Formulation and Therapeutic Evaluation of Isoxsuprine-Loaded Nanoparticles against Diabetes-Associated Stroke

Ischemic stroke is the second-leading cause of death. Hyperglycemia, which is characteristic of diabetes mellitus, contributes to the development of endothelial dysfunction and increases the risk of stroke. Isoxsuprine is an efficient beta-adrenergic agonist that improves blood flow to the ischemic...

Full description

Saved in:
Bibliographic Details
Published in:Pharmaceutics 2023-08, Vol.15 (9), p.2242
Main Authors: Abou-Taleb, Heba A, Aldosari, Basmah Nasser, Zaki, Randa Mohammed, Afzal, Obaid, Tulbah, Alaa S, Shahataa, Mary Girgis, Abo El-Ela, Fatma I, Salem, Heba F, Fouad, Amr Gamal
Format: Article
Language:English
Subjects:
Analysis
Bioavailability
Cholesterol
Diabetes
diabetes mellitus
Diabetics
Drug dosages
Efficiency
Ethanol
Evaluation
Health aspects
Ischemia
isoxsuprine
liposomes
Metabolism
Mortality
Nanoparticles
Patient compliance
Physiological aspects
Propylene
propylene glycol
Stroke
Variance analysis
Viscosity
Citations: Items that this one cites
Items that cite this one
Online Access:Get full text
Tags: Add Tag
No Tags, Be the first to tag this record!
Description
Summary:Ischemic stroke is the second-leading cause of death. Hyperglycemia, which is characteristic of diabetes mellitus, contributes to the development of endothelial dysfunction and increases the risk of stroke. Isoxsuprine is an efficient beta-adrenergic agonist that improves blood flow to the ischemic aria and stops the infarct core from growing. However, low bioavailability, a short biological half-life, and first-pass hepatic metabolism reduce the therapeutic efficacy of oral isoxsuprine. Therefore, the authors focused on developing isoxsuprine-loaded liposomes containing ethanol and propylene glycol (ILEP) formulation as nasal drops for the treatment of ischemic stroke in diabetic patients. Different ILEP formulations were optimized using Design Expert software, and the selected formulation was examined in vivo for its anti-stroke effect using a rat model of diabetes and stroke. The optimized ILEP, composed of 15% propylene glycol, 0.16% cholesterol, 10% ethanol, and 3.29% phospholipid, improved the sustainability, permeation, and targeting of isoxsuprine. Furthermore, the in vivo studies verified the improved neurological behavior and decreased dead shrunken neurons and vascular congestion of the rats treated with the optimized ILEP formulation, demonstrating its anti-stroke activity. In conclusion, our study found that treatment with an optimized ILEP formulation prevented the initiation and severity of stroke, especially in diabetic patients.
ISSN:1999-4923
1999-4923
DOI:10.3390/pharmaceutics15092242