Department of Anesthesiology, Fujian Provincial Hospital, Fujian Shengli Clinical Medical College, Fujian Medical University, Fuzhou, PR China.
Institute of Pharmaceutics, College of Pharmaceutical Sciences, Zhejiang University, Hangzhou, PR China.
Drug Dev Ind Pharm. 2022 Jun;48(6):255-264. doi: 10.1080/03639045.2022.2106995. Epub 2022 Aug 26.
Local analgesia is one of the most desirable methods for postoperative pain control, while the existing local anesthetics have a short duration of analgesic effect. Nano-drug carriers have been widely used in various fields and provide an excellent strategy for traditional drugs. Although the existing liposomes for local anesthetics have certain advantages, their instability and complexity of the preparation process still cannot be ignored. Here, we developed novel ropivacaine hydrochloride liposomes with improved stability and sustained release performance by combining ropivacaine hydrochloride with sodium oleate in liposomes hydrophobic ion-pairing (HIP). The liposomes are easy to prepare, inexpensive, and suitable for mass production. The infrared (IR), particle size, and Zeta potential measurements adequately characterized the complex, which showed a diameter of 81.09 nm and a zeta potential of -83.3 mV. Animal behavioral experiments, including the hot plate test and von Frey fiber test, demonstrated that the liposome system had a prolonged analgesic effect of 2 h conventional liposome preparations, consistent with the results of release experiments. In addition, cytotoxicity evaluations in RAW264.7 cells and evaluations revealed the biocompatibility and safety of the ropivacaine-sodium oleate ion-paired liposome (Rop-Ole-Lipo) system as a suitable local anesthetic for local pain management. Our findings provide a new idea for the preparation of local anesthetics.
局部麻醉是术后疼痛控制最理想的方法之一，而现有的局部麻醉剂的镇痛效果持续时间短。纳米药物载体已广泛应用于各个领域，为传统药物提供了一种极好的策略。尽管现有的局部麻醉用脂质体具有一定的优势，但它们的不稳定性和复杂的制备过程仍然不容忽视。在这里，我们通过将盐酸罗哌卡因与脂质体中的油酸钠结合，开发了一种新型的盐酸罗哌卡因脂质体，具有改善的稳定性和持续释放性能，这种脂质体通过脂质体疏水离子对（HIP）结合。该脂质体易于制备、成本低廉，适合大规模生产。红外（IR）、粒径和 Zeta 电位测量充分表征了该复合物，其粒径为 81.09nm，Zeta 电位为-83.3mV。动物行为学实验，包括热板试验和冯弗雷纤维试验，表明该脂质体系统具有比传统脂质体制剂延长 2 小时的镇痛作用，与释放实验结果一致。此外，在 RAW264.7 细胞中的细胞毒性评估和体内评估表明，盐酸罗哌卡因-油酸钠离子对脂质体（Rop-Ole-Lipo）系统作为局部疼痛管理的局部麻醉剂具有良好的生物相容性和安全性。我们的研究结果为局部麻醉剂的制备提供了新的思路。
