Multivesicular liposomal bupivacaine at the sciatic nerve.
Multivesicular liposomal bupivacaine at the sciatic nerve.
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DOI：
10.1016/j.biomaterials.2014.02.015
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发表时间：
2014-05
期刊：
影响因子：
14
通讯作者：
Kohane, Daniel S.
中科院分区：
文献类型：
--
作者：
McAlvin, J. Brian;Padera, Robert F.;Shankarappa, Sahadev A.;Reznor, Gaily;Kwon, Albert H.;Chiang, Homer H.;Yang, Jason;Kohane, Daniel S.
用于局部麻醉剂的缓释制剂的临床转化受到不良组织反应的限制。Exparel™（DepoFoam布比卡因）是一种新型脂质体局部麻醉剂制剂，其在神经组织附近的生物相容性尚未得到很好的表征。Exparel™注射导致大鼠坐骨神经阻滞持续240分钟，相比之下，0.5%（w/v）盐酸布比卡因为120分钟，1.31%（w/v）盐酸布比卡因为210分钟（布比卡因含量与Exparel™相同）。在注射后4天的组织切片上，Exparel™组中的中值炎症评分（4分中的2.5分）略高于用布比卡因溶液治疗的组（评分2分）。Exparel™组的肌肉毒性评分（6分中的2.5分）与0.5%（w/v）盐酸布比卡因组（3）相似，但显着低于1.31%（w/v）盐酸布比卡因组（5）。两周后，来自Exparel™的炎症（6分中的2分）大于来自0.5%（w/v）盐酸布比卡因（1）的炎症，并且与来自1.31%（w/v）盐酸布比卡因（1）的炎症相似。所有三组的肌毒性无统计学显著差异。在任何组中均未检测到神经毒性。对Exparel™的组织反应与0.5%（w/v）盐酸布比卡因的反应相似。在未来的临床评价中，监测局部组织损伤将非常重要。
Clinical translation of sustained release formulations for local anesthetics has been limited by adverse tissue reaction. Exparel™ (DepoFoam bupivacaine) is a new liposomal local anesthetic formulation whose biocompatibility near nerve tissue is not well characterized. Exparel™ injection caused sciatic nerve blockade in rats lasting 240 minutes compared to 120 minutes for 0.5% (w/v) bupivacaine HCl and 210 minutes for 1.31% (w/v) bupivacaine HCl (same bupivacaine content as Exparel™). On histologic sections four days after injection, median inflammation scores in the Exparel™ group (2.5 of 4) were slightly higher than in groups treated with bupivacaine solutions (score 2). Myotoxicity scores in the Exparel™ group (2.5 of 6) were similar to in the 0.5% (w/v) bupivacaine HCl group (3), but significantly less than in the 1.31% (w/v) bupivacaine HCl group (5). After two weeks, inflammation from Exparel™ (score 2 of 6) was greater than from 0.5% (w/v) bupivacaine HCl (1) and similar to that from 1.31% (w/v) bupivacaine HCl (1). Myotoxicity in all three groups was not statistically significantly different. No neurotoxicity was detected in any group. Tissue reaction to Exparel™ was similar to that of 0.5% (w/v) bupivacaine HCl. Surveillance for local tissue injury will be important during future clinical evaluation.
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