Background: The purpose of this study was to formulate, characterize and in-vitro cytotoxicity
of 5-Fluorouracil loaded controlled release nanoparticles for the treatment of skin cancer. The
patents on nanoparticles (US8414926B1), (US61654404A), (WO2007150075A3) etc. helped in the selection
polymers and method for the preparation of nanoparticles.
Methods: In the present study nanoparticles were prepared by simple ionic gelation method using various
concentrations of chitosan and sodium tripolyphosphate (TPP). Several process and formulation
parameters were screened and optimized using 25-2 fractional factorial design. The prepared nanoparticles
were evaluated for particle size, shape, charge, entrapment efficiency, crosslinking mechanism and
drug release study.
Results: The optimized 5-Fluorouracil loaded nanoparticle were found with particle size of of 320±2.1
nm, entrapment efficiency of 85.12%± 1.1% and Zeta potential of 29mv±1mv. Scanning electron microscopy
and dynamic light scattering technique revealed spherical particles with uniform size. The invitro
release profile showed controlled release up to 24 hr. Further study was carried using A375 basal
cell carcinoma cell-line to elucidate the mechanism of its cytotoxicity by MTT assay.
Conclusion: These results demonstrate that the possibility of delivering 5-Fluorouracil to skin with enhanced
encapsulation efficiency indicating effectiveness of the formulation for treatment of basal cell
carcinoma type of skin cancer.