Solid lipid nanoparticles as a drug delivery system to across the blood-brain barrier

Pharmacological treatment of central nervous system (CNS) disorders is difficult, because the blood–brain barrier (BBB) restricts the penetration of many drugs into the brain. To solve this unmet therapeutic need, nanosized drug carriers are the focus of research efforts to develop drug delivery systems for the CNS. For the successful delivery of nanoparticles (NPs) to the brain, targeting ligands on their surface is necessary. Our research aim was to design a nanoscale drug delivery system for a more efficient transfer of donepezil, an anticholinergic drug in the therapy of Alzheimer’s disease across the BBB. Rhodamine B-labeled solid lipid nanoparticles with donepezil cargo were prepared and targeted with apolipoprotein E (ApoE), a ligand of BBB receptors. Nanoparticles were characterized by measurement of size, polydispersity index, zeta potential, thermal analysis, Fourier-transform infrared spectroscopy, in vitro release, and stability. Cytotoxicity of nanoparticles were investigated by metabolic assay and impedance-based cell analysis. ApoE-targeting increased the uptake of lipid nanoparticles in cultured brain endothelial cells and neurons. Furthermore, the permeability of ApoE-targeted nanoparticles across a co-culture model of the BBB was also elevated. Our data indicate that ApoE, which binds BBB receptors, can potentially be exploited for successful CNS targeting of solid lipid nanoparticles.

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Solid Lipid Nanoparticles for Brain Targeting

Journal of Drug Delivery and Therapeutics ◽

10.22270/jddt.v9i6-s.3783 ◽

2019 ◽

Vol 9 (6-s) ◽

pp. 248-252

Author(s):

Sachin Raosaheb Hangargekar ◽

Pradeepkumar Mohanty ◽

Ashish Jain

Keyword(s):

Drug Delivery ◽

Blood Brain Barrier ◽

Solid Lipid Nanoparticles ◽

Drug Loading ◽

Specific Area ◽

Lipid Nanoparticles ◽

Brain Barrier ◽

Brain Targeting ◽

Solid Lipid ◽

Blood Brain

Brain is considered to be highly impermeable barrier, possessing different obstacles like presence of enzymes, presence of tight junctions that limit the entry for most of the drugs. The presence of these obstacles, possess a challenge for administration of the drugs. The conventional means of drug delivery in form of emulsions, fail to overcome these obstacles, and hence there is a need for newer drug delivery approach, that will cross these barriers of the brain. So, these nanoparticles can be an alternative to other conventional systems. They offer several advantages such as improved bioavailability and solubility that are composed of macromolecular materials like lipids and polymers possess low cytotoxicity, high drug loading capability, and good scalability these are the most effective colloidal carriers that have the ability to incorporate drugs into nanocarriers and used as drug targeting to specific area. Thus, this article will emphasise on properties of Blood Brain Barrier, strategies to overcome the blood–brain barrier, literature regarding the use of SLNs in various neurological disease states, production methods of SLN and its evaluation. Hence, these solid lipid formulations can be a new form and one of the promising approach for drug delivery system in future, that have remarkable possibility to cross the BBB. Keywords: Solid lipid nanoparticles, Nanocarriers, Blood–brain barrier

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