New Chitosan Nanospheres for the Delivery of 5-Fluorouracil: Preparation, Characterization and in vitro Studies
Roberta Cavalli, Federica Leone, Rosalba Minelli, Roberto Fantozzi and Chiara Dianzani
Pages 270-278 (9)
The aim of this work was to develop new chitosan nanospheres for the delivery of 5-fluorouracil (5-FU). Drug
loaded nanospheres were prepared using a technique derived from a combination of coacervation and emulsion droplet
coalescence methods. The size and morphology of nanospheres were characterized by laser light scattering and transmission
electron microscopy. The 5-FU interaction with chitosan nanospheres was investigated by DSC analysis and FT-IR
spectroscopy. The in vitro release was studied by dialysis bag technique. Cytotoxicity of 5-FU loaded chitosan nanospheres
was evaluated in vitro on HT29 and PC-3 cell lines. The effects of 5-FU loaded chitosan nanospheres on adhesion
of tumor cells to human umbilical vein endothelial cells (HUVEC) were also investigated. 5-FU loaded chitosan nanospheres
appeared with a spherical shape, with a mean diameter of about 200 nm and a negative zeta potential of about
- 6.0 mV. The successful interaction between drug and chitosan nanosphere matrix was demonstrated by both DSC and
FT-IR analyses. The quantitative determination of 5-FU was assayed by UV-Vis analysis. The encapsulation efficiency of
5-FU content was about 70%. A kinetic study of in vitro release demonstrated that the percentages of 5-FU delivered from
nanospheres was approx. 10% after 3 hours. The in vitro studies showed that 5-FU loaded nanospheres were effective in
reducing tumor cell proliferation in a time- and concentration-dependent manner. 5-FU nanospheres were also able to inhibit
both HT29 and PC-3 adhesion to HUVEC after 48 hours of treatment.
Chitosan, Drug delivery systems, 5-fluorouracil, Nanospheres, Sustained release.
Department of Drug Science and Technology, University of Torino, Via Pietro Giuria 9, 10125, Turin, Italy.