Application of Nanopharmaceutics for Flibanserin Brain Delivery Augmentation Via the Nasal Route

Overview

Journal Nanomaterials (Basel)

Date 2020 Jul 3

PMID 32610539

Citations 2

Authors

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

Affiliations

Soon will be listed here.

Abstract

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.

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