Background: Several studies have suggested the potential aptitude of polylactic-co-glycolic
acid (PLGA)-derived nanoparticles (NPs) to improve the antitumor efficacy of anticancer
drugs against colon cancer. Further, conjugation of lectins over the surface of the NPs may ameliorate
interaction and thus enhance the attachment of NPs with receptors.
Objective: The main goal of the study was to prepare and evaluate the targeting potential (in vivo)
of the optimized NPs against colorectal cancer.
Methods: The 5-fluorouracil (5-FU) loaded and wheat germ agglutinin (WGA)-conjugated PLGA-
NPs (WFUNPs) were prepared and then they were evaluated in vivo for targeting aptitude of
formulation using gamma scintigraphy after oral delivery. The WGA-conjugated and non-conjugated
optimized NPs were compared for any significant results. Further, optimized formulations were
also assessed for different parameters such as radiolabeling efficiency, sodium pertechnetate uptake,
stability of NPs, and organ distribution study.
Results: Findings suggested prolonged retention of 99mTc-tagged WFUNPs in the colonic region after
24 h study. Eventually, the outcome from conjugated formulation revealed enhanced bioavailability
of the drug in blood plasma for up to 24 h.
Conclusion: In conclusion, WGA-conjugation to NPs could improve the performance of the PLGA-
NPs in the treatment of colorectal cancer.