Jang You Jin, Lee Jin Ho, Seo Tae Beom, Oh Se Heang
Department of Nanobiomedical Science, Dankook University, Cheonan 31116, Republic of Korea.
Department of Advanced Materials, Hannam University, Daejeon 34054, Republic of Korea.
Eur J Pharm Biopharm. 2017 Jun;115:113-121. doi: 10.1016/j.ejpb.2017.02.007. Epub 2017 Feb 21.
Local anesthetics are adopted in clinical practice to manage the perioperative and/or postoperative pain. However, their relatively short duration of action limit their ability to meet clinical needs. Herein, we prepared a lidocaine/multivalent ion complex (icLD) using aqueous solutions containing positively charged LD and a multivalent counter-ion as a system for producing prolonged anesthesia. The results of the in vitro and in vivo experiments indicated that the icLD facilitates prolonged LD release even without adjuvants and thus provides nerve blockade for a long duration of action (∼14h) without further increase in neurotoxicity than the LD itself. These findings suggested that the icLD could be a practical strategy for effectively controlling perioperative and/or postoperative pain in clinical practice.
局部麻醉药在临床实践中用于处理围手术期和/或术后疼痛。然而,它们相对较短的作用时间限制了其满足临床需求的能力。在此,我们制备了一种利多卡因/多价离子复合物(icLD),使用含有带正电荷的利多卡因(LD)和多价抗衡离子的水溶液作为产生延长麻醉作用的系统。体外和体内实验结果表明,即使没有佐剂,icLD也有助于延长LD的释放,从而提供长时间的神经阻滞作用(约14小时),且与LD本身相比,神经毒性不会进一步增加。这些发现表明,icLD可能是临床实践中有效控制围手术期和/或术后疼痛的一种实用策略。