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[西他列汀搭载的快速溶解聚合物微针的制备及性能评价]

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

作者信息

Xue Qinglong, Zhuang Jian, Liu Fengyi, Zhang Xiaoning, Li Ming, Huang Yao, Sun Jingyao, Xu Hong, Xu Jiawei

机构信息

Institute of Plastic Machinery and Plastic Engineering (IPME), Beijing University of Chemical Technology, Beijing 100029, China.

Haitian Plastics Machinery Group Co., Ltd., Ningbo 315801, Zhejiang, China.

出版信息

Sheng Wu Gong Cheng Xue Bao. 2024 Jul 25;40(7):2246-2257. doi: 10.13345/j.cjb.230874.

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 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.

摘要

肥胖/超重人群数量的急剧增加是一项全球公共卫生挑战,迫切需要新颖有效的治疗方法。在本研究中,我们设计了一种以西格列汀为治疗肥胖症模型药物的快速溶解聚合物微针阵列贴片(SGN-PVP/PVA-MN),重点关注该贴片的制备过程。然后,我们对SGN-PVP/PVA-MN的形态和尺寸进行了表征。此外,我们深入研究了SGN-PVP/PVA-MN的机械性能、溶解性、皮肤穿刺能力以及透皮药物扩散和释放动力学。结果表明,SGN-PVP/PVA-MN具有良好的形态和机械性能,能够有效穿透角质层并形成微通道以实现快速透皮药物扩散。透皮扩散试验显示,2分钟内药物释放率为64.5%,10分钟内为95.7%。由于溶解迅速且药物扩散效率高,SGN-PVP/PVA-MN有望成为肥胖个体有效且安全的治疗选择。

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