Self-assembly drug conjugates for anticancer treatment

[Display omitted] •Many anticancer compounds are unable to demonstrate pharmacological activity because they do not reach therapeutic concentration at the site of action.•Nanotechnology is a useful tool to improve the selective delivery of anticancer compounds to their site of action.•An interesting application of anticancer nanotechnology is represented by nanostructures spontaneously obtained by self-assembly of drug conjugates linked to a proper chemical entity.•The generation of hetero-NPs could be exploited for personalized combined treatment of different types of diseases. Self-assembly drug conjugate preparation is a promising approach to improve activity and penetration through physiological barriers of potent small molecules, as well as to reduce any side effects. Drug conjugates can self-assemble in water to form nanoparticles (NPs) that offer several advantages because: (i) they are easy to obtain; (ii) they can reach high local drug concentration in tumor tissues; and (iii) they can reduce the side effects of drugs. All these factors improve drug pharmacokinetic properties. Here, we have reviewed the scope of nanotechnology-based self-assembly drug delivery approaches focusing on prodrugs able to form NPs by self-assembly; we have also summarized the current perspective and challenges facing the successful treatment of cancer.