Synthesis Of Amphiphilic Carrier HA-GMS And Evaluation Of Insulin Microemulsion Carrier

[Objective]To synthesize the amphiphilic compound of HA-GMS,increase HA’s hydrophobicity,enable it easier for the HA-GMS to pass through epithelial cells by the HA carboxyl group with the hydrophobic grouping of glycerol monostearate(GMS).As the carrier of protein and polypeptide drugs,HA-GMS is made into of water-in-oil(W/O)insulin nanoemulsion,optimized to study its physical and chemical properties,to increase insulin’s stability of gastrointestinal tract and improve its bioavailability.[Methods]Synthesize the emphiphilic esterification synthesis glycerol monostearate modified parents sex carrier hyaluronic acid(HA-GMS),by FT-IR and 1H-NMR’s characterization;optimize the prepared blank nanoemulsion’s oil phase,Km value and inner water phase adopting the low-energy emulsification,with the study index of nanoemulsion’s phase area and investigate the influence of the injected HA-GMS preparation to blank nanoemulsion;investigate the external release of nanoemulsion and study the characteristic of W/O nanoemulsion’s releasing curve with the addition of theophylline model;prepared W/O nanoemulsions of linear polypeptide drugs insulin(Insulin,INS),made experiments of physical,chemical properties and enzymatic degradation,and evaluate the pharmacodynamics of Insulin nanoemulsion with big rats as experimental animals.[Results]The experimental results show that:the esterification of hyaluronic acid carboxyl and glycerin monostearate hydroxyl has received success.The high-water-loading insulin microemulsion adding HA-GMS has been successfully prepared,with the content of water around 6%,and the average particle size of 33.9nm.By transmission electron microscopy,it showed the insulin microemulsion was the whole spherical or oval,and the size is relatively uniform.In the resistance enzymatic degradation of insulin microemulsions experiment,after 90 minutes,the insulin residual percentage were respectively 21%and 37%.The pharmacodynamic study showed that insulin has a certain hypoglycemic effect in the body,after 4 hours of rats were gastric,the blood sugar content was70.28%of the initial value,and the effect can last about 12 hours.