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.