scholarly journals Solid Lipid Nanoparticles for Brain Targeting

2019 ◽  
Vol 9 (6-s) ◽  
pp. 248-252
Author(s):  
Sachin Raosaheb Hangargekar ◽  
Pradeepkumar Mohanty ◽  
Ashish Jain

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

Pharmaceutics ◽  
2020 ◽  
Vol 13 (1) ◽  
pp. 38
Author(s):  
Gizem Rüya Topal ◽  
Mária Mészáros ◽  
Gergő Porkoláb ◽  
Anikó Szecskó ◽  
Tamás Ferenc Polgár ◽  
...  

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.


2018 ◽  
Vol 161 ◽  
pp. 302-313 ◽  
Author(s):  
Giulia Graverini ◽  
Vieri Piazzini ◽  
Elisa Landucci ◽  
Daniela Pantano ◽  
Pamela Nardiello ◽  
...  

2021 ◽  
Vol 14 (2) ◽  
pp. 126-142
Author(s):  
Anil K. Pawar ◽  
Laxman G. Hatmode ◽  
Harshada R. Khandelwal ◽  
Vishal C. Gurumukhi ◽  
Shailesh S. Chalikwar

Background: Solid lipid nanoparticles (SLN) have drawn increasing interest in recent years. These nanoparticles are formed from stable or solid lipid mixtures and then stabilized by emulsifiers. As nanoparticles, colloidal particles running in size somewhere in the 10 to 1000 nm range are known. SLN provides fascinating properties, such as minimal scale, massive surface area, high medication piling, correspondence of stages at the interface, and is interested in their ability to enhance drug execution. Main text: This paper provides a description of the choice of ingredients, the effect of lipids and their structure on the formulation, and the various methods of processing SLN. We explain the characteristics of SLN stability and the possibilities of SLN stabilization by lyophilization in this article. The relation between drug absorption and the complexity of SLN dispersions, which involves the existence of other colloidal structures and the physical state of the lipid, is uncommonly considered. We define the possible problems of SLN preparation and performance on the basis of characterization. First, the nasal route was known to accomplish the avoidance of first-pass hepatic metabolism in order to maximize absolute bioavailability, and secondly, the immediate nose-to-brain pathway to enhance the delivery of brain medicines. SLNs have been designated to increase drug permeability through the blood-brain barrier as a drug delivery device (BBB). Conclusion: To sum up, this article gives insight SLNs a colloidal drug carrier places together the compensations of polymeric nanoparticles, SLNs have numerous benefits such as easy incorporation of lipid and lipophilic as well as hydrophilic drugs, suitable physical stability, and available at low cost and easy to manufacture. The nasal route was accepted to exploit first its prevention of the hepatic first-pass metabolism to increase the absolute bioavailability, and second, the direct nose-to-brain pathway to enhance the brain drug delivery. SLNs were chosen as a drug delivery system to improve drug permeability across the blood-brain barrier (BBB) and consequently its brain delivery.


2017 ◽  
Vol 249 ◽  
pp. 103-110 ◽  
Author(s):  
R. Dal Magro ◽  
F. Ornaghi ◽  
I. Cambianica ◽  
S. Beretta ◽  
F. Re ◽  
...  

Pharmaceutics ◽  
2019 ◽  
Vol 11 (2) ◽  
pp. 65 ◽  
Author(s):  
Elisabetta Muntoni ◽  
Katia Martina ◽  
Elisabetta Marini ◽  
Marta Giorgis ◽  
Loretta Lazzarato ◽  
...  

Glioblastoma is the most common and invasive primary tumor of the central nervous system and normally has a negative prognosis. Biodistribution in healthy animal models is an important preliminary study aimed at investigating the efficacy of chemotherapy, as it is mainly addressed towards residual cells after surgery in a region with an intact blood–brain barrier. Nanoparticles have emerged as versatile vectors that can overcome the blood–brain barrier. In this experimental work, solid lipid nanoparticles, prepared using fatty acid coacervation, have been loaded with an active lipophilic ester of cytotoxic drug methotrexate, and functionalized with either transferrin or insulin, two proteins whose receptors are abundantly expressed on the blood–brain barrier. Functionalization has been achieved by grafting a maleimide moiety onto the nanoparticle’s surface and exploiting its reactivity towards thiolated proteins. The nanoparticles have been tested in vitro on a blood–brain barrier cellular model and in vivo for biodistribution in Wistar rats. Drug metabolites, in particular 7-hydroxymethotrexate, have also been investigated in the animal model. The data obtained indicate that the functionalization of the nanoparticles improved their ability to overcome the blood–brain barrier when a PEG spacer between the proteins and the nanoparticle’s surface was used. This is probably because this method provided improved ligand–receptor interactions and selectivity for the target tissue.


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