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Nanocomplex System of Bupivacaine with Dextran Sulfate for Parenteral Prolonged Delivery
Bulletin of the Korean Chemical Society ( IF 2.3 ) Pub Date : 2020-09-27 , DOI: 10.1002/bkcs.12098 Hyung Tae Kim 1 , Jun Soo Park 1 , Myung Joo Kang 1
Bulletin of the Korean Chemical Society ( IF 2.3 ) Pub Date : 2020-09-27 , DOI: 10.1002/bkcs.12098 Hyung Tae Kim 1 , Jun Soo Park 1 , Myung Joo Kang 1
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An electrostatic complex system of bupivacaine (BUP), an amide‐type analgesic agent, with an oppositely charged polymer was designed for parenteral sustained delivery. The complex was prepared by admixing the drug (0.25–1.0% w/v) with different anionic polymers (dextran sulfate, carboxymethylcellulose, or carboxymethyl dextran, 1.0–5.0% w/v), and then adding calcium ion (0–1.0% w/v) as the noncovalent crosslinking agent. Negatively charged complexes ranging from 10 to 2000 nm were formed after the positively charged BUP molecules amalgamated with the polymers after gentle agitation. Drug released from the complex was markedly sustained either by increasing the polymer to drug ratio, or by increasing the calcium ion content. The optimized nanocomplex consisted of the drug, dextran sulfate, and calcium ion at the ratio of 1:20:20 w/w/w, which supplied a sustained release profile over 7 days. Therefore, novel nanocomplex is expected to be an effective tool to provide a sustained release of the analgesic agent.
中文翻译：
布比卡因与硫酸葡聚糖的纳米复合系统用于肠胃外延长递送
布比卡因（BUP）是一种酰胺类镇痛剂，带有带相反电荷的聚合物的静电复合体系是为肠胃外持续给药而设计的。通过将药物（0.25–1.0％w / v）与不同的阴离子聚合物（硫酸葡聚糖，羧甲基纤维素或羧甲基葡聚糖，1.0–5.0％w / v）混合，然后添加钙离子（0–1.0％ w / v）作为非共价交联剂。轻度搅拌后，带正电荷的BUP分子与聚合物合并后，形成10至2000 nm的带负电荷的复合物。通过增加聚合物与药物的比例或增加钙离子含量，可以显着维持从复合物中释放出的药物。优化的纳米复合物由药物，硫酸葡聚糖和钙离子组成，比例为1:20:20 w / w / w，在7天内提供了持续释放特性。因此，新型的纳米复合物有望成为提供止痛剂持续释放的有效工具。
更新日期：2020-10-19
中文翻译：
布比卡因与硫酸葡聚糖的纳米复合系统用于肠胃外延长递送
布比卡因（BUP）是一种酰胺类镇痛剂，带有带相反电荷的聚合物的静电复合体系是为肠胃外持续给药而设计的。通过将药物（0.25–1.0％w / v）与不同的阴离子聚合物（硫酸葡聚糖，羧甲基纤维素或羧甲基葡聚糖，1.0–5.0％w / v）混合，然后添加钙离子（0–1.0％ w / v）作为非共价交联剂。轻度搅拌后，带正电荷的BUP分子与聚合物合并后，形成10至2000 nm的带负电荷的复合物。通过增加聚合物与药物的比例或增加钙离子含量，可以显着维持从复合物中释放出的药物。优化的纳米复合物由药物，硫酸葡聚糖和钙离子组成，比例为1:20:20 w / w / w，在7天内提供了持续释放特性。因此，新型的纳米复合物有望成为提供止痛剂持续释放的有效工具。
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