Cancer mortality is increasing at an alarming rate across the globe. Albeit, many therapeutics are available commercially, they are not effective and have no cure up to today. Moreover, the knowledge gap in cancer therapy persists, representing a potential blind spot for the innovation of effective anticancer therapeutics. This review presents an update on current advancements in nanopeptide therapeutics. Herein, a detailed exploration of peptide-functionalized nanoparticles for the development of nanotherapeutics was carried out. Different approaches that include self-assembly nanostructures, solid phase peptide synthesis, ligand exchange, chemical reduction, and conjugation methods for assembling peptides for functionalizing nanodrugs are also highlighted. An outlook on biomedical applications is also reviewed. Additionally, a comprehensive discussion on targeted cancer cell therapy and mechanism of action are provided. The present review reflects the functional novelty of nanodrugs to improve stability, accessibility, bioavailability, and specificity toward cancerous cells. Finally, it summarizes the current challenges and future perspectives on the formulation of these nanodrugs.
© 2022 The Authors. Published by American Chemical Society.