Aim: To design D-Mannose conjugated 5-Fluorouracil (5-FU) loaded Jackfruit seed
starch nanoparticles (JFSSNPs) for site-specific delivery.
Background: Liver cancer is the third leading cause of death in the world and the fifth most often
diagnosed cancer. It is a major global threat to public health. Treatment of liver cancer with conventional
method bears several side effects, thus to undertake these side effects as a formulation challenge,
it is necessary to develop novel target-specific drug delivery system for the effective and better
localization of drug into the proximity of target with restricting the movement of the drug in normal
Objective: To optimize and characterize the developed D-Mannose conjugated 5-Fluorouracil (5--
FU) loaded Jackfruit seed starch nanoparticles (JFSSNPs) for effective treatment of liver cancer.
Materials and Methods: 5-FU loaded JFSSNPs were prepared and optimized formulations having
higher encapsulation efficiency were conjugated with D-Mannose. These formulations were characterized
for size, morphology, zeta potential, X-Ray Diffraction, and Differential Scanning
Calorimetry. The potential of NPs was studied using in vitro cytotoxicity assay, in vivo kinetic
studies, and bio-distribution studies.
Result and Discussion: 5-Fluorouracil loaded NPs had a particle size between 336 to 802nm with
drug entrapment efficiency between 64.2 to 82.3%. In XRD analysis, 5-FU peak was diminished in
the diffractogram, which could be attributed to the successful incorporation of the drug in amorphous
form. DSC study suggests there was no physical interaction between 5-FU and Polymer. NPs
showed sustained in vitro 5-FU release up to 2 hours. In vivo, mannose conjugated NPs prolonged
the plasma level of 5-FU and assisted in the selective accumulation of 5-FU in the liver (vs. other
organs spleen, kidney, lungs, and heart) compared to unconjugated one and plain drug.
Conclusion: In vivo, bio-distribution, and plasma profile studies resulted in a significantly higher
concentration of 5-Fluorouracil liver, suggesting that these carriers are efficient, viable, and targeted
carrier of 5-FU treatment of liver cancer.