Document Detail

Efficacy of surface charge in targeting pegylated nanoparticles of sulpiride to the brain.
MedLine Citation:
PMID:  19941957     Owner:  NLM     Status:  MEDLINE    
The objective of the study was to formulate sulpiride-loaded nanoparticles (NPs) that can improve bioretention and achieve dose reduction by passively targeting the drug near the site of action. Methoxy PEG-PLA and maleimide PEG-PLA were synthesized via ring opening polymerization of L-lactide and used to prepare pegylated nanoparticles (NPs) loaded with sulpiride by emulsification and solvent evaporation method. Thiolated cationized bovine serum albumin (CBSA) was conjugated through the maleimide function to the NPs. Rhodamine B and Alexa Fluor 488 were used as fluorescent markers for nanoparticle uptake studies. The nanoparticles were characterized for particle size, zeta potential and drug loading. Sprague Dawley rats were administered with each of CBSA-NPs, BSA-NPs and uncoated NPs (10mg/kg) via tail vein; plasma and urine concentrations were measured and tissue sections were observed under fluorescence microscope. Characterized particles (mean particle size 329+/-44 nm) indicated the conjugation of cationic albumin to NPs (zeta potential shift from -39 mV to -19 mV). Fluorescence showed a high accumulation of CBSA-NPs in brain compared to that of BSA-NPs and uncoated NPs supported by plasma and urine profile. The significant results proved that CBSA-NPs could be a promising brain drug delivery for sulpiride.
Tapan Parikh; Murali Mohan Bommana; Emilio Squillante
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Publication Detail:
Type:  Journal Article     Date:  2009-11-24
Journal Detail:
Title:  European journal of pharmaceutics and biopharmaceutics : official journal of Arbeitsgemeinschaft f?r Pharmazeutische Verfahrenstechnik e.V     Volume:  74     ISSN:  1873-3441     ISO Abbreviation:  Eur J Pharm Biopharm     Publication Date:  2010 Mar 
Date Detail:
Created Date:  2010-03-08     Completed Date:  2010-06-21     Revised Date:  -    
Medline Journal Info:
Nlm Unique ID:  9109778     Medline TA:  Eur J Pharm Biopharm     Country:  Netherlands    
Other Details:
Languages:  eng     Pagination:  442-50     Citation Subset:  IM    
Copyright Information:
(c) 2009 Elsevier B.V. All rights reserved.
Department of Pharmacy and Administrative Sciences, Saint Johns University, New York 11439, USA.
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MeSH Terms
Brain / drug effects*,  metabolism
Drug Carriers / chemistry*
Drug Compounding
Drug Delivery Systems / methods
Injections, Intravenous
Maleimides / chemical synthesis,  chemistry*
Microscopy, Electron, Scanning
Nanoparticles / chemistry*
Particle Size
Polyesters / chemistry*
Polyethylene Glycols / chemical synthesis,  chemistry*
Rats, Sprague-Dawley
Serum Albumin, Bovine / chemistry
Sulpiride / administration & dosage*,  blood,  pharmacokinetics,  urine
Surface Properties
Tissue Distribution
Reg. No./Substance:
0/Drug Carriers; 0/Maleimides; 0/Polyesters; 0/Polyethylene Glycols; 0/Serum Albumin, Bovine; 0/methoxy poly(ethylene glycol)-poly(lactide); 15676-16-1/Sulpiride

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