The development and scale-up of biodegradable polymeric nanoparticles loaded with ibuprofen

This study aims to ascertain the influence of variables in the production of blank and ibuprofen-loaded polymeric nanoparticles (IbNPs), as well as to scale up nanoparticle (NP) preparation 30-fold. Blank NP and IbNP with a matrix of poly (lactide-co-glycolide) (PLGA) were prepared by modified spontaneous emulsion solvent diffusion (SESD). The variables, organic solvent type, surfactant type and concentration, polymer concentration, aqueous phase volume, mixing speed, and manufacturing temperature, were investigated. Particle size, encapsulation efficiency (EE), drug loading and drug release were characterized. The smallest blank NP (175 nm) was obtained using a dimethy sulfoxide (DMSO):ethanol (50:50) organic solvent system with poly (vinyl alcohol) (PVA, 0.5% (w/w)) under magnetic stirring. The smallest IbNP obtained was 152 nm. The EE was highest at 30:100, drug:polymer ratio with a drug loading of 17.2%. Key NP characteristics, particle size, EE, drug loading and total drug release time of 30-fold scaled-up batch were not significantly different from lab-scale batch; however, 50% drug release for the scaled-up batch was significantly sooner (p < 0.05) than the lab-scale batch.

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► Blank NP and IbNP were prepared by modified SESD.
► IbNP has small size, high encapsulation efficiency and high drug-loading ratio.
► A 30-fold scaled-up batch of IbNP was prepared without the change in key characteristics.
► Variables on nanoparticle production by modified SESD were systematically analyzed.