通过可溶解微针(LH-DMNs)增强盐酸利多卡因的透皮给药用于快速局部麻醉
Enhanced Transdermal Delivery of Lidocaine Hydrochloride via Dissolvable Microneedles (LH-DMNs) for Rapid Local Anesthesia.
作者信息
Bian Shengtai, Chen Jie, Chen Ran, Feng Shilun, Ming Zizhen
机构信息
Microfluidics Research & Innovation Laboratory, School of Sport Science, Beijing Sport University, Beijing 100084, China.
Health Service Center of Qingshanhu Subdistrict Community, Hangzhou 311300, China.
出版信息
Biosensors (Basel). 2025 Aug 21;15(8):552. doi: 10.3390/bios15080552.
Microneedles represent an emerging transdermal drug delivery platform offering painless, minimally invasive penetration of the stratum corneum. This study addresses limitations of conventional lidocaine hydrochloride formulations, such as slow onset and poor patient compliance, by developing lidocaine hydrochloride-loaded dissolvable microneedles (LH-DMNs) for rapid local anesthesia. LH-DMNs were fabricated via centrifugal casting using polyvinyl alcohol (PVA) as the matrix material in polydimethylsiloxane (PDMS) negative molds, which imparts high mechanical strength to the microneedles. Biocompatibility assessments showed negligible skin irritation, resolving within 3 min. And drug-loading capacity reached 24.0 ± 2.84 mg per patch. Pharmacodynamic evaluation via mouse hot plate tests demonstrated significant analgesia, increasing paw withdrawal latency to 36.11 ± 1.62 s at 5 min post-application ( < 0.01). The results demonstrated that the LH-DMNs significantly elevated the pain threshold in mice within 5 min, surpassing the efficacy of conventional anesthetic gels and providing a rapid and effective solution for pain relief. These findings validate the system's rapid drug release and efficacy, positioning dissolvable microneedles as a clinically viable alternative for enhanced transdermal anesthesia.
微针代表了一种新兴的经皮给药平台,可实现无痛、微创穿透角质层。本研究通过开发用于快速局部麻醉的载盐酸利多卡因的可溶微针(LH-DMNs),解决了传统盐酸利多卡因制剂起效缓慢和患者依从性差等局限性。LH-DMNs是通过离心浇铸法制备的,以聚乙烯醇(PVA)为基质材料,在聚二甲基硅氧烷(PDMS)阴模中成型,这赋予了微针较高的机械强度。生物相容性评估显示皮肤刺激性可忽略不计,在3分钟内即可消退。每片微针的载药量达到24.0±2.84毫克。通过小鼠热板试验进行的药效学评估显示出显著的镇痛效果,给药后5分钟时,爪部缩回潜伏期增加至36.11±1.62秒(P<0.01)。结果表明,LH-DMNs在5分钟内显著提高了小鼠的痛阈,超过了传统麻醉凝胶的疗效,为缓解疼痛提供了一种快速有效的解决方案。这些发现证实了该系统的快速药物释放和疗效,将可溶微针定位为增强经皮麻醉的一种临床上可行的替代方案。