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Purpose: To develop poly-lactic-co-glycolic acid (PLGA)-based nanoparticles (NPs) for the delivery of sunitinib malate (STM) to colon cancer cells.

Methods: Three different formulations (F1–F3) were developed by nano-precipitation technique using various concentrations of PLGA. The NPs were evaluated for particle size, polydispersity index, zeta potential, drug entrapment, and drug loading, using differential scanning calorimetry (DSC), Fouriertransform infrared spectroscopy (FTIR), x-ray diffraction (XRD), and scanning electron microscopy (SEM). Furthermore, in vitro drug release and anticancer studies were carried out on the formulations.

Results: Among the three NPs, optimized NP (F3) of STM was chosen for in vitro anti-cancer study against H-29 human colon cancer cells lines based on its particle size (132.9 nm), PDI (0.115), zeta potential (-38.12 mV), entrapment efficiency (52.42%), drug loading (5.24%), and drug release (91.26% in 48 h). A significant anti-cancer activity of the optimized NPs was observed, relative to free STM.

Conclusion: These findings suggest that STM-loaded NPs possess significant anti-cancer activity against human colon cancer HT-29 cells lines.