Sciatic nerve blockade with lipid-protein-sugar particles containing bupivacaine
Sciatic nerve blockade with lipid-protein-sugar particles containing bupivacaine
复制标题
DOI：
10.1023/a:1026470831256
复制
发表时间：
2000-10-01
影响因子：
3.7
通讯作者：
Langer, R
中科院分区：
文献类型：
--
作者：
Kohane, DS;Lipp, M;Langer, R
目的.评估脂蛋白糖颗粒（LPSP）通过经皮注射提供长时间局部麻醉的有效性。方法。在体外表征和优化含布比卡因的LPSP。雄性Sprague-Dawley大鼠接受含布比卡因LPSP的坐骨神经阻滞。在后爪中测量感觉和运动神经阻滞，以及对侧功能缺陷（全身药物分布的测量）。以聚乳酸-羟基乙酸（PLGA）微球为对照。10%（w/w）布比卡因LPSP（60%二棕榈酰磷脂酰胆碱）的直径为4.4 ± 0.39 μ m，振实密度为0.11 ± 0.04 μ g/ml。这些LPSP和50%（w/w）PLGA微球具有相当的感觉阻滞持续时间（468 +/- 210 min vs. 706 +/- 344 min，p = 0.08），尽管LPSP产生的运动阻滞持续时间短得多（508 +/- 258 min vs. 1062 +/- 456 min，p = 0.005）。两组的全身毒性均极轻微。LPSP提供的感觉阻滞持续时间与PLGA微球相当，载药量较低。LPSP的运动阻滞时间比PLGA微球短。LPSP似乎适用于延长神经阻滞。考虑到它们的大小和低密度，它们可能对气道的表面麻醉有用。
Purpose. To assess the efficacy of lipid-protein-sugar particles (LPSPs) in providing prolonged duration local anesthesia by percutaneous injection.Methods. Bupivacaine-containing LPSPs were characterized and optimized in vitro. Male Sprague-Dawley rats were given sciatic nerve blocks with bupivacaine-containing LPSPs. Sensory and motor nerve blockade were measured in the hindpaw, as were contralateral functional deficits (a measure of systemic drug distribution). Poly(lacticco-glycolic) acid (PLGA) microspheres were used as a reference.Results. 10% (w/w) bupivacaine LPSPs (60% dipalmitoylphosphatidylcholine) were 4.4 +/- 0.39 mum in diameter, with a tap density of 0.11 +/- 0.04 g/ml. These LPSPs and 50% (w/w) PLGA microspheres had comparable durations of sensory blockade (468 +/- 210 min vs. 706 +/- 344 min, p = 0.08), although the LPSPs produced a much lesser duration of motor blockade (508 +/- 258 min vs. 1062 +/- 456 min, p = 0.005). Systemic toxicity was minimal in both groups.Conclusions. LPSPs provide sensory blockade durations comparable to those from PLGA microspheres, with a smaller amount of drug loading. Motor blockade is shorter with LPSPs than with PLGA microspheres. LPSPs appear to be suitable for extended nerve blockade. Given their size and low density, they may be useful for topical anesthesia of the airway.