温敏型水凝胶包载布比卡因对延长神经阻滞时间的研究

Prolongation of nerve blockade ultilizing thermogel-retarding bupivacaine compounds

目的 为了延长单次注射局部麻醉药制剂所产生的作用时间,将临床上常见水溶性局麻药包载于可注射的、生物可降解的、温度敏感性的水凝胶中,研究坐骨神经阻滞延长的效果,同时对水凝胶生物相容性进行评价。方法对20只大鼠分为4组,分别给予大鼠随机分为4组,每组5只大鼠,乙醚吸入麻醉后行坐骨神经阻滞术,分别给予:1)0.75wt.%BUP·HCl溶液PBS(对照组);2)0.75wt.%BFB Pluronic F127水凝胶,称为Pluronic F127/BFB;3)0.75wt.%BFB PAla-PEG-PAla水凝胶,PAla-PEG-PAla/BFB;4)0.75wt.%BFBPLGA-PEG-PLGA水凝胶,标记为PLGA-PEG-PLGA/BFB,并对阻滞效果进行评估。结果痛觉复苏的顺序(由早到晚)为BUP·HCl>PLGAPEG-PLGA/BFB>PAla-PEG-PAla/BFB>Pluronic F127/BFB。运动机能比痛觉功能更快恢复。所有大鼠均未观察到明显的神经毒性,但局部肌肉组织炎症反应明显。结论 水凝胶能够显著延长布比卡因的作用时间,且水凝胶的降解时间与局部的组织反应严重程度成反比。

Objective To extend the local anesthetic effect from a single injection,we made hydrophobic alkaline of bupivacaine from clinically common ultilized water-soluble local anesthetics,and package it into biodegradable,temperature-sensitive hydrogels.Applying the new kind of local anesthetics encapsulation agents to extend the effect of sciatic nerve block has been researched,at the same time,local tissue reaction of the injection site has also been explored.Methods Rats underwent sciatic nerve block,sensory blockade and motor block was evaluated.Results The order of sensory recovery(earliest to last)was as follows:BUP·HCl>PLGA-PEG-PLGA>PAla-PEG-PAla>Pluronic F127.Motor function appears to return to normal faster than sensory function.An inflammatory response was apparent in the PAlaPEG-PAla and PLGA-PEG-PLGA groups.Nerve damage was not present in any group.Conclusion Choosing a biomaterial with a residue time similar to that of the drug’s intended duration may improve the therapeutic benefits while minimizing toxic side effects.