Improved Anticancer Activity of Paclitaxel via Folic Acid-Mediated Chitosan Nanoparticles

Abstract

Purpose: Colorectal Cancer (CRC) is among the most prevalent malignancies of the gastrointestinal tract. Globally, it ranks as the third most frequently diagnosed cancer and the second leading cause of cancer-associated mortality. The objective of the research work was to develop a formulation with improved targeting characteristics for the efficient treatment of CRC. Thus, Folic Acid (FA) functionalized Paclitaxel (PAC) loaded Chitosan (CH) Nanoparticles (FA-CH-PAC-NPs) were developed and characterized.
Methods: The ionic gelation process was employed to develop Chitosan Nanoparticles (CH-NPs), which were then conjugated with FA utilizing the carbodiimide chemistry approach. Size of particles, surface structure, drug entrapment efficiency, and zeta potential are some of the critical factors that were taken into consideration when evaluating the formulations and optimizing them for different process variables. Furthermore, the MCF-7 cell line was used to assess In vitro cytotoxicity of improved formulations.
Results: The optimized FA-conjugated formulations exhibited an average particle size and zeta potential of 299 nm and 4.9 mV, respectively, and the drug entrapment efficiency was an excellent 83.5%. Eventually, the % PAC released from pure PAC, CH-PAC-NPs, and FA-CH-PAC-NPs was found to be 97.20%, 57.65%, and 68.88%, respectively, after a 24 h study period. The IC50 values, representing the concentration at which 50% of cell growth is inhibited, were 135.74 ± 0.053 µg/ml for PAC and significantly lower at 42.72 ± 0.132 µg/ml for FA-CH-PAC-NPs.
Conclusion: The results suggest that the optimized formulation FA-CH-PAC-NPs would have improved anticancer effects as well as targeting capability for the management of CRC.