Abstract

Sunitinib malate (SM) is a multi-targeted tyrosine kinase (TK) inhibitor. It is proposed as a potent anticancer drug intended for colon cancer. The current work aimed at developing Sunitinib malate -loaded nanoparticles for colon- targeting. SM loaded ES100-nanoparticles were developed by nano-precipitation method using poly vinyl alcohol (PVA) as stabilizer. Different formulation of ESNP (F1-F3) were prepared and evaluated for particle size, poly-dispersity index, and drug entrapment, using Fourier transform infrared spectroscopy (FTIR), x-ray diffraction (XRD), and scanning electron microscopy (SEM). The optimized formulation was further studied by in-vitro drug release and anticancer cell line study. The mean particle size, PDI, %EE of optimized SM loaded ESNPF2 was found to be 384.8±5.53 nm, 0.58, and 60.31% respectively. In vitro release of the optimized ESNPF2 showed 10.2 % drug release till 2 h, at 4h 29.6% and 12 h and 24 h 66.45%, 82.2% respectively at pH 7.4. SEM images and surface morphology confirmed that nanoparticles were spherical and had smooth surfaces. An MTT assay was conducted in the colon cancer cell lines (CACO2) to evaluate anti-cancerous activity of SM. SM loaded ESNPF2 showed a high potential against colon cancer cells. The overall results suggest that SM loaded ES100-nanoparticels could be a potential option for colon targeting.

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