Development and characterization of folic acid-conjugated chitosan nanoparticles for targeted and controlled delivery of gemcitabinein lung cancer therapeutics

The present study was designed to investigate the tumor-targeting potential of gemcitabine (GEM)-loaded surface-tailored chitosan (CS)/poly (ethylene glycol) nanoparticles (FA-PEG-GEM-NPs). The nanoparticles encapsulated with GEM were prepared, characterized, and tethered with folic acid. The developed formulations were characterized with respect to particle size/poly-dispersity index, shape, and zeta potential analysis. The in vitro study shows the sustained drug-release kinetics during 48h. The present result shows remarkable cytotoxicity rendered by GEM when delivered through FA-PEG-GEM-NPs formulation. The microscopic assessment is suggestive of significant uptake of FA-PEG-GEM-NPs in comparison with the unmodified PEG-GEM-NPs and free drug. Finally, our results advocate for the sizeable compatibility, comparatively less organ toxicity, and higher anti-tumor activity of ligand-anchored and PEGylated CS nanoparticles in vitro and corroborated by in vivo investigations. In conclusion, it is interpreted that surface-tailored nanoparticles are capable to ferry bioactives selectively and specifically to tumor sites with the interception of minimal side effects, thereby suggesting their potential application in cancer therapeutics.