ABSTRACT:
Colorectal cancer (CRC) is the third most common cancer in men and the second in women worldwide. In colorectal cancer therapy, as it is in other cancers, biodistribution to tumor tissue can be limited and not reach effective concentrations. Concanavalin (Con-A) conjugated polylactic-co-glycolic acid (PLGA) nanoparticles loaded with 5-fluorouracil (5-FU), were prepared and evaluated under in vitro and in vivo conditions. Con-A conjugated 5-FU nanoparticles (CFUNP) was employed as the carriers for cancer treatment. Solvent evaporation method was employed for the preparation of nanoparticles and characterized for particles size, size distribution, zeta potential, surface morphology, % drug entrapment and in vitro drug release in the simulated intestinal fluid. Optimized nanoparticles were conjugated with Con-A and further characterized by Con-A conjugation efficiency, mucoadhesion, and gamma scintigraphy study. Conjugated nanoparticles sustained the drug release significantly (p<0.05) over a period of 24 h when compared to the marketed formulation of 5-FU. A measurable number of counts of 99mTc-tagged CFUNP3 formulation after 24h study period suggested retention of nanoparticles for a prolonged period of time in the colonic region. These results suggested that Con-A conjugated nanoparticles could be considered as a promising carrier for selectively targeting drug(s) to the colon for the treatment of colon cancer.