Development and Characterization of a Glimepiride-Loaded Gelatin-Coated Mesoporous Hollow Silica Nanoparticle Formulation and Evaluation of Its Hypoglycemic Effect on Type-2 Diabetes Model Rats
Development and Characterization of a Glimepiride-Loaded Gelatin-Coated Mesoporous Hollow Silica Nanoparticle Formulation and Evaluation of Its Hypoglycemic Effect on Type-2 Diabetes Model Rats
复制标题
格列美脲明胶包覆介孔中空二氧化硅纳米颗粒制剂的开发和表征及其对 2 型糖尿病模型大鼠的降血糖作用评价
DOI：
10.1089/adt.2020.987
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发表时间：
2020
影响因子：
1.8
通讯作者：
Lin Rong
中科院分区：
文献类型：
--
作者：
Yu XueWen;Liu Tao;Lin Rong
本研究制备了明胶包覆的介孔二氧化硅空心纳米球（GSN）作为药物载体，以提高格列美脲（GLM）的水溶性和调节其释放速率。采用吸附法将GLM负载到GSN中，并利用差示扫描量热仪（DSC）和X射线衍射仪（XRD）对载药样品（GLM-GSN）进行表征。进行了大鼠细胞摄取实验和在体肠摄取实验。此外，还进行了体外药物溶出度、药动学和药效学实验。GLM-GSN具有良好的载药量（39.7% ± 0.7%）和缓释效果。DSC和XRD结果表明，GSN中的GLM为非晶态。细胞吸收实验和在体肠吸收实验表明GSN可被有效吸收，MTT实验表明GSN具有良好的生物相容性。此外，GLM-GSN在药代动力学实验中具有较高的生物利用度，在药效学实验中对2型糖尿病模型大鼠具有显著的降血糖作用。这项研究清楚地表明，GSN是一个有前途的平台，提供GLM治疗2型糖尿病。
In this study, we prepared gelatin-coated mesoporous hollow silica nanospheres (GSN) as a drug carrier to improve the water solubility and regulate the release rate of glimepiride (GLM). GLM was loaded into GSN by an absorption method, and drug-loaded samples (GLM-GSN) were characterized by differential scanning calorimeter (DSC) and X-ray diffraction (XRD). Cellular uptake andin vivointestinal uptake experiments were performed in rats. In addition, the studies ofin-vitrodrug dissolution, pharmacokinetics, and pharmacodynamic experiments also were performed. GLM-GSN showed excellent drug loading (39.7% ± 0.7%) and sustained GLM release. The state of GLM in GSN was amorphous according to DSC and XRD results. Cellular uptake andin vivointestinal uptake experiments indicated that GSN could be effectively absorbed, and an MTT experiment demonstrated that GSN had good biocompatibility. Furthermore, the GLM-GSN had a higher bioavailability in pharmacokinetics experiments and a prominent hypoglycemic effect on type-2 diabetes model rats in pharmacodynamic experiments. This study clearly shows that GSN is a promising platform for delivering GLM for the treatment of type-2 diabetes.