Influence of PEGylation on PLGA nanoparticle properties, hydrophobic drug release and interactions with human serum albumin

The Journal of Pharmacy and Pharmacology
Tendai SamkangeAdmire Dube

Abstract

To evaluate the impact of PEG content on poly(lactic-co-glycolic acid) (PLGA) NP physicochemical properties, hydrophobic drug release (rifampicin as a model drug) and human serum protein binding. Rifampicin loaded and unloaded nanoparticles with PEG content of 0-17% (w/w) were prepared by an emulsification-evaporation technique. Nanoparticles were characterized for size, zeta potential and morphology. PEGlyation was confirmed using proton nuclear magnetic resonance (1H NMR). Fluorescence spectroscopy and dynamic light scattering were used to determine nanoparticle-protein binding, binding constants and stability of nanoparticles in human serum, respectively. Drug loading and release were determined by UV-VIS spectroscopy and drug release data was mathematically modelled. A NP PEG content of 17% w/w significantly retarded release of rifampicin from PLGA NPs and altered kinetics of drug release. Stern-Volmer (Ksv) protein binding constants decreased upon PEG incorporation. A 2% w/w PEG was sufficient to significantly reduce protein binding extent to PLGA NPs and maintain particle size distributions. The ability to fine tune drug release and formation of protein corona around nanoparticles is crucial to formulation scientists. Thi...Continue Reading

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Citations

Apr 7, 2020·Journal of Biomaterials Science. Polymer Edition·Samira KhalediSoodabeh Davaran
Apr 30, 2021·International Journal of Pharmaceutics·Renata Ribeiro de CastroBruno Sarmento

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