Sucrose Acetate Isobutyrate as an In situ Forming Implant for Sustained Release of Local Anesthetics
Sucrose Acetate Isobutyrate as an In situ Forming Implant for Sustained Release of Local Anesthetics
复制标题
蔗糖乙酸异丁酸酯作为局部麻醉剂持续释放的原位成型植入物
DOI：
10.2174/1567201816666181119112952
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发表时间：
2019-01-01
影响因子：
2.4
通讯作者：
Zhu, Yuxuan
中科院分区：
文献类型：
--
作者：
Li, Hanmei;Xu, Yuling;Zhu, Yuxuan
目的：本研究设计并制备了一种可注射的醋酸异丁酸蔗糖酯（sucroseacetateisobutyrate，SAIB）给药系统（drugdeliverysystem，SADS），用于罗哌卡因（Ropivacaine，RP）的缓释，以延长局部麻醉的持续时间。结果：RP-SADS具有良好的体外释药特性和体内药动学特性。特别是，RP-SADS显着降低了初始突释后，皮下注射在rats.Conclusion：在大鼠的药效学分析，神经阻滞的持续时间延长了超过3倍的RP-SADS制剂相比，RP解决方案。此外，RP-SADS在体外和体内均表现出良好的生物相容性。因此，基于SiDS的贮库技术是一种安全的局部麻醉药缓释策略，具有长期镇痛作用。
Objective: In this study, an injectable Sucrose Acetate Isobutyrate (SAIB) drug delivery system (SADS) was designed and fabricated for the sustained release of Ropivacaine (RP) to prolong the duration of local anesthesia.Methods: By mixing SAIB, RP, and N-methyl-2-pyrrolidone, the SADS was prepared in a sol state with low viscosity before injection. After subcutaneous injection, the pre-gel solution underwent gelation in situ to form a drug-released depot.Result: The in vitro release profiles and in vivo pharmacokinetic analysis indicated that RP-SADS had suitable controlled release properties. Particularly, the RP-SADS significantly reduced the initial burst release after subcutaneous injection in rats.Conclusion: In a pharmacodynamic analysis of rats, the duration of nerve blockade was prolonged by over 3-fold for the RP-SADS formulation compared to RP solution. Additionally, RP-SADS showed good biocompatibility in vitro and in vivo. Thus, the SiDS-based depot technology is a safe drug delivery strategy for the sustained release of local anesthetics with long-term analgesia effects.