聚乙烯醇
透皮
聚合物
材料科学
化学工程
溶解
热稳定性
化学
高分子化学
有机化学
药理学
医学
工程类
作者
Han Liu,Baorui Wang,Mengzhen Xing,Fanda Meng,Suohui Zhang,Guiqin Yang,Aguo Cheng,Chenxin Yan,Bo Xu,Yunhua Gao
标识
DOI:10.1016/j.ijpharm.2023.122863
摘要
As low-temperature storage and transportation of peptides require high costs, improving the dosage form of peptides can reduce costs. We developed a thermostable and fast-releasing stratified dissolving microneedle (SDMN) system for delivering exenatide (EXT) to patients with type 2 diabetes. Among the tested polymers, dextran and polyvinyl alcohol (PVA) were the best at stabilizing EXT under high-temperature storage for 9 weeks. The two polymers possess a relatively high glass transition temperature (Tg) and weak hydrogen bonding between PVA and EXT. Additionally, zinc sulfate (ZnSO4) had a stabilizing effect on EXT among the selected stabilizers, suggesting that EXT formed a dimer after coordination with zinc ions (Zn2+). In addition, the denaturation temperature (Tm) of EXT was increased by adding ZnSO4, thus stabilizing EXT. Accordingly, SDMNs consisting of a tip layer (dextran encapsulating the Zn2+-EXT complex) and a base layer (PVA) were fabricated. Within 2 min of implantation, the EXT loaded on the patch was quickly released into the skin. Transdermal pharmacokinetics studies showed that manufactured SDMNs generated comparable efficacy to subcutaneous injection. Significantly, the remaining EXT amount was not significantly different under storage at 40 °C and -20 °C for 3 months, supporting that the SDMN system had excellent delivery efficiency and stability, thus reducing the dependence on the cold chain.
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