磁响应利多卡因微球的制备及其用于兔坐骨神经阻滞的效果  

Preparation of magnetic lidocaine microsphere and effects on sciatic nerve block in rabbits

作　　者：喻谦 郑灵希 李强 卢晓英[2] 郑传东 Yu Qian;Zheng Lingxi;Li Qiang;Lu Xiaoying;Zheng Chuandong(Department of Anesthesiology,the Third People′s Hospital of Chengdu,Southwest Jiaotong University,Chengdu 610031,China;Key Laboratory for Advanced Technologies of Materials,Ministry of Education School of Material Science and Engineering,Southwest Jiaotong University,Chengdu 611756,China)

机构地区：[1]西南交通大学附属医院,成都市第三人民医院麻醉科,成都610031 [2]材料先进技术教育部重点实验室、西南交通大学材料科学与工程学院,成都611756

出　　处：《中华麻醉学杂志》2022年第11期1343-1347,共5页Chinese Journal of Anesthesiology

基　　金：四川省卫生健康委员会医学科技项目(21PJ142)。

摘　　要：目的:拟制备磁响应利多卡因微球并评价其用于兔坐骨神经阻滞的效果。方法:通过W 1/O/W 2复乳法制备磁响应利多卡因微球,观察其体外表征,通过磁强计测量微球磁响应参数,并绘制磁滞回线。计算包封率、载药率,绘制体外释放曲线。选取健康家兔15只,雌雄各半,5~6月龄,体重3.0~3.5 kg。根据随机数字表法分为3组(n=5):磁响应利多卡因微球组(PL组)、生理盐水对照组(C组)和利多卡因组(L组),分别将磁响应利多卡因微球缓释剂2 ml、生理盐水2 ml、2%利多卡因2 ml通过导管注入家兔坐骨神经周围。并于注药后60 h撤除磁铁。于注药前(T_(0))、注药后30 min(T_(1))、2 h(T_(2))、8 h(T_(3))、16 h(T_(4))、24 h(T_(5))、48 h(T_(6))、60 h(T_(7))、62 h(T_(8))和64 h(T_(9))时测定双侧坐骨神经干复合动作电位和传导速度,采用趾张反射评分和改良Tarlov评分评定阻滞效果。结果:磁响应利多卡因微球粉末为棕色,扫描电镜下观察成单分散、规整的球形,直径为(9±3)μm。在无外加磁场的情况时,磁滞回线经过原点,且无磁滞现象产生。包封率为46.18%,载药量为6.02%,60 h体外释放率达到97%。与C组比较,PL组T_(1)~T_(8)时坐骨神经动作电位和传导速度、趾张反射评分和改良Tarlov评分降低(P<0.05);与L组比较,PL组T_(1)时坐骨神经动作电位和传导速度升高,T_(2)~T_(8)时动作电位降低,T_(3)~T_(8)时传导速度降低,趾张反射评分T_(1)时升高,T_(3)~T_(8)时降低,改良Tarlov评分T_(1)、T_(2)时升高,T_(3)~T_(8)时降低(P<0.05)。结论:本研究成功制备磁响应利多卡因微球,具有良好的磁响应性和缓释性,可显著延长兔坐骨神经阻滞时间。Objective To develop a novel sustained-release local anesthetic microspheres and evaluate the effects on sciatic nerve block in rabbits.Methods The magnetic lidocaine microspheres were prepared by W_(1)/O/W_(2) compound emulsion method,investigating their external morphology,measuring the magnetic response characteristics by the VSM and draw the hysteresis loop.The encapsulation efficiency and drug-loading rate were calculated,and the cumulative release curves in vitro were drawn.Fifteen healthy rabbits(half male and half female),aged 5-6 months,weighing 3.0-3.5 kg,were selected for sciatic nerve block and divided into 3 groups(n=5 each)using a random number table method:magnetic response lidocaine microspheres group(PL group),normal saline control group(C group)and lidocaine group(L group).Magnetic response lidocaine microsphere buffer 2 ml,normal saline 2 ml and 2%lidocaine 2 ml were injected around the rabbit sciatic nerve through a catheter in PL,C and L groups,respectively.The applied magnetic field was withdrawn at 60 h after injection.Before injection(T_(0))and at 30 min and 2,8,16,24,48,60,62 and 64 h after injection(T_(1-9)),the compound action potentials and conduction velocities of bilateral sciatic nerve trunks were measured,and block was assessed using toe reflex score and modified Tarlov score.Results The magnetic lidocaine microspheres were brown in color and observed as monodisperse,regular spheres with a diameter of(9±3)μm,an encapsulation rate of 46.18%,a drug loading of 6.02%,and a superparamagnetic release rate of 97%in vitro at 60 h.The hysteresis loop passed through the origin and no hysteresis occurred with the absence of an external magnetic field.Compared with C group,the action potentials and conduction velocities of the sciatic nerve,toe reflex score and modified Tarlov score were significantly decreased at T_(1)-T_(8)in PL group(P<0.05).Compared with L group,the action potentials and conduction velocities of the sciatic nerve were significantly increased at T_(1),the action potential

关 键 词：利多卡因 微球体 磁性 神经传导阻滞 聚乳酸羟基乙酸 

分 类 号：R614[医药卫生—麻醉学]