Liu Yi, Tan Feng, Zhao Decheng, Zhang Liwen, Zhang Nianni, Bai Chengwei, Guo Ziyang, Guan Xiongjian, Chen Guanyu
School of Pharmaceutical Sciences (Shenzhen), Sun Yat-sen University Shenzhen Campus, Shenzhen 518107, China.
Pharmaceutics. 2025 Jun 4;17(6):737. doi: 10.3390/pharmaceutics17060737.
Microneedles represent an innovative transdermal drug delivery approach, especially for protein antigens. This study aimed to develop a dual-functional, dissolvable microneedle system loaded with β-glucan and fucoidan in a hyaluronic acid matrix to achieve transdermal immunomodulation and reactive oxygen species (ROS) regulation, exploring its potential in inflammatory disease management and antigen delivery. The microneedles were fabricated using a two-step casting method. Their morphology, mechanical strength, and dissolution kinetics were characterized. In vitro experiments evaluated the ROS-modulating effects on human dermal fibroblasts, while in vivo studies on C57 mice investigated immune activation and lymph node accumulation of ovalbumin antigen. The microneedles exhibited a mechanical strength exceeding 7.45 N/needle and dissolved within 50 s. β-glucan transiently reduced ROS levels at 6 h followed by a rebound, whereas fucoidan sustained ROS suppression after 12 h. In mice, β-glucan-loaded microneedles triggered local immune activation, and fucoidan-incorporated microneedles enhanced ovalbumin accumulation in lymph nodes by 2.1-fold compared to controls. Integrating β-glucan's immunostimulatory and fucoidan's ROS-scavenging/lymphatic-targeting properties within a single microneedle platform offers a promising multifunctional strategy for treating inflammatory diseases and delivering protein antigens.
微针代表了一种创新的经皮给药方法,尤其适用于蛋白质抗原。本研究旨在开发一种双功能、可溶解的微针系统,该系统在透明质酸基质中负载β-葡聚糖和岩藻依聚糖,以实现经皮免疫调节和活性氧(ROS)调节,探索其在炎症性疾病管理和抗原递送方面的潜力。微针采用两步浇铸法制造。对其形态、机械强度和溶解动力学进行了表征。体外实验评估了对人皮肤成纤维细胞的ROS调节作用,而对C57小鼠的体内研究则考察了卵清蛋白抗原的免疫激活和淋巴结聚集情况。微针的机械强度超过7.45 N/针,并在50秒内溶解。β-葡聚糖在6小时时短暂降低ROS水平,随后出现反弹,而岩藻依聚糖在12小时后持续抑制ROS。在小鼠中,负载β-葡聚糖的微针引发局部免疫激活,与对照组相比,掺入岩藻依聚糖的微针使卵清蛋白在淋巴结中的积累增加了2.1倍。在单个微针平台上整合β-葡聚糖的免疫刺激特性和岩藻依聚糖的ROS清除/淋巴靶向特性,为治疗炎症性疾病和递送蛋白质抗原提供了一种有前景的多功能策略。