Faculty of Pharmacy, Isra University, PO Box 22 and 23, Amman, Jordan.
Institute of Applied Dermatopharmacy, Martin Luther University Halle-Wittenberg, Weinbergweg 23, 06120 Halle (Saale), Germany.
Int J Pharm. 2022 Mar 25;616:121511. doi: 10.1016/j.ijpharm.2022.121511. Epub 2022 Jan 26.
In this study, insulin was loaded into non-ionic colloidal carrier systems (CCS) to be used as nano-sized drug delivery systems for transdermal administration. The CCS were characterized for their rheological properties, droplet size and drug loading. Also, the transdermal flux of insulin was estimated using Franz diffusion cells through the epidermis and all the layers of the rats' skin. The efficacy of the administration of the CCS was assessed in vivo transdermally in rats. Based on the rheological properties and droplet size results, the formulated fluids were identified as nano-sized systems having an aqueous colloidal phase, where the hydrophilic peptide is located. Also, a flux of insulin as high as 0.119 ± 0.016 and 1.328 ± 0.047 iu/cmh through the rat's skin and epidermis, respectively, could be achieved using CCSIn2. Moreover, the monitoring of the blood sugar level over 6.5 h after a single transdermal administration of CCS exhibited a slight decrease. However, a significant drop in the blood sugar level was observed when they were administered once every two days over 10 days. The developed insulin-loaded CCS containing the penetration enhancer DMSO are nano-sized drug delivery systems and can induce a delayed therapeutic effect by repeating the administration.
在这项研究中,胰岛素被载入非离子胶体载体系统(CCS)中,用作经皮给药的纳米药物传递系统。CCS 的流变特性、粒径和载药量都得到了表征。此外,还使用 Franz 扩散池通过表皮和大鼠皮肤的所有层来估计胰岛素的经皮通量。CCS 经皮给药的疗效在大鼠体内进行了评估。根据流变特性和粒径结果,所配制的液体被鉴定为纳米级系统,具有亲水性肽所在的水性胶体相。此外,使用 CCSIn2 可以分别实现高达 0.119±0.016 和 1.328±0.047 iu/cmh 的胰岛素经皮和表皮通量。此外,单次经皮给予 CCS 后 6.5 小时监测血糖水平显示略有下降。然而,当在 10 天内每隔两天给予一次时,血糖水平显著下降。含有渗透增强剂 DMSO 的载胰岛素 CCS 是纳米级药物传递系统,通过重复给药可以诱导延迟的治疗效果。