Document Detail

Sialic acid and glycopeptides conjugated PLGA nanoparticles for central nervous system targeting: In vivo pharmacological evidence and biodistribution.
MedLine Citation:
PMID:  20338201     Owner:  NLM     Status:  MEDLINE    
Polymeric nanoparticles (Np) have been considered as strategic carriers for brain targeting. Specific ligands on the surface allowed the Np to cross the Blood-Brain Barrier (BBB) carrying model drugs within the brain district after their i.v. administration in experimental animals. It is known that sialic acid receptors are present in several organs, including in the brain parenchyma. Thus, in this paper, we prepared PLGA Np surface modified with a BBB-penetrating peptide (similopioid peptide) for BBB crossing and with a sialic acid residue (SA) for the interaction with brain receptors. This double coverage could allow to obtain novel targeted Np with a prolonged residence within the brain parenchyma, thus letting to reach a long-lasting brain delivery of drugs. The central analgesic activity of Loperamide (opioid drug, unable to cross the BBB) loaded in these novel Np was evaluated in order to point out the capability of the Np to reach and to remain in the brain. The results showed that the pharmacological effect induced by loaded Np administration remained significant over 24h. Using confocal and fluorescent microscopies, the novel Np were localized within the tissue parenchyma (brain, kidney, liver, spleen and lung). Finally, the biodistribution studies showed a localization of the 6% of the injected dose into the CNS over a prolonged time (24h). Notwithstanding an increased accumulation of SA-covered Np in those organs showing SA-receptors (liver, kidney, and lung), the pharmacological and biodistribution results are proofs of the ability of double targeted Np to enter the brain allowing the drug to be released over a prolonged time.
G Tosi; A V Vergoni; B Ruozi; L Bondioli; L Badiali; F Rivasi; L Costantino; F Forni; M A Vandelli
Publication Detail:
Type:  Journal Article     Date:  2010-03-23
Journal Detail:
Title:  Journal of controlled release : official journal of the Controlled Release Society     Volume:  145     ISSN:  1873-4995     ISO Abbreviation:  J Control Release     Publication Date:  2010 Jul 
Date Detail:
Created Date:  2010-06-01     Completed Date:  2010-09-16     Revised Date:  -    
Medline Journal Info:
Nlm Unique ID:  8607908     Medline TA:  J Control Release     Country:  Netherlands    
Other Details:
Languages:  eng     Pagination:  49-57     Citation Subset:  IM    
Copyright Information:
2010 Elsevier B.V. All rights reserved.
Department of Pharmaceutical Sciences, University of Modena and Reggio Emilia, Italy.
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MeSH Terms
Brain / drug effects*,  metabolism
Drug Carriers / chemistry*
Glycopeptides / chemistry*
Lactic Acid / chemistry*
Loperamide / administration & dosage,  pharmacokinetics,  therapeutic use
Microscopy, Electron, Scanning
N-Acetylneuraminic Acid / chemistry*
Nanoparticles / chemistry*
Organ Specificity
Pain / drug therapy
Particle Size
Polyglycolic Acid / chemistry*
Rats, Inbred Strains
Surface Properties
Tissue Distribution
Reg. No./Substance:
0/Drug Carriers; 0/Glycopeptides; 0/polylactic acid-polyglycolic acid copolymer; 131-48-6/N-Acetylneuraminic Acid; 26009-03-0/Polyglycolic Acid; 50-21-5/Lactic Acid; 53179-11-6/Loperamide

From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine

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