One-step Synthesis Of Hydrazide/Taurine Mixed Side Group Polymer And Preparation Of Hydrazone Coupled Adriamycin Nanoparticles

Thiolactone derivatives have become a suitable potential platform for developing multifunctional modified polymer prodrugs.Thiolactone ring can release thiofunctional groups such as sulfhydryl which can be used for further reaction through reaction with primary amine,and then add to carbon-carbon double bond which lacks electrons through click reaction.Relevant scientific research results show that thiolactone derivatives have great potential in designing new polymer structures.Therefore,we use hydrazine hydrate,taurine and ethanolamine as mixed aminolysis agents to aminolyze thiolactone to produce sulfhydryl and acryloyl for Michael addition reaction,prepare different thiolactone-acryloyl skeleton in one step,and then connect adriamycin to hydrazine hydrate side chain through acylhydrazone bond,hoping to make the finally prepared polymer adriamycin prodrug nanoparticles have p H responsiveness.Finally,we studied the particle size,stability,drug release and drug loading of the polymer adriamycin prodrug nanoparticles.The preliminary research results show that the polymer skeleton of the polymer nanoparticles can be prepared in one step,and nanoparticles are formed by self-assembly of adriamycin residues and hydrophilicity of sulfonate and hydroxyl groups.The particle size is controlled at about30 nm,which can be stably stored for a long time,with only a small amount of release at p H 7.4,and the release amount can reach 80% at p H 5.0,thus realizing the pH responsiveness of this nano-drug.