Department of Pharmaceutics, Srikrupa Institute of Pharmaceutical Sciences, Vill: Velikatta, Mdl: Kondapak, Dist: Siddipet, Telungana state 502277, India.
Department of Pharmaceutics, Srikrupa Institute of Pharmaceutical Sciences, Vill: Velikatta, Mdl: Kondapak, Dist: Siddipet, Telungana state 502277, India.
Int J Biol Macromol. 2019 Mar 15;125:278-289. doi: 10.1016/j.ijbiomac.2018.12.009. Epub 2018 Dec 3.
Combined therapy is a promising approach over its preference to minimize the dose, adverse effects and enhanced therapeutic efficiency in a various diseases including diabetes.
The present research work is to explore combined synergistic anti-diabetic potential of chitosan and pectin with Metformin (CPM) nano-formulation, with special emphasis on effect of Metformin when integrated with bio polymers.
The biohybrid nanoparticles (CPMNP) were formulated by ionic gelation process. The optimized formulation was examined for various in vitro characterizations, in vivo anti-diabetic potential, biodistribution and targeting efficiency.
The optimized biohybrid showed higher content of Metformin 92.1 ± 3.3% and extended release. The pectin coated nanoparticles had smooth spherical morphology with 581.8 nm size and positive surface charge (+41.76 mV). The biohybrid regulated blood glucose, improved the glucose utilization in vital organs, control the dyslipdimea and renal impairment in diabetic rats. CPMNP-4 significantly enhanced the up regulation of IRA, GLUT-2 and GK receptor gene expression and down regulate the TNF-α and IL-6 in pancreas. Also, nanoparticles showed healthier biodistribution simultaneously capability to penetrate in vital organs.
The combined synergistic effects of Metformin and biopolymers are due their corresponding mechanism to enhance glucose uptake, minimized the adverse effects during diabetic therapy.
联合治疗是一种很有前途的方法，它优于最小化剂量、减少不良反应并提高多种疾病（包括糖尿病）的治疗效果。
本研究旨在探索壳聚糖和果胶与二甲双胍（CPM）纳米制剂的协同抗糖尿病作用，特别强调二甲双胍与生物聚合物结合时的效果。
通过离子凝胶化工艺制备生物杂化纳米颗粒（CPMNP）。对优化的配方进行了各种体外特性、体内抗糖尿病潜力、生物分布和靶向效率的研究。
优化的生物杂化显示出更高的二甲双胍含量（92.1±3.3%）和延长的释放。果胶包被的纳米颗粒具有光滑的球形形态，粒径为 581.8nm，表面带正电荷（+41.76mV）。生物杂化物调节血糖，改善重要器官的葡萄糖利用，控制糖尿病大鼠的血脂异常和肾功能损害。CPMNP-4 显著上调了 IRA、GLUT-2 和 GK 受体基因的表达，并下调了胰腺中的 TNF-α和 IL-6。此外，纳米颗粒表现出更健康的生物分布，同时具有穿透重要器官的能力。
二甲双胍和生物聚合物的联合协同作用是由于它们各自的机制，能够增强葡萄糖摄取，减少糖尿病治疗过程中的不良反应。
