高溶解和低溶解局部麻醉剂的共同晶体双向调节它们的释放,以长效止痛
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Updated: Jan 9, 2026

Intracranial Pharmacotherapy and Pain Assays in Rodents
Published on: April 9, 2019
Yujun Zhang1, Weiwei Wu1, Jing Liu1
1Department of Anesthesiology, West China Hospital, Sichuan University, Chengdu, China; Laboratory of Anesthesia and Critical Care Medicine, National-Local Joint Engineering Research Centre of Translational Medicine of Anesthesiology, West China Hospital, Sichuan university, Chengdu, China.
这项研究引入了一种新的共同晶体策略,使用类纳米颗粒来控制局部麻醉剂的释放. 这种方法为有效的疼痛管理提供了有希望的长效麻醉制剂.
科学领域:
- 制药科学 制药科学
- 材料科学 材料科学 材料科学
- 纳米技术 纳米技术
背景情况:
- 设计长效药物配方在控制具有不同溶解度的药物的释放方面面临挑战.
- 高溶性药物需要缓解释放,而溶性较差的药物需要增强释放以获得治疗效果.
研究的目的:
- 用纳米粒子开发一种具有不同溶解度的局部麻醉剂的共同晶体策略.
- 为了实现对药物释放动态的双向控制,以改善长效配方.
主要方法:
- 设计者自组装纳米颗粒被用于通过静电相互作用形成与QX314-OH (高度溶解) 和levobupivacaine (不溶解) 的纳米复合体.
- 药物的联合结晶是通过 π-π 堆叠和纳米复合体内的结合来诱导的.
- 由此产生的共同晶体在氨酸水凝中配制,用于控制释放研究.
主要成果:
- 同晶体配方显示QX314-OH的缓慢释放和levobupivacaine的加速释放.
- 利沃布皮瓦卡因通过促进其细胞内积累来增强QX314-OH的疗效.
- 该配方在多种动物模型中表现出长期作用的止痛作用,具有良好的安全性.
结论:
- 同晶体策略有效地提供了对具有不同溶解度的药物的释放的双向控制.
- 这种方法为临床疼痛控制应用提供了一个有前途的长效麻醉制剂.
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