Solid Lipid Nanoparticles (SLNs): An Advanced Drug Delivery System Targeting Brain through BBB

The blood–brain barrier (BBB) plays a vital role in the protection and maintenance of homeostasis in the brain. In this way, it is an interesting target as an interface for various types of drug delivery, specifically in the context of the treatment of several neuropathological conditions where the therapeutic agents cannot cross the BBB. Drug toxicity and on-target specificity are among some of the limitations associated with current neurotherapeutics. In recent years, advances in nanodrug delivery have enabled the carrier system containing the active therapeutic drug to target the signaling pathways and pathophysiology that are closely linked to central nervous system (CNS) disorders such as Alzheimer’s disease (AD), Parkinson’s disease (PD), Huntington’s disease (HD), multiple sclerosis (MS), brain tumor, epilepsy, ischemic stroke, and neurodegeneration. At present, among the nano formulations, solid lipid nanoparticles (SLNs) have emerged as a putative drug carrier system that can deliver the active therapeutics (drug-loaded SLNs) across the BBB at the target site of the brain, offering a novel approach with controlled drug delivery, longer circulation time, target specificity, and higher efficacy, and more importantly, reducing toxicity in a biomimetic way. This paper highlights the synthesis and application of SLNs as a novel nontoxic formulation strategy to carry CNS drugs across the BBB to improve the use of therapeutics agents in treating major neurological disorders in future clinics.

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ApoE-Targeting Increases the Transfer of Solid Lipid Nanoparticles with Donepezil Cargo across a Culture Model of the Blood–Brain Barrier

Pharmaceutics ◽

10.3390/pharmaceutics13010038 ◽

2020 ◽

Vol 13 (1) ◽

pp. 38

Author(s):

Gizem Rüya Topal ◽

Mária Mészáros ◽

Gergő Porkoláb ◽

Anikó Szecskó ◽

Tamás Ferenc Polgár ◽

...

Keyword(s):

Drug Delivery ◽

Blood Brain Barrier ◽

Solid Lipid Nanoparticles ◽

Lipid Nanoparticles ◽

Brain Barrier ◽

Brain Targeting ◽

Solid Lipid ◽

Blood Brain ◽

Culture Model ◽

The Brain

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: A drug carrier system

Chronicles of Young Scientists ◽

10.4103/2229-5186.79346 ◽

2011 ◽

Vol 2 (1) ◽

pp. 26 ◽

Cited By ~ 2

Author(s):

HardikR Mody ◽

RashmiR Kokardekar

Keyword(s):

Solid Lipid Nanoparticles ◽

Drug Carrier ◽

Lipid Nanoparticles ◽

Carrier System ◽

Solid Lipid ◽

Drug Carrier System

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SOLID LIPID NANOPARTICLES (SLNs) AS NANO DRUG DELIVERY CARRIERS: PREPARATION, CHARACTERIZATION AND APPLICATION

International Journal of Applied Pharmaceutics ◽

10.22159/ijap.2020v12i1.35312 ◽

2019 ◽

pp. 1-9

Author(s):

MONA QUSHAWY ◽

ALI NASR

Keyword(s):

Drug Delivery ◽

Solid Lipid Nanoparticles ◽

Colloidal Particles ◽

Drug Carrier ◽

Physical Stability ◽

Controlled Drug Release ◽

Drug Carriers ◽

Colloidal Dispersion ◽

Lipid Nanoparticles ◽

Solid Lipid

Over the last few years, there has been a significant consideration of solid lipid nanoparticles (SLNs) as an alternative method to other colloidal dispersion methods for drug delivery. Special consideration has been given to the use of SLNs as a drug carrier in recent years. SLNs are aqueous dispersions in which the colloidal particles consist of solid lipids that are biodegradable. As a result of their physical stability, the protection of the entrapped drug from decomposition, the provision of controlled drug release, and the exceptional acceptability, SLNs have several advantages over other drug carriers. This article focuses on the techniques of SLNs preparation and characterization, the effect of formulation variables on SLNs properties, the routes of administration, and the pharmaceutical applications. The data used for this review was collected by searching on Google Scholar and PubMed using the following keywords during the period from 2010 to date.

