Aim: Formulation, optimization and anticancer activity of spray-dried Doxorubicin loaded
folic acid conjugated Gelatin nanoparticles (DOX-FA-GN).
Methods: Doxorubicin loaded gelatin nanoparticles (DOX-GN) were prepared by the Coacervation
phase separation method, optimized using DoE and then conjugated with folic acid by covalent coupling
to formulate Doxorubicin loaded folic acid conjugated nanoparticles (DOX-FA-GN). The formulated
nanoparticles were characterized to evaluate its physicochemical properties. Cellular uptake
and cell viability studies were carried out using MTT assay and biodistribution studies were
carried out in Wistar rats.
Results: Particle size, PDI and entrapment efficiency for optimized DOX-GN were found to be
152.3 ± 9.3 nm 0.294 ± 0.1 and 86.9± 3.4% while for DOX-FA-GN, 193.9 ± 12.3 nm 0.247 ± 0.2
and 84 ± 3.6%. The cytotoxic studies showed a cell viability of 75.1% for DOX-GN and 29.5%
DOX-FA-GN. Biodistribution studies were found to be statistically insignificant for conjugated
nanoparticles with excellent flow properties. Significantly higher DOX distribution in the lungs
was observed in the case of DOX-FA-GN.
Conclusion: There was a higher uptake of DOX on HeLa cells with DOX-FA-GN compared to
DOX-GN. Also, the biodistribution of Dox in the lungs of Wistar rats was higher in conjugated
nanoparticles as compared to unconjugated nanoparticles.