周围神经
效力
渗透(战争)
材料科学
药理学
布比卡因
药品
药物输送
毒性
神经毒剂
神经阻滞
麻醉
医学
纳米技术
体外
化学
解剖
内科学
生物化学
酶
乙酰胆碱酯酶
运筹学
工程类
作者
Yuhao Cai,Qi Li,Ursula Wesselmann,Chao Zhao
标识
DOI:10.1002/adfm.202406876
摘要
Abstract Peripherally injected local anesthetics exhibit limited ability to penetrate peripheral nerve barriers, which limits their effectiveness in peripheral nerve block and increases the risk of adverse effects. In this work, it is demonstrated that exosomes derived from Human Embryo Kidney 293 cells can effectively traverse the perineurium, which is the rate‐limiting barrier within PNBs that local anesthetics need to cross before acting on axons. Based on this finding, these exosomes are used as a carrier for bupivacaine (BUP), a local anesthetic commonly used in clinical settings. The in vitro assessments revealed that the prepared exosomal bupivacaine (BUP@EXO) achieves a BUP loading capacity of up to 82.33% and sustained release of BUP for over 30 days. In rats, a single peripheral injection of BUP@EXO, containing 0.75 mg of BUP, which is ineffective for BUP alone, induced a 2‐h sensory nerve blockade without significant motor impairments. Increasing the BUP dose in BUP@EXO to 2.5 mg, a highly toxic dose for BUP alone, extended the sensory nerve blockade to 12 h without causing systemic cardiotoxicity and local neurotoxicity and myotoxicity.
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