Preparation of Tegafur-pyropheophorbide Acid A Micelles
Objective To synthesize the conjugate of tegafur and pyropheophorbic acid A.It was loaded into micelles to achieve the synergistic of photodynamic therapy and chemotherapy for antitumor efficiency.Methods Succinic anhydride was used to link tegafur derivative and pyropheophorbic acid A and its structure was characterized by NMR and MS.The loaded micelles were prepared by the solvent evaporation and characterized by drug loading capacity,morphology,particle size,ζ potential as well as antitumor activity in vitro.Results The structure of conjugate was confirmed as desired.The par-ticle size of loaded micelles was 143.9 nm,which was verified by Malvern laser particle size analyzer and transmission elec-tron microscope.The drug loaded micelles could release drug continuously for more than 72 h,and laser irradiation could ac-celerate drug release.The drug loaded micelles irradiated by laser could enhance the anti-tumor effect in vitro,which IC50 value was 14.81 µg·mL-1,and its cytotoxicity increased to 1.43 folds compared with TF administrated only.Conclusion The micelles loaded with tegafur-pyropheophorbic acid A can release tegafur sustainable,and effectively improve the in vitro anti-tumor efficiency.
万方数据
维普
