HA-GMS-INS胰岛素口服纳米给药系统研究

目的:建立透明质酸-单硬脂酸甘油酿-胰岛素(HA-GMS-INS)口服纳米给药系统,并进行成药性研究.方法:利用酿化反应合成载体HA-GMS,单因素法筛选制备工艺,通过红外光谱和核磁共振氢谱对结构进行表征;采用低能乳化法制备HA-GMS-INS,用多分散激光粒度仪和透射电镜测定纳米乳的粒径及形态,并对胰岛素的体外释放性...

Oral nano drug delivery system of HA-GMS-INS insulin

OBJECTIVE To establish an oral nano-drug delivery system of hyaluronic acid-glycerymonostearate-insulin(HA-GMS-INS). METHODS After preparation by low-energy emulsification,HA-GMS-INS was screened by single-factor method and its structure characterized by infrared spectroscopy and nuclear magnetic resonance hydrogen spectroscopy.Particle size and morphology of nanoemulsion were determined by laser analyzer and transmission electron microscope.And in vitro release performance and anti-enzymatic hydrolysis were also examined.A diabetic mice model was utilized for elucidating its oral hypoglycemic effect. RESULTS The optimized nanoemulsion has a round appearance with an average particle size of 37.19 nm.In release medium of simulated gastric fluid,the cumulative release degree reached around 40%at 2 h;in release medium of simulated intestinal fluid,release completed at 6 h.The experimental results of anti-enzymolysis for pepsin and trypsin demonstrated that insulin-loaded oral nanoemulsion with HA-GMS as a carrier had a certain protective effect on insulin.Compared with another three groups,HA-GMS insulin nanoemulsion had marked hypoglycemic effect and blood glucose level dropped to 72.3%of initial blood glucose level at 6 h after dosing. CONCLUSION Oral nano drug delivery system of HA-GMS-INS may boost the stability of INS in gastrointestinal tract and improve the hypoglycemic effect in diabetic mice.