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In vitroevaluation of idebenone-loaded solid lipid nanoparticles for drug delivery to the brain

Drug Development and Industrial Pharmacy ◽

10.3109/03639045.2010.539231 ◽

2011 ◽

Vol 37 (6) ◽

pp. 737-746 ◽

Cited By ~ 55

Author(s):

Lucia Montenegro ◽

Agata Campisi ◽

Maria Grazia Sarpietro ◽

Claudia Carbone ◽

Rosaria Acquaviva ◽

...

Keyword(s):

Drug Delivery ◽

Solid Lipid Nanoparticles ◽

Lipid Nanoparticles ◽

Solid Lipid ◽

The Brain

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Development of Solid Lipid Nanoparticles of Lamivudine for Brain Targeting

International Journal of Drug Delivery Technology ◽

10.25258/ijddt.v1i1.8837 ◽

2009 ◽

Vol 1 (1) ◽

Cited By ~ 1

Author(s):

Pravin Patil ◽

Anil Sharma ◽

Subhash Dadarwal ◽

Vijay Sharma

Keyword(s):

Drug Delivery ◽

Drug Release ◽

Solid Lipid Nanoparticles ◽

Rotation Speed ◽

Lipid Nanoparticles ◽

Brain Targeting ◽

Brain Penetration ◽

Solid Lipid ◽

Diffusion Technique

The objective of present investigation was to enhance brain penetration of Lamivudine, one of the most widely used drugs for the treatment of AIDS. This was achieved through incorporating the drug into solid lipid nanoparticles (SLN) prepared by using emulsion solvent diffusion technique. The formulations were characterized for surface morphology, size and size distribution, percent drug entrapment and drug release. The optimum rotation speed, resulting into better drug entrapment and percent yield, was in the range of 1000-1250 r/min. In vitro cumulative % drug release from optimized SLN formulation was found 40-50 % in PBS (pH-7.4) and SGF (pH-1.2) respectively for 10 h. After 24 h more than 65 % of the drug was released from all formulations in both mediums meeting the requirement for drug delivery for prolong period of time.

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Solid Lipid Nanoparticles: A Promising Drug Delivery Technology

International Journal of Pharmaceutical Sciences and Nanotechnology ◽

10.37285/ijpsn.2009.2.2.3 ◽

2009 ◽

Vol 2 (2) ◽

pp. 509-516

Author(s):

S. Pragati ◽

S. Kuldeep ◽

S. Ashok ◽

M. Satheesh

Keyword(s):

Drug Delivery ◽

Solid Lipid Nanoparticles ◽

Large Scale ◽

Colloidal Particles ◽

Scale Up ◽

Lipid Nanoparticles ◽

Scale Production ◽

Research Activity ◽

New Approach ◽

Solid Lipid

One of the situations in the treatment of disease is the delivery of efficacious medication of appropriate concentration to the site of action in a controlled and continual manner. Nanoparticle represents an important particulate carrier system, developed accordingly. Nanoparticles are solid colloidal particles ranging in size from 1 to 1000 nm and composed of macromolecular material. Nanoparticles could be polymeric or lipidic (SLNs). Industry estimates suggest that approximately 40% of lipophilic drug candidates fail due to solubility and formulation stability issues, prompting significant research activity in advanced lipophile delivery technologies. Solid lipid nanoparticle technology represents a promising new approach to lipophile drug delivery. Solid lipid nanoparticles (SLNs) are important advancement in this area. The bioacceptable and biodegradable nature of SLNs makes them less toxic as compared to polymeric nanoparticles. Supplemented with small size which prolongs the circulation time in blood, feasible scale up for large scale production and absence of burst effect makes them interesting candidates for study. In this present review this new approach is discussed in terms of their preparation, advantages, characterization and special features.

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