The targeting ligand folic acid (FA) and amphiphilic linoleyl chitosan oligosaccharide (LCOS) with excellent biocompatibility were linked to the carboxyl substituted meso-tetraphenylporphyrin (TPP) of 5-(4-carboxyl)phenyl-10,15,20-triphenyl porphyrin (CPTPP) through acylation reaction. Then the potential drug loading system of CPTPP-FA-LCOS with photosensitive function was obtained. The chemical structure of CPTPP-FA-LCOS was characterized by FTIR, UV-Vis, TEM and fluorescence spectrum. The critical micelle concentration (cmc) of CPTPP-FA-LCOS was also determined using surface tension method. The results showed that cmc value of CPTPP-FA-LCOS was 2.5×10-3 mg/mL. CPTPP-FA-LCOS could be formed into spherical nano-micelles and the particle size was between 70 and 120 nm. The results of preliminary MTT (methyl thiazolyl tetrazolim) suggested that the cell viability was reduced to less than 50% under the light when the concentration of CPTPP-FA-LCOS was 0.4 mg/mL, which suggested the obvious phototoxicity of CPTPP-FA-LCOS.