Over
the past few decades, tremendous progress has been made in
the development of engineering nanomaterials, which opened new horizons
in the field of diagnosis and treatment of various diseases. In particular,
self-assembled organic nanomaterials with intriguing features including
delicate structure tailoring, facile processability, low cost, and
excellent biocompatibility have shown outstanding potential in biomedical
applications because of the enhanced permeability and retention (EPR)
effect and multifunctional properties. In this review, we briefly
introduce distinctive merits of self-assembled organic nanomaterials
for biomedical applications. The main focus will be placed on summarizing
recent advances in self-assembled organic nanomedicine for drug delivery,
bioimaging, and cancer phototherapy, followed by highlighting a critical
perspective on further development of self-assembled organic nanomaterials
for future clinical translation. We believe that the above themes
will appeal to researchers from different fields, including material,
chemical, and biological sciences, as well as pharmaceutics.