Chitosan Nanomedicine in Cancer Therapy: Targeted Delivery and Cellular Uptake

Macromol Biosci. 2021 May;21(5):e2100005. doi: 10.1002/mabi.202100005. Epub 2021 Mar 19.


Nanomedicine has gained much attention for the management and treatment of cancers due to the distinctive physicochemical properties of the drug-loaded particles. Chitosan's cationic nature is attractive for the development of such particles for drug delivery, transfection, and controlled release. The particle properties can be improved by modification of the polymer or the particle themselves. The physicochemical properties of chitosan particles are analyzed in 126 recent studies, which allows to highlight their impact on passive and active targeted drug delivery, cellular uptake, and tumor growth inhibition (TGI). From 2012 to 2019, out of 40 in vivo studies, only 4 studies are found reporting a reduction in tumor size by using chitosan particles while all other studies reported tumor growth inhibition relative to controls. A total of 23 studies are analyzed for cellular uptake including 12 studies reporting cellular uptake mechanisms. Understanding and exploiting the processes involved in targeted delivery, endocytosis, and exocytosis by controlling the physicochemical properties of chitosan particles are important for the development of safe and efficient nanomedicine. It is concluded based on the recent literature available on chitosan particles that combination therapies can play a pivotal role in transformation of chitosan nanomedicine from bench to bedside.

Keywords: cellular uptake; chitosan; exocytosis; particle physico chemical properties; protein corona; targeted delivery; tumor growth inhibition.

Publication types

  • Research Support, Non-U.S. Gov't
  • Review

MeSH terms

  • Animals
  • Antineoplastic Agents / administration & dosage*
  • Antineoplastic Agents / therapeutic use
  • Body Fluids / metabolism
  • Chitosan / administration & dosage*
  • Chitosan / chemistry
  • Drug Delivery Systems*
  • Endocytosis
  • Humans
  • Nanomedicine*
  • Neoplasms / drug therapy*
  • Particle Size
  • Surface Properties


  • Antineoplastic Agents
  • Chitosan