| 초록 |
To develop a targeted drug delivery system for cancer therapy, heparin-retinoic acid (HR) and heparin-folic acid-retinoic acid (HFR) amphiphilic bioconjugates were synthesized by chemical conjugation of hydrophobic retinoic acid (RA) and a targeting ligand, folic acid (FA), to the heparin backbone. In aqueous media, the HR and HFR bioconjugates self-assembled to form spherical nanoparticles with varied mean diameter of 100 ~ 200 nm and negatively charged surface (-36 ~ -21 mV), depending on the coupling ratio of RA. From MTT assay, HFR nanoparticles displayed higher cytotoxicity on folate receptor positive KB cells compared to the RA and HR nanoparticles. Furthermore, in a human tumor xenograft nude mouse model, HFR nanoparticles showed higher inhibition of tumor growth than RA and HR nanoparticles. These results indicate that HFR nanoparticles are promising biomaterial for active targeting of folate receptor positive tumor. |
