Cancer is considered one of the most threatening diseases worldwide. Although many therapeutic
approaches have been developed and optimized for ameliorating patient’s conditions and life expectancy, however,
it frequently remains an incurable pathology. Notably, conventional treatments may reveal inefficient in
the presence of metastasis development, multidrug resistance and inability to achieve targeted drug delivery.
In the last decades, nanomedicine has gained a prominent role, due to many properties ascribable to nanomaterials.
It is worth mentioning their small size, their ability to be loaded with small drugs and bioactive molecules
and the possibility to be functionalized for tumor targeting. Natural vehicles have been exploited, such as
exosomes, and designed, such as liposomes. Biomimetic nanomaterials have been engineered, by modification
with biological membrane coating. Several nanoparticles have already entered clinical trials and some liposomal
formulations have been approved for therapeutic applications. In this review, natural and synthetic nanocarriers
functionalized for actively targeting cancer cells will be described, focusing on their advantages with respect to
conventional treatments. Recent innovations related to biomimetic nanoparticles camouflaged with membranes
isolated from different types of cells will be reported, together with their promising applications. Finally, a short
overview on the latest advances in carrier-free nanomaterials will be provided.