Department of Pharmaceutics, School of Pharmacy, Anurag University, Hyderabad 500088, India.
Department of Basic Health Sciences, Preparatory Year, Princess Nourah bint Abdulrahman University, Riyadh 11671, Saudi Arabia.
Molecules. 2022 Jul 13;27(14):4470. doi: 10.3390/molecules27144470.
The nano-drug delivery system has gained greater acceptability for poorly soluble drugs. Alogliptin (ALG) is a FDA-approved oral anti-hyperglycemic drug that inhibits dipeptidyl peptidase-4. The present study is designed to prepare polymeric ALG nanoparticles (NPs) for the management of diabetes. ALG-NPs were prepared using the nanoprecipitation method and further optimized by Box−Behnken experimental design (BBD). The formulation was optimized by varying the independent variables Eudragit RSPO (A), Tween 20 (B), and sonication time (C), and the effects on the hydrodynamic diameter (Y1) and entrapment efficiency (Y2) were evaluated. The optimized ALG-NPs were further evaluated for in vitro release, intestinal permeation, and pharmacokinetic and anti-diabetic activity. The prepared ALG-NPs show a hydrodynamic diameter of between 272.34 nm and 482.87 nm, and an entrapment efficiency of between 64.43 and 95.21%. The in vitro release data of ALG-NPs reveals a prolonged release pattern (84.52 ± 4.1%) in 24 h. The permeation study results show a 2.35-fold higher permeation flux than pure ALG. ALG-NPs exhibit a significantly (p < 0.05) higher pharmacokinetic profile than pure ALG. They also significantly (p < 0.05) reduce the blood sugar levels as compared to pure ALG. The findings of the study support the application of ALG-entrapped Eudragit RSPO nanoparticles as an alternative carrier for the improvement of therapeutic activity.
纳米药物传递系统在难溶性药物方面得到了更广泛的认可。阿格列汀（ALG）是一种经美国食品和药物管理局批准的口服抗高血糖药物，可抑制二肽基肽酶-4。本研究旨在制备用于治疗糖尿病的聚合物阿格列汀纳米颗粒（NPs）。采用纳米沉淀法制备 ALG-NPs，并通过 Box-Behnken 实验设计（BBD）进一步优化。通过改变独立变量 Eudragit RSPO（A）、吐温 20（B）和超声时间（C）来优化配方，并评估对水动力直径（Y1）和包封效率（Y2）的影响。进一步评价优化后的 ALG-NPs 的体外释放、肠道渗透、药代动力学和抗糖尿病活性。所制备的 ALG-NPs 的水动力直径在 272.34nm 至 482.87nm 之间，包封效率在 64.43%至 95.21%之间。ALG-NPs 的体外释放数据显示，在 24 小时内呈现出延长的释放模式（84.52±4.1%）。渗透研究结果表明，渗透通量比纯 ALG 高 2.35 倍。ALG-NPs 的药代动力学特征明显（p<0.05）优于纯 ALG。与纯 ALG 相比，它们还能显著（p<0.05）降低血糖水平。研究结果支持将包封 ALG 的 Eudragit RSPO 纳米颗粒作为改善治疗活性的替代载体的应用。
