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 world and fifth most often diagnosed cancer is the 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 drug in normal tissues.
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 formulation had higher encapsulation efficiency
were conjugated with D-Mannose. These formulations were characterized for size, morphology, zeta potential, X-Ray Diffraction, and Differential Scanning Calorimetry. Potential of NPs were studied using in vitro cytotoxicity assay, in vivo kinetic studies and bio-distribution studies.
Result and discussion:
5-Fluorouracil loaded NPs had particle size between 336 to 802nm with drug entrapment efficiency
was 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 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 assist 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 significantly higher concentration of 5-
Fluorouracil liver suggesting that these carriers are efficient, viable, and targeted carrier of 5-FU treatment of liver cancer.