Lipid Nanocarriers Overlaid with Chitosan for Brain Delivery of Berberine via the Nasal Route

Pharmaceuticals

Izzeddin Alsalahat¹  Ibrahim A. Naguib²  Marwa F. Ahmed²  Hadel A. Abo El-Enin³  Hussein M. Eid⁴  Mohammed H. Elkomy⁵  Omar A. Alsaidan⁵  Mohammed M. Ghoneim⁶ 

[1] Complement Biology Group, Systems Immunity Research Institute, School of Medicine, Cardiff University, Cardiff CF14 4XW, UK;Department of Pharmaceutical Chemistry, College of Pharmacy, Taif University, P.O. Box 11099, Taif 21944, Saudi Arabia;Department of Pharmaceutics and Industrial Pharmacy, College of Pharmacy, Taif University, P.O. Box 11099, Taif 21944, Saudi Arabia;Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Beni-Suef University, Beni-Suef 62521, Egypt;Department of Pharmaceutics, College of Pharmacy, Jouf University, P.O. Box 2014, Sakaka 72341, Saudi Arabia;Department of Pharmacy Practice, Faculty of Pharmacy, AlMaarefa University, P.O. Box 71666, Ad Diriyah 13713, Saudi Arabia;

关键词: intranasal;    lipidic nanoparticles;    coatings;    nutraceuticals;    brain targeting;    biodistribution;   

DOI  :  10.3390/ph15030281

来源: DOAJ

【 摘 要 】

This research aimed to design, optimize, and evaluate berberine-laden nanostructured lipid carriers overlaid with chitosan (BER-CTS-NLCs) for efficient brain delivery via the intranasal route. The nanostructured lipid carriers containing berberine (BER-NLCs) were formulated via hot homogenization and ultrasonication strategy and optimized for the influence of a variety of causal variables, including the amount of glycerol monostearate (solid lipid), poloxamer 407 (surfactant) concentration, and oleic acid (liquid lipid) amount, on size of the particles, entrapment, and the total drug release after 24 h. The optimal BER-NLCs formulation was then coated with chitosan. Their diameter, in vitro release, surface charge, morphology, ex vivo permeability, pH, histological, and in vivo (pharmacokinetics and brain uptake) parameters were estimated. BER-CTS-NLCs had a size of 180.9 ± 4.3 nm, sustained-release properties, positive surface charge of 36.8 mV, and augmented ex-vivo permeation via nasal mucosa. The histopathological assessment revealed that the BER-CTS-NLCs system is safe for nasal delivery. Pharmacokinetic and brain accumulation experiments showed that animals treated intranasally with BER-CTS-NLCs had substantially greater drug levels in the brain. The ratios of BER brain/blood levels at 30 min, AUC_brain/AUC_blood, drug transport percentage, and drug targeting efficiency for BER-CTS-NLCs (IN) were higher compared to BER solution (IN), suggesting enhanced brain targeting. The optimized nanoparticulate system is speculated to be a successful approach for boosting the effect of BER in treating CNS diseases, such as Alzheimer’s disease, through intranasal therapy.

【 授权许可】

Unknown