Intranasally administered melatonin core-shell polymeric nanocapsules: A promising treatment modality for cerebral ischemia.

Autor: Bseiso EA; Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, October 6 University, Giza Governorate, Egypt., Abd El-Aal SA; Department of Pharmacy, Kut University College, Al Kut, Wasit 52001, Iraq., Nasr M; Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Ain-Shams University, Cairo, Egypt. Electronic address: drmahanasr@pharma.asu.edu.eg., Sammour OA; Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Ain-Shams University, Cairo, Egypt., Abd El Gawad NA; Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, October 6 University, Giza Governorate, Egypt; Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Cairo University, Egypt.
Jazyk: angličtina
Zdroj: Life sciences [Life Sci] 2022 Oct 01; Vol. 306, pp. 120797. Date of Electronic Publication: 2022 Jul 14.
DOI: 10.1016/j.lfs.2022.120797
Abstrakt: Aims: The neurohormone melatonin (MEL) has been reported as a promising neuroprotective molecule, however it suffers pharmaceutical limitations such as poor solubility and low bioavailability, which hinder its pharmacological and clinical potential. In the current work, MEL was loaded in core-shell nanocarrier system; polymeric nanocapsules (PNCs), and assessed for its potential in cerebral ischemia reperfusion injury rat model when administered intranasally.
Key Findings: Adopting a D-optimal factorial design, MEL-PNCs were successfully formulated using the nanoprecipitation technique. MEL-PNCs exhibited a particle size ranging from 143.5 to 444 nm, negative zeta potential values ranging from -24.2 to -38.7 mV, cumulative release % for MEL ranging from 36.79 to 41.31 % over 8 h period, with overall good storage properties. The selected MEL-PNCs formulation displayed 8-fold higher permeation than the drug solution across sheep nasal mucosa. MEL-PNCs administered intranasally decreased oxidative stress and hippocampal inflammation, and the histological examination revealed the significant restoration of hippocampal neurons.
Significance: MEL-PNCs administered intranasally could be a promising treatment modality in brain ischemia.
(Copyright © 2022 Elsevier Inc. All rights reserved.)
Databáze: MEDLINE
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