搭载西他列汀的速溶型聚合物微针的制备与性能评价

Preparation and performance evaluation of fast dissolving polymer microneedles piggybacked with sitagliptin

摘要:

全球肥胖/超重人数急剧上升，逐步成为一个全球公共卫生难题，因此迫切需要有效的治疗手段。本研究设计了一种新型治疗肥胖的西他列汀模型药物速溶型聚合物微针阵列贴片(sitagliptin-PVP/PVA-microneedles, SGN-PVP/PVA-MN)，重点研究了该贴片的制备工艺，对微针阵列的形貌尺寸进行了表征，并探究了SGN-PVP/PVA-MN的力学性能、皮肤穿刺性能、溶解性能以及药物扩散性能。结果表明SGN-PVP/PVA-MN具备良好的形貌和力学性能，能够有效穿透皮肤角质层并开启微通道，实现药物的迅速透皮扩散。体外药物透皮扩散试验表明SGN-PVP/PVA-MN在2 min内释放了64.5%的药物，在10 min内释放95.7%的药物。SGN-PVP/PVA-MN具有快速溶解特性和较高药物扩散效率，可为肥胖症患者提供一种有效、安全的治疗选择。

Abstract:

The dramatic rise in the number of obese/overweight people is a global public health challenge that urgently requires novel and effective therapies. In this study, we designed a fast dissolving polymer microneedle array patch (SGN-PVP/PVA-MN) with sitagliptin as a model drug for treating obesity, focusing on the preparation process of the patch. We then characterized the morphology and dimensions of SGN-PVP/PVA-MN. Furthermore, we delved into the mechanical properties, solubility, skin-puncturing capability, and transdermal drug diffusion and release kinetics of SGN-PVP/PVA-MN. The results demonstrated that SGN-PVP/PVA-MN exhibited favorable morphology and mechanical properties, effectively penetrating the stratum corneum and creating microchannels for rapid transdermal drug diffusion. The in vitro transdermal diffusion assays revealed the release of 64.5% of the drug within 2 min and 95.7% within 10 min. With rapid dissolution and high drug diffusion efficiency, SGN-PVP/PVA-MN is poised to serve as an effective and safe treatment option for the individuals with obesity.