Mohammad Amin Raeisi Estabragh
1,2 
, Abbas Pardakhty
1* , Saeid Ahmadzadeh
3, Shahriar Dabiri
4, Reza Malekpour Afshar
4, Mohammad Farajli Abbasi
5* 1 Pharmaceutics Research Center, Institute of Neuropharmacology, Kerman University of Medical Sciences, Kerman, Iran.
2 Student Research Committee, Kerman University of Medical Sciences, Kerman, Iran.
3 Pharmaceutical Sciences and Cosmetic Products Research Center, Kerman University of Medical Sciences, Kerman, Iran.
4 Pathology and Stem Cell Research Center, Afzalipour Faculty of Medicine, Kerman University of Medical Sciences, Kerman, Iran.
5 Neuroscience Research Center, Institute of Neuropharmacology, Kerman University of Medical Sciences, Kerman, Iran.
*Corresponding Authors: Mohammad Farajli Abbasi and Abbas Pardakhty, Emails: m.fabbasi@kmu.ac.ir and abpardakhty@kmu.ac.ir, Email:
drpardakhti@yahoo.com; Mohammad Farajli Abbasi and Abbas Pardakhty, Emails: m.fabbasi@kmu.ac.ir and abpardakhty@kmu.ac.ir, Email:
mohammad.f.abbasi@gmail.com
Abstract
Purpose: Free radicals such as hydroxyl and peroxide are contributing factors to neuronaldestruction in cerebral ischemia. Alpha-lipoic acid (ALA) is one of the potent knownantioxidants. Preparation of ALA niosomes allows IV injection and can increase bioavailabilityand penetration into the central nervous system (CNS).Methods: Film hydration method was used to prepare different niosomes composed of Span®,Tween®, and cholesterol at different molar ratio. ALA and niosome-forming compounds weredissolved in chloroform, before removing the organic solvent by rotary evaporator. Animalswere randomly divided into four groups: Sham, control group, intravenous (IV) injection ofempty niosomes plus intraperitoneal (IP) injection of ALA solution, and finally, IV injectionof ALA niosomes. Rats were subjected to deep anesthesia before inducing cerebral ischemia,then, their internal common carotid arteries were clamped for 15 min and reperfusion wasdone for 30 min. Niosomal ALA was injected intravenously just before declamping.Results: Mean volume diameter of the prepared niosomes was between 4.36 ± 0.82 and 19.95± 1.21 μm in different formulations. Encapsulation efficiency percent (EE%) of ALA in theselected formulation, Span60/Tween60/cholesterol (35:35:30 molar ratio), was 94.5 ± 0.2, and59.27 ± 5.61% of ALA was released after 4h. In the niosomal group, the rate of reduction incomplications of cerebral ischemia such as histopathologic changes and acute damage (fromscore 3 to 1) in CNS was higher than other groups.Conclusion: The obtained results show that niosomes can be used as effective drug deliverysystems for ALA in cerebral ischemia.