title_full | A Tailored Thermosensitive PLGA-PEG-PLGA/Emulsomes Composite for Enhanced Oxcarbazepine Brain Delivery via the Nasal Route |
| title_fullStr | A Tailored Thermosensitive PLGA-PEG-PLGA/Emulsomes Composite for Enhanced Oxcarbazepine Brain Delivery via the Nasal Route |
| title_full_unstemmed | A Tailored Thermosensitive PLGA-PEG-PLGA/Emulsomes Composite for Enhanced Oxcarbazepine Brain Delivery via the Nasal Route |
| title_short | A Tailored Thermosensitive PLGA-PEG-PLGA/Emulsomes Composite for Enhanced Oxcarbazepine Brain Delivery via the Nasal Route |
| title_sort | tailored thermosensitive plga peg plga emulsomes composite for enhanced oxcarbazepine brain delivery via the nasal route |
| topic | nose to brain delivery antiepileptic drug drug delivery block copolymers thermogel system |
| url | https://www.mdpi.com/1999-4923/10/4/217 |
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