The LM-WSFC with free amine group was purely prepared by salts removal method and identified by spectroscopic assay. The LM-WSFC nanoparticle modified hydrophobically would be used to both of intravenous injection and oral administration of hydrophobic drugs due to their adequate size for administration. We measured NMR, IR, and photon correlation spectroscopy (PCS) to investigate the characteristics of the nanoparticles. The synthesis of hydrophobically modified-chitosan nanoparticles was identified from the results of 1H-NMR, IR spectrum. From the results of surface morphology observed by TEM and AFM, spherical nanoparticles were identified and its size was 30~100 nm. At PCS measurement, the more increase the number of substitutive group, the more decrease the positive charge of nanoparticle surface. Resultantly, nanoparticles using hydrophobically modified-chitosan were tested as a suitable device for the drug targeting system to the tumor cell.