5-Fluorouracil Loaded Orally Administered WGA-decorated Poly(lacticco- glycolic Acid) Nanoparticles for Treatment of Colorectal Cancer: In Vivo Evaluation

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.