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Injectable in situ forming gel based on lyotropic liquid crystal for persistent postoperative analgesia
Acta Biomaterialia ( IF 9.7 ) Pub Date : 2017-12-08 , DOI: 10.1016/j.actbio.2017.11.057
Liling Mei , Yecheng Xie , Ying Huang , Bei Wang , Jintian Chen , Guilan Quan , Xin Pan , Hu Liu , Lili Wang , Xianguo Liu , Chuanbin Wu

Local anesthetics have been widely used for postoperative analgesia. However, multiple injections or local infiltration is required due to the short half-lives of local anesthetics after single injection, which results in poor compliance and increasing medical expense. In this study, an in situ forming gel (ISFG) based on lyotropic liquid crystal was developed to deliver bupivacaine hydrochloride (BUP) for long-acting postoperative analgesia. BUP-ISFG was designed to be administrated as a precursor solution which would spontaneously transform into gel with well-defined internal nanostructures for sustained drug release at the site of administration when exposed to physiological fluid. A lamellar-hexagonal-cubic phase transition occurred during the in situ gelation. The lamellar phase of the precursor solution endows it with low viscosity for good syringeability while the unique nanostructures of hexagonal and cubic phases of the in situ gel provide sustained drug release. Persistent analgesia effect in vivo was achieved with BUP-ISFG, and the plasma BUP concentration was found to be steadier compared to commercially available BUP for injection. In addition, the ISFG displayed acceptable biocompatibility and good biodegradability. The findings are positive about ISFG as a sustained release system for persistent postoperative analgesia.

Statement of Significance

To address the issue of insufficient postoperative analgesia associated with short half-lives of local anesthetics after single injection, an in situ forming gel (ISFG) based on lyotropic liquid crystal was developed to deliver bupivacaine hydrochloride (BUP) for postoperative analgesia over three days. The results demonstrated that persistent analgesia effect in vivo was achieved with single injection of BUP-ISFG, and the plasma BUP concentration was found to be steadier compared to commercially available BUP injection.

The BUP-ISFG possessed a lamellar-hexagonal-cubic phase transition with corresponding crystal change in 3D nanostructure during the in situ gelation. The relationship between crystal nanostructure and carrier function, might provide some insights to the design and clinical applications of the drug delivery systems based on lyotropic liquid crystal.



中文翻译:

基于溶致液晶的可注射原位形成凝胶用于术后持续镇痛

局部麻醉已被广泛用于术后镇痛。但是,由于单次注射后局麻药的半衰期短,因此需要多次注射或局部浸润,这导致依从性差并增加了医疗费用。在这项研究中,开发了一种基于溶致液晶的原位形成凝胶(ISFG),以递送盐酸布比卡因(BUP)进行长效术后镇痛。BUP-ISFG设计为以前体溶液形式给药,当暴露于生理液中时,该溶液会自发转变为具有明确内部纳米结构的凝胶,以在给药部位持续释放药物。在原位发生层状六方立方相变凝胶化。前体溶液的层状相赋予其低粘度,以实现良好的可注射性,而原位凝胶的六方相和立方相的独特纳米结构可提供持续的药物释放。使用BUP-ISFG可获得体内持久的镇痛效果,并且与市售的注射用BUP相比,血浆BUP浓度更稳定。另外,ISFG显示出可接受的生物相容性和良好的生物降解性。该发现对ISFG作为术后持续镇痛的持续释放系统具有积极意义。

重要声明

为了解决与单次注射后局部麻醉药半衰期短相关的术后镇痛不足的问题,开发了一种基于溶致液晶的原位形成凝胶(ISFG)以在三天内为术后镇痛提供盐酸布比卡因(BUP)。结果表明,单次注射BUP-ISFG可达到体内持久镇痛效果与市售BUP注射相比,血浆BUP浓度更稳定。

在原位凝胶化过程中 BUP-ISFG具有层状六方立方相变,并具有相应的3D纳米结构晶体变化。晶体纳米结构与载体功能之间的关系可能会为基于溶致液晶的药物递送系统的设计和临床应用提供一些见识。

更新日期:2017-12-14
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