The role of peptides in blood‐brain barrier nanotechnology

Teixidó, Meritxell; Giralt, Ernest

doi:10.1002/psc.983

Cited by 29 publications

(15 citation statements)

References 121 publications

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“…Delivery to the brain is a complex process as compounds must cross a natural defense mechanism, the BBB, designed to keep harmful substances out of this organ. [36] The parallel artificial membrane permeability assay (PAMPA) uses an artificial membrane in the form of filtersupported phospholipid bilayers. To mimic the BBB, a porcine polar lipid extract is used to coat the filter.…”

Section: Resultsmentioning

confidence: 99%

Benzimidazolium Salts as Small, Nonpeptidic and BBB‐Permeable Human Prolyl Oligopeptidase Inhibitors

et al. 2008

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Prolyl oligopeptidase (POP) is a cytosolic serine peptidase that hydrolyzes proline-containing peptides at the carboxy terminus of proline residues. This peptidase has gained importance as a target for the treatment of cognitive disturbances of patients with neuropsychiatric diseases. Our research addresses the identification of POP inhibitors from a small focused library of polar heterocyclic compounds arising from multicomponent reactions. Two selective POP-specific inhibitors were identified on the basis of their inhibition of dipeptidyl peptidase IV. The most active compounds were evaluated for their in vitro transport through the blood-brain barrier (BBB) using a parallel artificial membrane permeability assay. Our results show for the first time that benzimidazolium salts are new POP-inhibitory scaffolds with properties of solubility, specificity, and lipophilicity that may allow them to cross the BBB by passive diffusion. These findings constitute an excellent starting point to synthesize new POP inhibitors with enhanced properties.

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Section: Resultsmentioning

confidence: 99%

Benzimidazolium Salts as Small, Nonpeptidic and BBB‐Permeable Human Prolyl Oligopeptidase Inhibitors

et al. 2008

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“…[46] Targeting to the brain and overcoming the blood brain barrier (BBB) is another important application for peptide ligands. [47] Prades et al designed a retro-enantio 12 amino acid peptide sequence to target the TfR at a binding site different to Tf. [48] TfRs are heavily expressed in the brain microvasculature.…”

Section: Targeting Ligandsmentioning

confidence: 99%

Particle Targeting in Complex Biological Media

Dai

Bertleff‐Zieschang

Braunger

et al. 2017

Adv Healthcare Materials

100

102

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Over the past few decades, nanoengineered particles have gained increasing interest for applications in the biomedical realm, including diagnosis, imaging, and therapy. When functionalized with targeting ligands, these particles have the potential to interact with specific cells and tissues, and accumulate at desired target sites, reducing side effects and improve overall efficacy in applications such as vaccination and drug delivery. However, when targeted particles enter a complex biological environment, the adsorption of biomolecules and the formation of a surface coating (e.g., a protein corona) changes the properties of the carriers and can render their behavior unpredictable. For this reason, it is of importance to consider the potential challenges imposed by the biological environment at the early stages of particle design. This review describes parameters that affect the targeting ability of particulate drug carriers, with an emphasis on the effect of the protein corona. We highlight strategies for exploiting the protein corona to improve the targeting ability of particles. Finally, we provide suggestions for complementing current in vitro assays used for the evaluation of targeting and carrier efficacy with new and emerging techniques (e.g., 3D models and flow‐based technologies) to advance fundamental understanding in bio‐nano science and to accelerate the development of targeted particles for biomedical applications.

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“…TAT-GS nanoparticle-mediated calcitonin gene-related peptide (CGRP) gene delivery has been proposed to be an innovative strategy for cerebral vasospasm [22]. Therefore, normal brain drugs combining with peptides, nanotechnology and magnetic targeting may greatly improve the treatment of brain disorders [23].…”

Section: Introductionmentioning

confidence: 99%

Brain-Targeted Delivery of Trans-Activating Transcriptor-Conjugated Magnetic PLGA/Lipid Nanoparticles

et al. 2014

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Magnetic poly (D,L-lactide-co-glycolide) (PLGA)/lipid nanoparticles (MPLs) were fabricated from PLGA, L-α-phosphatidylethanolamine (DOPE), 1,2-distearoyl-sn-glycero-3-phosphoethanolamine-N-amino (polyethylene glycol) (DSPE-PEG-NH2), and magnetic nanoparticles (NPs), and then conjugated to trans-activating transcriptor (TAT) peptide. The TAT-MPLs were designed to target the brain by magnetic guidance and TAT conjugation. The drugs hesperidin (HES), naringin (NAR), and glutathione (GSH) were encapsulated in MPLs with drug loading capacity (>10%) and drug encapsulation efficiency (>90%). The therapeutic efficacy of the drug-loaded TAT-MPLs in bEnd.3 cells was compared with that of drug-loaded MPLs. The cells accumulated higher levels of TAT-MPLs than MPLs. In addition, the accumulation of QD-loaded fluorescein isothiocyanate (FITC)-labeled TAT-MPLs in bEnd.3 cells was dose and time dependent. Our results show that TAT-conjugated MPLs may function as an effective drug delivery system that crosses the blood brain barrier to the brain.

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The role of peptides in blood‐brain barrier nanotechnology

Cited by 29 publications

References 121 publications

Benzimidazolium Salts as Small, Nonpeptidic and BBB‐Permeable Human Prolyl Oligopeptidase Inhibitors

Benzimidazolium Salts as Small, Nonpeptidic and BBB‐Permeable Human Prolyl Oligopeptidase Inhibitors

Particle Targeting in Complex Biological Media

Brain-Targeted Delivery of Trans-Activating Transcriptor-Conjugated Magnetic PLGA/Lipid Nanoparticles

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