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罗哌卡因乳酸羟基乙酸共聚物微球在小鼠的坐骨神经阻滞时效及生物相容性 被引量:8

The pharmacodynamics and biocompatibility of ropivacaine loading poly(lactide-co-glycolide) microspheres in mice
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摘要 目的研究罗哌卡因乳酸羟基乙酸共聚物微球(RVP-PLGA-MS)在小鼠的坐骨神经阻滞时效及体内的生物相容性。方法雌性昆明小鼠25只,双侧坐骨神经旁分别植入RVP-PLGA-MS和乳酸羟基乙酸共聚物空白微球(PLAC-PLGA-MS)建立动物模型(每侧植药量为400mg/kg)。按微球植入后4、10、18、30、48h分为A、B、C、D、E五组,以PLAC-PLGA-MS植入侧为对照,采用热踏板法及4-point scale评分测定小鼠坐骨神经的阻滞效应。考察小鼠RVP-PLGA-MS植入侧手术切口情况,坐骨神经、周围组织及全身主要脏器的病理学变化研究其生物相容性。结果微球植入后4~30h小鼠RVP-PLGA-MS植入侧肢体感觉阻滞时间明显较PLAC-PLGA-MS植入侧长(P<0.05)。PLAC-PLGA-MS植入侧肢体运动均未受阻滞,4-point scale评分均为1分;RVP-PLGA-MS植入侧在药物植入后4h至30h4-point scale评分为1~3分,明显高于PLAC-PLGA-MS侧,运动阻滞轻微(P<0.05),48h后感觉运动阻滞恢复。RVP-PLGA-MS植入侧手术切口未见明显的炎症反应;神经及附近组织病理切片仅见轻微炎症改变,全身主要脏器无病理学改变。结论RVP-PL-GA-MS在小鼠体内可显著延长罗哌卡因的作用时效,且组织相容性好。 Objective To evaluate the efficacy and bioeompatibility of a newformulation of ropivacaine loaded in an fatty acid based biodegradable polymer poly (PLGA) when implanted near the sciatic nerve of mice. Methods Twenty five Kunming mice were implanted with the polymer ropivaeaine microspheres( RVD-PLGA-MS) 400 mg/kg and the placebo microspheres( PLAC-PLGA- MS) 400 mg/kg nearby the two scialic nerves, respectively, which were randomly divided into five grouds of A,B,C,D and E by the implantation time points of 1,10, 18,30 and 48 h. The efficacy of the polymer drug combination was determined by measuring the sensory and motor nerve blockade for 48 h. Sensory tests were performed using YLS-6B hot plate, the latency to withdraw the hide paw from the hot plate used as the respond time to the thermal nociception. Motor tests were performed to examine the ability to splay and flex of the bind paw by 1-point scale. The disposed mice were sacrificed one week later,and microscopic examination of the main internal organs and the tissues of implanted sites was performed. Results From t to 30 h after implantation, the microspheres in mice, the withdrawal latency of the polymer-ropivacaine microspheres sides were longer in the mice implanted RVP-PLGA MS than those implanted PLAC-PLGA-MS(P〈0.05). The 4-point scale of motor tests showed that, at 4 to 30 h, the polymer ropivacaine microspheres sides were 1-3, the placebo microspheres sides were 1, the sensory and motor nerve blockade recovered after 48 h. Microscopic examination of the implanted sites revealed that only mild infiltration in examined tissues with no pathological findings for internal organs were found. Conclusion Polymer ropivacaine microspheres can prolong analgesic eficacy of ropivacaine and has good biocompatibility in mice.
出处 《临床麻醉学杂志》 CAS CSCD 北大核心 2010年第2期148-150,共3页 Journal of Clinical Anesthesiology
关键词 镇痛 罗哌卡因乳酸羟乙基乙酸共聚物微球 生物相容性 Analgesia Polymer-ropivacaine microsphcres Biocompatibility
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参考文献7

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二级参考文献6

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