The surface-functionalised gelatin nanoparticles (GNPs) containing cisplatin were developed and characterised for breast cancer targeting using fibroblast growth factor-2 (FGF2) receptors which are overexpressed on breast cancer cells. The GNPs were prepared using two-step desolvation method and then the surface of GNPs was functionalised with activated heparin. They were characterised for surface morphology, particle size and size distribution, surface charge, entrapment efficiency and in vitro drug release. The results revealed that the mean diameter of GNPs was 173 +/- 2.2nm with smooth surface, which was increased to 189 +/- 3.4nm after coupling with heparin (H-GNPs). The targeting effect of H-GNPs and GNPs was investigated by in vitro cell uptake study on human breast cancer MDA-MB-231 cell line, which exhibited greater uptake of H-GNPs as compared to GNPs. Therefore, it is suggested that H-GNPs can be used as an effective carrier for solid tumour targeting.