Application of Nanopharmaceutics for Flibanserin Brain Delivery Augmentation Via the Nasal Route
Flibanserin (FLB) is a nonhormonal medicine approved by the Food and Drug Administration (FDA) to treat the hypoactive sexual appetite disorder in females. However, the peroral administration of the medicine is greatly affected by its poor bioavailability as a result of its extensive first-pass effe...
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doaj-077f3c81644140c9a73e947d7caf9c3d2020-11-25T03:54:32ZengMDPI AGNanomaterials2079-49912020-06-01101270127010.3390/nano10071270Application of Nanopharmaceutics for Flibanserin Brain Delivery Augmentation Via the Nasal RouteOsama A. A. Ahmed0Usama A. Fahmy1Shaimaa M. Badr-Eldin2Hibah M. Aldawsari3Zuhier A. Awan4Hani Z. Asfour5Ahmed K. Kammoun6Giuseppe Caruso7Filippo Caraci8Anas Alfarsi9Raniyah A. Al-Ghamdi10Rawan A. Al-Ghamdi11Nabil A. Alhakamy12Department of Pharmaceutics, Faculty of Pharmacy, King Abdulaziz University, Jeddah 21589, Saudi ArabiaDepartment of Pharmaceutics, Faculty of Pharmacy, King Abdulaziz University, Jeddah 21589, Saudi ArabiaDepartment of Pharmaceutics, Faculty of Pharmacy, King Abdulaziz University, Jeddah 21589, Saudi ArabiaDepartment of Pharmaceutics, Faculty of Pharmacy, King Abdulaziz University, Jeddah 21589, Saudi ArabiaDepartment of Clinical Biochemistry, Faculty of Medicine, King Abdulaziz University, Jeddah 21589, Saudi ArabiaDepartment of Medical Microbiology and Parasitology, Faculty of Medicine, King Abdulaziz University. Jeddah 21589, Saudi ArabiaDepartment of Pharmaceutical Chemistry, Faculty of Pharmacy, King Abdulaziz University, Jeddah 21589, Saudi ArabiaOasi Research Institute - IRCCS, Via Conte Ruggero, 73, 94018 Troina (EN), ItalyOasi Research Institute - IRCCS, Via Conte Ruggero, 73, 94018 Troina (EN), ItalyDepartment of Pharmaceutics, Faculty of Pharmacy, King Abdulaziz University, Jeddah 21589, Saudi ArabiaIbn Sina National College for Medical Studies, Clinical Pharmacy Department, Jeddah 22421, Saudi ArabiaIbn Sina National College for Medical Studies, Jeddah 22421, Saudi ArabiaDepartment of Pharmaceutics, Faculty of Pharmacy, King Abdulaziz University, Jeddah 21589, Saudi ArabiaFlibanserin (FLB) is a nonhormonal medicine approved by the Food and Drug Administration (FDA) to treat the hypoactive sexual appetite disorder in females. However, the peroral administration of the medicine is greatly affected by its poor bioavailability as a result of its extensive first-pass effect and poor solubility. Aiming at circumventing these drawbacks, this work involves the formulation of optimized FLB transfersome (TRF) loaded intranasal hydrogel. Box–Behnken design was utilized for the improvement of FLB TRFs with decreased size. The FLB-to-phospholipid molar ratio, the edge activator hydrophilic lipophilic balance, and the pH of the hydration medium all exhibited significant effects on the TRF size. The optimized/developed TRFs were unilamellar in shape. Hydroxypropyl methyl cellulose based hydrogel filled with the optimized FLB TRFs exhibited an improved ex vivo permeation when compared with the control FLB-loaded hydrogel. In addition, the optimized TRF-loaded hydrogel exhibited higher bioavailability and enhanced brain delivery relative to the control hydrogel following intranasal administration in Wistar rats. The results foreshadow the possible potential application of the proposed intranasal optimized FLB-TRF-loaded hydrogel to increase the bioavailability and nose-to-brain delivery of the drug.https://www.mdpi.com/2079-4991/10/7/1270flibanserintransfersomeshydrogelex vivo permeationin vivo pharmacokinetics |
