Preparation and in vitro anti-tumor activity of hyaluronic acid-glycine-camptothecin polymer micelles
Objective To synthesize hyaluronic acid-glycine-camptothecin polymer micelles(HA-Gly-CPT micelles),evaluate the quality,and to determine its anti-tumor activity in vitro.Methods Glycine was used to connect hyaluronic acid with camptothecin to form an amphiphilic polymer,whose structure was characterized by IR and 1H-NMR.After preparing the micelles by direct dissolution method,the size,Zeta potential,and stability of the micelles were measured by Malvin laser particle size analyzer.The morphology of nano-micelles was observed by transmission electron microscopy.Dialysis was used to determine its pH responsive drug release in vitro.The anti-tumor activity was determined by MTT assay.Results The structure of HA-Gly-CPT was confirmed by IR and 1H-NMR.The HA-Gly-CPT micelles were spherical with an average particle size of(279.86±4.15)nm and a Zeta potential of(～20.17±0.52)mV.The release rate of camptothecin reached 50％in an acidic medium(pH 5.0)after 48 hours.MTT experiment showed that HA-Gly-CPT micelles had no significant cytotoxicity on the normal L929 cells,while the micelles inhibited the growth of MCF-7 by more than 80％at a concentration of 50 μg·mL-1.Conclusion Amphiphilic polymers and pH responsive HA-Gly-CPT micelles are successfully synthesized,confirming the obvious anti-tumor activity in vitro of HA-Gly-CPT micelles.
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