Construction And Evaluation Of Micellar Carrier Of OHA-VES Nano-polymer Targeting Tumor

Objective Synthesis and characterization of block copolymers oHA-VES.Prepara tion of docetaxel oHA-VES/F68 mixed polymer micelles and study their physical and ch emical properties,and the oHA-VES/F68 in vitro and in vivo evaluation.Methods The amphiphilic block polymer material was synthesized by the amide reaction of HA with VES.The ultrasound was prepared oHA-VES/F68 mixed polymer micelles,investigate the oHA-VES/F68-DTX of morphology,particle size,Zeta potential,coating rate,drug-polymer interactions,and in vitro release,the critical micelle concentration(CMC)was investigated by pyrene fluorescence probe.Using transmission electron microscopy(TEM)and dynamic light scattering particle size instrument melvin on the morphology of nanoparticles,particle size and zeta potential were characterized.Dialysis method is used to investigate in vitro release.Using infrared(FTIR)and nuclear magnetic resonance hydrogen spectrum(1H NMR)identification of oHA-VES.The in vitro cytotoxicity was investigated using the MTT method in cell MCF-7.Fluorescence intensity of polymer micelles in mice was investigated by DiR as a fluorescent probe in vivo.Results Designed oHA-VES polymer through amidation reaction,The ultrasound was prepared oHA-VES/F68 mixed polymer micelles.The designed oHA-VES/F68-DTX showed nearly spherical particles with a mean particle size of(91.2±7.51)and(-10.4±0.47)mV,The EE and DL could reach up to(80.36±1.54)% and(2.69±0.26)%.Under transmission electron microscopy,polymer micelles display regular shape,uniform distribution of particle size.The dissolution rate was 80.74% of the total quantity in 72 hour.IC50 of DTX on MCF-7 cells determined by CCK-8 was 9.3 μg·mL-1,oHA-VES/F68-DTX revealed greater cytotoxicity,while oHA-VES blank micelles showed no cytotoxicity.In vivo imaging experiment showed oHA-VES/F68 polymer micelles in vivo significantly improve the targeting property of polymer micelles.Conclusions The ultrasound was prepared oHA-VES/F68-DTX mixed polymer micelles,this method is simple,exact and convenient.oHA-VES/F68-DTX had a uniform particle size distribution,higher encapsulation efficiency.The result of in vitro cells experiment showed that oHA-VES/F68-DTX has a significant cytotoxicity effect on cells.In vivo experiment showed that oHA-VES/F68-DTX possess excellent targeting ability.oHA-VES prepared via electrostatic attraction was an effective carrier for delivering DTX to tumors.