In the present study, we have found that both OCTN2 and ATB0,+ are expressed a much higher level in human colon cancer cells than in normal colon cells, which provides a unique opportunity to examine the potential dual targeting of LC-PLGA NPs to OCTN2 and ATB0,+ to enhance the delivery of chemotherapeutic agents in a tumor cell-specific manner. This evidence concerns the gene SLC22A5 and neoplasm.