UEA I-bearing nanoparticles for brain delivery following intranasal administration.
Int J Pharm
; 340(1-2): 207-15, 2007 Aug 01.
Article
em En
| MEDLINE
| ID: mdl-17499948
ABSTRACT
Surface engineering of nanoparticles with lectins opened a novel pathway to improve the brain uptake of agents loaded by biodegradable PEG-PLA nanoparticles following intranasal administration. Ulex europeus agglutinin I (UEA I), specifically binding to l-fucose, which is largely located in the olfactory epithelium, was selected as a promising targeting ligand and conjugated onto the PEG-PLA nanoparticles surface with an optimized protocol relying on maleimide-mediated covalent binding technique. The in vivo results in rats suggested that UEA I modification at the nanoparticles surface facilitated the absorption of a fluorescent marker--6-coumarin associated with the nanoparticles into the brain following intranasal administration with significant increase in the area under the concentration-time curve (about 1.7 times) in different brain tissues compared with that of coumarin incorporated in the unmodified ones. UEA I-conjugation also elevated the brain-targeting efficiency of nanoparticles. Inhibition experiment of specific sugar suggested that the interactions between the nasal mucosa and the lectinised nanoparticles were due to the immobilization of carbohydrate-binding pockets on the surface of the nanoparticles. Distribution profiles of UEA I-modified nanoparticles indicated their higher affinity to the olfactory mucosa than to the respiratory one. Therefore, the UEA I-modified nanoparticles might serve as potential carriers for brain drug delivery, especially for mental therapeutics with multiple biological effects.
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Coleções:
01-internacional
Base de dados:
MEDLINE
Assunto principal:
Polietilenoglicóis
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Encéfalo
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Portadores de Fármacos
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Cumarínicos
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Lectinas de Plantas
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Nanopartículas
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Corantes Fluorescentes
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Lactatos
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Mucosa Nasal
Tipo de estudo:
Guideline
Limite:
Animals
Idioma:
En
Revista:
Int J Pharm
Ano de publicação:
2007
Tipo de documento:
Article