Purpose: Formulation, optimization and anticancer activity of spray-dried Doxorubicin loaded folic acid
conjugated Gelatin nanoparticles (DOX-FA-GN).
Method: 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.
Result: Particle size, PDI and entrapment efficiency for optimized DOX-GN was 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 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.
Conclusions: 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