Our results from both in vitro and in vivo experiments demonstrated that the prepared liposome produced better antitumor activity compared to free CPT-11, an extended period outflow of irinotecan took time from PEGylated liposomes and proposed encouraging expectations on the use of EGFR-targeted DSPE-PEG2000 liposomes as CPT-11 delivery system for CRC targeting therapy. Here, EGFR is linked to colorectal carcinoma.