右美托咪定
止痛药
生物相容性
麻醉
材料科学
布比卡因
局部麻醉剂
体内
医学
生物医学工程
药理学
生物
生物技术
冶金
镇静
作者
Wenjing Zhang,Weiguo Xu,Ning Cong,Mingqiang Li,Guoqing Zhao,Wenhao Jiang,Jianxun Ding,Xuesi Chen
出处
期刊:Biomaterials
[Elsevier]
日期:2018-10-01
卷期号:181: 378-391
被引量:63
标识
DOI:10.1016/j.biomaterials.2018.07.051
摘要
Local anesthetics are a class of drugs, which have wide applications in the treatment of acute and chronic pain. However, their analgesic effects only last for a few hours because of their short half-life, which is insufficient for clinical application, especially for long-term surgery or postoperative analgesia. Herein, an injectable hydrogel/microsphere (GEL/MS) composite co-encapsulating bupivacaine (BUP) and dexmedetomidine (DEX) was developed for effective sustained analgesia. The GEL/MS composite appeared as a three-dimensional porous network microstructure and displayed sustained sequential release of DEX and BUP over several days in vitro, without obvious burst release. In this composite, DEX was released from the GEL matrix preferentially, exhibited long-term vasoconstriction effect and improved the local anesthetic concentration at injection site by preventing BUP from diffusing into the blood circulation. BUP was released subsequently from the MS for blockage of the Na+ channel on nerve cell membranes and provided long-term analgesia. In vivo analgesic effect demonstrated that DEX significantly prolonged the effect of analgesia when synergistically administered with BUP in the GEL/MS composite. Moreover, the GEL/MS composite exhibited good biodegradability and biocompatibility in histological analyses. Taken together, the administration of BUP and DEX in the GEL/MS composite achieved a synergistic effect in prolonging analgesia without causing toxicity, and thus represented a potential strategy for long-acting analgesia therapy.
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