Preparation of Ropivacaine Encapsulated by Zeolite Imidazole Framework Microspheres as Sustained‐Release System and Efficacy Evaluation. Issue 21 (9th March 2023)

• Record Type: Journal Article
• Authors: Wang, Peng; Wang, Guangyu; Tang, Hongwen; Feng, Siwen; Tan, Lichuan; Zhang, Pu; Wei, Guihua; Wang, Cuijuan
• Is Part Of: Chemistry. Volume 29:Issue 21(2023)
• Page Start: n/a
• Page End: n/a
• Publication Date: 2023-03-09
• Subjects: biological safety -- drug delivery -- ropivacaine -- sciatic nerve block -- zeolite analogues; Chemistry -- Periodicals; 540
• DOI: 10.1002/chem.202203458
• Languages: English
• ISSNs: 0947-6539

Abstract

Abstract: The management of persistent postoperative pain still remains a clinical challenge currently. Although ropivacaine (RVC) is widely used for postoperative analgesia as a local anesthetic, the short half‐life makes it difficult to achieve the desired duration of analgesia. Herein, a RVC sustained‐release microspheres encapsulated by zeolite imidazole framework‐8 (RVC@ZIF‐8) was synthesized for the first time, which prolonged the sustained‐release of RVC and decreased the resulting drug toxicity. RVC can continuously release in vitro for at least 96 h with high drug loading of 30.6 % and RVC@ZIF‐8 had excellent biocompatibility and low cytotoxicity. In sciatic nerve block model, the sensory block time of RVC@ZIF‐8 was significantly prolonged compared with RVC, achieving more than 72 h post injection and no inflammation or lesion were found. Based on high drug loading, ideal sustained‐release and superior biological safety, RVC@ZIF‐8 will be a novel delivery material for local anesthetic with potential application. Abstract : A ropivacaine microspheres encapsulated by zeolite imidazole framework (RVC@ZIF‐8) as sustained‐release system was prepared for the first time. This novel material exhibits a high drug loading rate and superior biological safety, with a continuously release in vitro for at least 96 h, and the sensory block time was more than 72 h in vivo pharmacodynamic.