Preparaiton And Properties Of C60Nanoparticles As Targeted Prodrug

Now prodrug has become very popular in pharmaceutical field due to the physical andchemical disadvantages of traditional drugs. After reviewing many research papers about drugcarriers and properties of C60, combined with biological application of C60and somefeatures of tumor cells, herein we designed and synthesized a targeted Adriamycine C60prodrug.First C60was reduced to produce hydroxyl groups on its surface, which were thencarboxylated with succinic anhydride. Afterwards we designed an SEG chain with hydrazonebond which would degrade under acid condition, and an SEG folic acid targeted chain; thetwo chains were connected to the surface of carboxylated C60, and then conjugated withAdriamycine and folic acid, thus the folic acid targeted Adriamycine C60prodrug wasobtained. At the same time another prodrug without folic acid targeted chain was prepared asa control group.1H Nuclear Magnetic Resonance Instrument, Liquid Chromatographic-MassSpectrometer, UV-vis Spectrophotometry Meter, Fourier Transform Infrared Spectroscopywere used to confirm the two prodrugs synthesized.The release experiment proves the folic acid targeted C60prodrug have better drugrelease ability in acid condition. Using the fluorescence characteristics of Adriamycine,thetargeted prodrug’s ability to enter the cells was observed and confirmed. Furthermore, C60folic acid targeted prodrug’s and the non-targeted prodrug’s ability to enter HeLa, L929, A540cells was investigated, and experimental results showed that the folic acid targetedAdriamycin prodrug is easier to enter HeLa cells which have folate receptors. MTT testsshowed that the folic acid targeted prodrug can enhance the toxicity toward HeLa cells whichhave folate receptors, but reduced the toxicity to the cells without folate receptors, such asL929and A540.In summary, we combined C60, folic acid and Adriamycine to synthesize a prodrug withgood efficacy and low side effects for cancer treatment. It may offer a new way for treatmentof cancer, and also provide a new approach for prodrug synthesis.