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首页> 外文期刊>Journal of drug targeting >Polymeric alginate nanoparticles containing the local anesthetic bupivacaine.
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Polymeric alginate nanoparticles containing the local anesthetic bupivacaine.

机译:含有局部麻醉药布比卡因的聚合藻酸盐纳米颗粒。

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摘要

Bupivacaine (BVC; S75-R25, NovaBupi(R) is an amide-type local anesthetic. Sodium alginate is a water-soluble linear polysaccharide. The present study reports the development of alginate/bis(2-ethylhexyl) sulfosuccinate (AOT) and alginate/chitosan nanoparticle formulations containing BVC (0.5%). The amounts of BVC associated in the alginate/AOT and alginate/chitosan nanoparticles were 87 +/- 1.5 and 76 +/- 0.9%, respectively. The average diameters and zeta potentials of the nanoparticles were measured for 30 days, and the results demonstrated the good stability of these particles in solution. The in vitro release kinetics showed a different behavior for the release profile of BVC in solution, compared with BVC-loaded alginate nanoparticles. In vitro and in vivo assays showed that alginate-chitosan BVC (BVC(ALG-CHIT)) and alginate-AOT BVC (BVC(ALG-AOT)) presented low cytotoxicity in 3T3-fibroblasts, enhanced the intensity, and prolonged the duration of motor and sensory blockades in a sciatic nerve blockade model.
机译:布比卡因(BVC; S75-R25,NovaBupi®是一种酰胺型局麻药。海藻酸钠是一种水溶性线性多糖。本研究报告了海藻酸钠/双(2-乙基己基)磺基琥珀酸酯(AOT)和含BVC(0.5%)的藻酸盐/壳聚糖纳米颗粒制剂,藻酸盐/ AOT和藻酸盐/壳聚糖纳米颗粒中缔合的BVC量分别为87 +/- 1.5和76 +/- 0.9%。测量了30天的纳米颗粒,结果证明了这些颗粒在溶液中的良好稳定性;与负载BVC的藻酸盐纳米颗粒相比,体外释放动力学显示溶液中BVC的释放曲线具有不同的行为。体内试验表明,藻酸盐-壳聚糖BVC(BVC(ALG-CHIT))和藻酸盐-AOT BVC(BVC(ALG-AOT))在3T3-成纤维细胞中表现出低细胞毒性,增强强度,并延长运动和感觉的持续时间在SC中的封锁睫状神经阻滞模型。

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