Long-circulating pegylated polycyanoacrylate nanoparticles as new drug carrier for brain delivery.
Abstract
Purpose The aim of this study was to evaluate the ability of long-circulating PEGylated cyanoacrylate nanoparticles to diffuse into the brain tissue. Methods Biodistribution profiles and brain concentrations of [14C]-radiolabeled PEG-PHDCA, polysorbate 80 or poloxamine 908-coated PHDCA nanoparticles, and uncoated PHDCA nanoparticles were determined by radioactivity counting after intravenous administration in mice and rats. In addition, the integrity of the blood-brain barrier (BBB) after nanoparticles administration was evaluated by in vivo quantification of the diffusion of [14C]-sucrose into the brain. The location of fluorescent nanoparticles in the brain was also investigated by epi-fluorescent microscopy. Results Based on their long-circulating characteristics, PEGylated PHDCA nanoparticles penetrated into the brain to a larger extent than all the other tested formulations. Particles were localized in the ependymal cells of the choroid plexuses, in the epithelial cells of pia mater and ventricles, and to a lower extent in the capillary endothelial cells of BBB. These phenomena occurred without any modification of BBB permeability whereas polysorbate 80-coated nanoparticles owed, in part, their efficacy to BBB permeabilization induced by the surfactant. Poloxamine 908-coated nanoparticles failed to increase brain concentration probably because of their inability to interact with cells. Conclusions This study proposes PEGylated poly (cyanoacrylate) nanoparticles as a new…
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For intravenous injection, at least 90% of nanoparticles have been observed to be sequestered within tissues and organs prior to reaching the brain, so intra-arterial injections might be more reliable.
“For intravenous injection, at least 90% of nanoparticles have been observed to be sequestered within tissues and organs prior to reaching the brain (Calvo et al., 2001), so intra-arterial injections might be more reliable.”
From Human Brain/Cloud Interface (2019) · cites this paper as Calvo et al., 2001
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- Authors
- Calvo, P., Gouritin, B., Chacun, H., Desmaële, D., D'Angelo, J., Noel, J.-P., Georgin, D., Fattal, E., Andreux, J. P., & Couvreur, P.
- Affiliations
- Université Paris-Sud (FR)
- Commissariat à l'Énergie Atomique et aux Énergies Alternatives (FR)
- Corresponding author
- Couvreur, Patrick
- Venue
- Pharmaceutical Research
- Published
- 2001-08
- Volume
- 18
- Issue
- 8
- Pages
- 1157-1166
- ISSN
- 0724-8741 (ISSN-L)
- 1573-904X
- OpenAlex
- W66478222
- Cited by
- 443
- References
- 1
- Citations by year
- 2025: 4 · 2024: 11 · 2023: 9 · 2022: 12 · 2021: 14 · 2020: 20 · 2019: 17 · 2018: 20 · 2017: 14 · 2016: 31 · 2015: 17 · 2014: 21 · 2013: 32 · 2012: 27
- FWCI
- 6.37
- Type
- journal article
- Language
- en
- Open access
- closed
- Licence
- Locations
- Pharmaceutical Research (publishedVersion)
- PubMed (publishedVersion)
- Topics
- Physical Sciences › Materials Science › Biomaterials › Nanoparticle-Based Drug Delivery
- Life Sciences › Neuroscience › Neurology › Barrier Structure and Function Studies
- Life Sciences › Pharmacology, Toxicology and Pharmaceutics › Pharmaceutical Science › Advanced Drug Delivery Systems
- Keywords
- PEGylated nanoparticles, brain drug delivery, blood-brain barrier, tissue distribution, polysorbate 80 coating, blood-brain barrier permeability, choroid plexus, surface coating effects
- MeSH terms
- Acrylic Resins, Animals, Blood-Brain Barrier, Brain, Chemistry, Physical, Diffusion, Drug Carriers, Fluorescent Dyes, Isotope Labeling, Male, Microspheres, Particle Size, Permeability, Polyethylene Glycols, Sucrose, Surface-Active Agents, Suspensions, Tissue Distribution, Drug Delivery Systems, Mice, Rats, Chemical Phenomena
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