Synthesis of combinatorial Janus nanoparticles based on EpCAM‐PEG/PCL for targeted therapy of human colorectal adenocarcinoma

Abstract Active targeted nanotechnology‐based drug delivery systems have gained significant favor because they have the ability to decrease side effects, improve drug bioavailability, and the potency of anticancer treatment. In this study, functional amphiphilic Janus nanoparticles (JNPs), consisting of hydrophilic and hydrophobic biocompatible polymers as two distinct sides, have been prepared via a robust and simple synthesis method. The surface‐active hydrophilic side of this Janus platform is functionalized with an aptamer against epithelial cell adhesion molecule (EpCAM) to deliver Doxorubicin (DOX) for the treatment of metastasis colorectal adenocarcinoma HT29 cells. The Janus morphology of the nanoparticles and their cell penetration behavior are shown in microscopic evaluations. By evaluating the prepared DOX‐loaded aptamer–modified JNPs by cell‐toxicity assay and confocal microscopy, it was determined that the utilization of an internalization strategy to enhance cell uptake would increase the anticancer effect of the Janus nanocarrier and improve the capacity to deliver the chemotherapeutical drug site‐specifically.