Supachettapun Chamaiporn, Ali Mohammad Asif, Muangsin Nongnuj, Nguyen Linh Viet, Ho Van Anh, Okajima Maiko K, Kaneko Tatsuo, Matsumura Kazuaki
School of Materials Science, Japan Advanced Institute of Science and Technology, 1-1 Asahidai, Nomi, Ishikawa 923-1292, Japan.
Program in Petrochemistry and Polymer Science, Faculty of Science, Chulalongkorn University, Bangkok 10330, Thailand.
J Mater Chem B. 2025 Jul 10;13(27):8014-8025. doi: 10.1039/d5tb00542f.
Hydrogel microneedles (HMNs) are promising transdermal delivery systems. We prepared HMNs using a mixture of poly(vinyl alcohol) (PVA), sacran, and quaternised sacran (Q-sacran) crosslinked with citric acid (CA). The impact of the polymer composition, crosslinking time, and annealing temperature on the HMN properties was studied. Fourier transform infrared (FT-IR) spectroscopy and thermogravimetric analysis (TGA) revealed the formation of networks composed of polymers containing CA and the corresponding HMNs. The highest swelling degree of HMNs was 440 ± 23%. Mechanical testing confirmed that HMNs were strong enough to penetrate the skin. The PVA/sacran HMNs were durable with a maximum force of 43 ± 1.2 N. These HMNs penetrated the Parafilm®-simulated skin up to 630-760 μm, while PVA/Q-sacran HMNs exhibited a penetration depth of 500 μm. The biocompatibility of HMNs was confirmed through cytotoxicity assays using L929 fibroblasts and B16F1 melanoma cells. The doxorubicin-loaded HMNs exhibited a controlled release profile and a potent anticancer activity against B16F1 melanoma cells. This work suggests that the PVA/sacran and PVA/Q-sacran HMNs can be used as new tools for transdermal drug delivery as mechanically tunable and biocompatible systems.
水凝胶微针（HMNs）是很有前景的经皮给药系统。我们使用聚乙烯醇（PVA）、脱乙酰硫酸软骨素和季铵化脱乙酰硫酸软骨素（Q - 脱乙酰硫酸软骨素）的混合物与柠檬酸（CA）交联制备了HMNs。研究了聚合物组成、交联时间和退火温度对HMN性能的影响。傅里叶变换红外（FT - IR）光谱和热重分析（TGA）揭示了由含CA的聚合物和相应的HMNs组成的网络的形成。HMNs的最高溶胀度为440±23%。力学测试证实HMNs强度足以穿透皮肤。PVA/脱乙酰硫酸软骨素HMNs耐用，最大力为43±1.2 N。这些HMNs穿透Parafilm®模拟皮肤达630 - 760μm，而PVA/Q - 脱乙酰硫酸软骨素HMNs的穿透深度为500μm。通过使用L929成纤维细胞和B16F1黑色素瘤细胞的细胞毒性试验证实了HMNs的生物相容性。载有阿霉素的HMNs表现出控释特性，并对B16F1黑色素瘤细胞具有强大的抗癌活性。这项工作表明，PVA/脱乙酰硫酸软骨素和PVA/Q - 脱乙酰硫酸软骨素HMNs可作为经皮给药的新工具，作为机械可调谐和生物相容的系统。
