Background: Cancer is one of the most awful lethal diseases all over the world and the success
of its current chemotherapeutic treatment strategies is limited due to several associated drawbacks.
The exploration of cancer cell physiology and its microenvironment has exposed the potential of various
classes of nanocarriers to deliver anticancer chemotherapeutic agents at the tumor target site.
These nanocarriers must evade the immune surveillance system and achieve target selectivity. Besides,
they must gain access into the interior of cancerous cells, evade endosomal entrapment and discharge the
drugs in a sustained manner. Chitosan, the second naturally abundant polysaccharide is a biocompatible,
biodegradable and mucoadhesive cationic polymer which has been exploited extensively in the last few
years in the effective delivery of anticancer chemotherapeutics to the target tumor cells. Therapeutic
agent-loaded surface modified chitosan nanoparticles are established to be more stable, permeable and
Conclusion: This review will provide an up-to-date evidence-based background on recent pharmaceutical
advancements in the transformation of chitosan nanoparticles for smart anticancer therapeutic
Highlights: • Efforts to improve cancer chemotherapy by exploiting the intrinsic differences between
normal and neoplastic cells to achieve maximum effective drug delivery to target cancer cells through
bioengineered chitosan nano delivery vectors are discussed.
• The easy manipulation of surface characteristics of chitosan based nanoparticles by various functionalization
methods to achieve targeted drug delivery proves its potential to be an essential tool for the
advancement of anticancer drug-delivery vectors.