介孔碳纳米粒改善格列美脲降糖效果的临床观察

Clinical Observation on the Hypoglycemic Effect of Glimepiride Improved by Mesoporous Carbon Nanoparticles

目的采用介孔碳纳米球(mesoporous carbon nanospheres,MCN)来包载格列美脲(glimepiride,GM)改善其水溶性,并考察包载后的降糖效果。方法以MCN为载体,通过吸附法包载格列美脲,通过透射电镜考察纳米粒的结构和粒径大小,通过差示扫描量热法对载药体系进行表征,通过MTT实验和细胞摄取实验考察载体对Caco-2细胞毒性和Caco-2细胞对载体的摄取能力,通过药效学实验考察格列美脲介孔碳纳米粒的降糖效果。结果成功制备MCN表征结果显示呈规则的球形,粒径约为100 nm,并且药物以无定型的形式存在于MCN的孔隙中,对于Caco-2细胞基本无毒,并且Caco-2细胞对其有较高的摄取,药效学结果显示格列美脲介孔碳纳米粒的降糖效果明显。结论MCN能够改善格列美脲的水溶性,提高降糖效果。

Objective To improve the water solubility of glimepiride(GM)with mesoporous carbon nanospheres(MCN),and investigate the hypoglycemic effect of the drug.Methods With MCN as the carrier,glimepiride was encapsulated by adsorption method,the structure and size of the nanoparticles were observed by transmission electron microscope,and the drug-loaded system was characterized by differential scanning calorimetry.Cytotoxicity of the carrier to Caco-2 cells and the uptake ability of the carrier by Caco-2 cells were investigated by MTT assay and cell uptake assay.Results MCN was successfully prepared.The characterization results showed that the drug was spherical with a diameter of about 100 nm,and the drug existed in the pores of MCN in an amorphous form.The drug was basically non-toxic to Caco-2 cells and Caco-2 cells had a high uptake of it.The pharmacodynamic results showed that glimepiride mesoporous carbon nanoparticles had obvious hypoglycemic effect.Conclusion MCN can improve the water solubility of glimepiride and improve the hypoglycemic effect.