collection |
DOAJ |
language |
English |
format |
Article |
sources |
DOAJ |
author |
Osama A. A. Ahmed Usama A. Fahmy Shaimaa M. Badr-Eldin Hibah M. Aldawsari Zuhier A. Awan Hani Z. Asfour Ahmed K. Kammoun Giuseppe Caruso Filippo Caraci Anas Alfarsi Raniyah A. Al-Ghamdi Rawan A. Al-Ghamdi Nabil A. Alhakamy |
spellingShingle |
Osama A. A. Ahmed Usama A. Fahmy Shaimaa M. Badr-Eldin Hibah M. Aldawsari Zuhier A. Awan Hani Z. Asfour Ahmed K. Kammoun Giuseppe Caruso Filippo Caraci Anas Alfarsi Raniyah A. Al-Ghamdi Rawan A. Al-Ghamdi Nabil A. Alhakamy Application of Nanopharmaceutics for Flibanserin Brain Delivery Augmentation Via the Nasal Route Nanomaterials flibanserin transfersomes hydrogel ex vivo permeation in vivo pharmacokinetics |
author_facet |
Osama A. A. Ahmed Usama A. Fahmy Shaimaa M. Badr-Eldin Hibah M. Aldawsari Zuhier A. Awan Hani Z. Asfour Ahmed K. Kammoun Giuseppe Caruso Filippo Caraci Anas Alfarsi Raniyah A. Al-Ghamdi Rawan A. Al-Ghamdi Nabil A. Alhakamy |
author_sort |
Osama A. A. Ahmed |
title |
Application of Nanopharmaceutics for Flibanserin Brain Delivery Augmentation Via the Nasal Route |
title_short |
Application of Nanopharmaceutics for Flibanserin Brain Delivery Augmentation Via the Nasal Route |
title_full |
Application of Nanopharmaceutics for Flibanserin Brain Delivery Augmentation Via the Nasal Route |
title_fullStr |
Application of Nanopharmaceutics for Flibanserin Brain Delivery Augmentation Via the Nasal Route |
title_full_unstemmed |
Application of Nanopharmaceutics for Flibanserin Brain Delivery Augmentation Via the Nasal Route |
title_sort |
application of nanopharmaceutics for flibanserin brain delivery augmentation via the nasal route |
publisher |
MDPI AG |
series |
Nanomaterials |
issn |
2079-4991 |
publishDate |
2020-06-01 |
description |
Flibanserin (FLB) is a nonhormonal medicine approved by the Food and Drug Administration (FDA) to treat the hypoactive sexual appetite disorder in females. However, the peroral administration of the medicine is greatly affected by its poor bioavailability as a result of its extensive first-pass effect and poor solubility. Aiming at circumventing these drawbacks, this work involves the formulation of optimized FLB transfersome (TRF) loaded intranasal hydrogel. Box–Behnken design was utilized for the improvement of FLB TRFs with decreased size. The FLB-to-phospholipid molar ratio, the edge activator hydrophilic lipophilic balance, and the pH of the hydration medium all exhibited significant effects on the TRF size. The optimized/developed TRFs were unilamellar in shape. Hydroxypropyl methyl cellulose based hydrogel filled with the optimized FLB TRFs exhibited an improved ex vivo permeation when compared with the control FLB-loaded hydrogel. In addition, the optimized TRF-loaded hydrogel exhibited higher bioavailability and enhanced brain delivery relative to the control hydrogel following intranasal administration in Wistar rats. The results foreshadow the possible potential application of the proposed intranasal optimized FLB-TRF-loaded hydrogel to increase the bioavailability and nose-to-brain delivery of the drug. |
topic |
flibanserin transfersomes hydrogel ex vivo permeation in vivo pharmacokinetics |
url |
https://www.mdpi.com/2079-4991/10/7/1270 |
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