Combination of 5-fluorouracil and low molecular weight hyaluronic acid improves efficiency of the targeting to tumors

摘要

Purpose: To develop a new HA-5-FU conjugates to improves efficiency of the targeting to tumors. Methods: HA-5-FU conjugates were synthesized by using adipicdihydrazide as a linker. Using MTT method of A2780, HepG2, Hela for cell model in vitro to evaluate the antitumor activity of HA-5-FU and 5-FU. Biodistribution of HA-5-FU in tumor-bearing mice was determined by HPLC assay. Results: The inhibition of conjugates to the A2780 and HepG2 cells show the drug was concentration-dependent and time-dependent. Biodistribution in vivo showed that HA-5-FU extended the half life of 5-FU in plasma and the retention time in tumors which demonstrated the targeting to tumors. Conclusion: The HA-5-FU conjugates can extend the circulation time of drugs in plasma and enhance the therapeutic effect of drugs on tumors.