As FDA approved the application of DSPE-PEG2000 (1,2-distearoyl-sn-glycero-3-phosphoethanolamine-PEG2000) in the drug formulations [34] and knowing the importance of EGFR in the treatment of colorectal cancers (CRCs) [10, 11], we sought to evaluate the antitumor effects of EGFR-Lipo-CPT-11 through cell proliferation, ROS formation, and cell apoptosis in vitro. Here, EGFR is linked to colorectal cancer.