Studying the effect of physically‐adsorbed coating polymers on the cytotoxic activity of optimized bisdemethoxycurcumin loaded‐PLGA nanoparticles

The aim of this work was to study the effect of different physically‐adsorbed coating polymers on the cytotoxic activity of optimized bisdemethoxycurcumin (BDMC) loaded‐PLGA nanoparticles. BDMC‐loaded poly(DL‐lactide‐co‐glycolide) (PLGA) nanoparticles were prepared adopting the nanoprecipitation technique according to a full factorial study design. The effects of three independent variables each at two levels, namely: the polymer type, polymer concentration, and poly vinyl alcohol concentration were studied. The particles were optimized regarding particle size and entrapment efficiency where sizes <200 nm and entrapment efficiencies reaching ∼98% were obtained. The particles were further characterized using x‐ray diffraction, transmission electron microscopy, andin‐vitrorelease studies. A selected formulation was subjected to physical coating using various coating moieties, namely: PEG 4000, Tween 80 and Pluronic F68, to impart a hydrophilic stealth character to the surface. The surface hydrophobicity was assessed using the Rose Bengal dye test where the hydrophilicity character followed the following order: Tween 80 > PEG 4000 > Pluronic F68. The particles coating rendered the particles suitable for cancer‐targeting regarding particle size measurements, morphology, release kinetics, and stability studies. Moreover, cytotoxicity testing was performed using HepG‐2 cells. Coated NPs showed the highest inhibition of malignant cells viability compared to the uncoated NPs and free BDMC where the IC50of Pluronic‐F68 coated NPs was 0.54 ± 0.01 µg/mL. The augmented effect against malignant cells poses these particles as a successful cancer remedy.