Efficacy of surface charge in targeting pegylated nanoparticles of sulpiride to the brain

被引：56

作者：

Parikh, Tapan ^{[1
]}

Bommana, Murali Mohan ^{[1
]}

Squillante, Emilio, III ^{[1
]}

机构：

[1] St Johns Univ, Dept Pharm & Adm Sci, Coll Pharm, Queens, NY 11439 USA

来源：

EUROPEAN JOURNAL OF PHARMACEUTICS AND BIOPHARMACEUTICS | 2010年 / 74卷 / 03期

关键词：

Adsorption; Albumin; Blood-brain barrier; Cationized bovine serum albumin; CNS; Drug targeting; Pegylation; Microscopy; Nanoparticles; Sulpiride; Surface charge; DELIVERY; DRUG; BARRIER;

D O I：

10.1016/j.ejpb.2009.11.001

中图分类号：

R9 [药学];

学科分类号：

1007 ;

摘要：

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 t-lactide and used to prepare pegylated nanoparticles (NPs) loaded with sulphide by emulsification and solvent evaporation method Thiolated canonized bovine serum albumin (CBSA) was conjugated through the maleimide function to the NPs Rhodamine B and Alexa Fluor (R) 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 (10 mg/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 (c) 2009 Elsevier B.V All rights reserved

引用

页码：442 / 450

页数：9

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