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载有罗哌卡因和倍他米松的 PLGA 微球用于小鼠坐骨神经阻滞。

PLGA-based microspheres containing ropivacaine and betamethasone for sciatic nerve block in mice.

机构信息

Department of intensive care unit, the Ninth People's Hospital of Chongqing, Chongqing, China.

出版信息

Pharm Dev Technol. 2022 Jun;27(5):503-510. doi: 10.1080/10837450.2020.1871011. Epub 2022 Jun 2.

Abstract

The aim of the present study was to develop Poly (lactic-co-glycolic acid) (PLGA)-based microspheres containing ropivacaine and betamethasone (RPC/BTM PLGA MS) by emulsion-solvent evaporation method. RPC/BTM PLGA MS were characterized by physical properties, such as morphology and particle size, and drug release. In addition, pharmacokinetics and pharmacodynamics of RPC/BTM PLGA MS were also investigated. The prepared RPC/BTM PLGA MS was suitable for local injection with a well-dispersed spherical shape, high stability, and high encapsulation efficiency. The mean diameter was 14.8 ± 1.2 µm and the polydispersity index (PDI) was 0.32 ± 0.04. In an study of drug release, it can be concluded that the RPC/BTM PLGA MS exhibited sustained and long-term release properties for 16 days. Furthermore, the result of an study indicated that the RPC/BTM PLGA MS had sustained release effect and the pharmacodynamics result showed that preparing RPC/BTM PLGA MS as microsphere preparation could not only extend the drug effect time but also prolong the duration of local anesthetics compared with the common RPC PLGA MS.

摘要

本研究旨在通过乳化-溶剂挥发法制备载罗哌卡因和倍他米松的聚(乳酸-共-乙醇酸)(PLGA)微球(RPC/BTM PLGA MS)。通过形态和粒径等物理性质以及药物释放来表征 RPC/BTM PLGA MS。此外,还研究了 RPC/BTM PLGA MS 的药代动力学和药效学。所制备的 RPC/BTM PLGA MS 适合局部注射,具有良好的分散球形、高稳定性和高包封效率。平均粒径为 14.8±1.2μm,多分散指数(PDI)为 0.32±0.04。在药物释放研究中,可以得出结论,RPC/BTM PLGA MS 表现出持续和长期释放的特性,持续时间为 16 天。此外,研究结果表明,RPC/BTM PLGA MS 具有持续释放的效果,药效学结果表明,与普通 RPC PLGA MS 相比,将 RPC/BTM PLGA MS 制备成微球制剂不仅可以延长药物作用时间,还可以延长局部麻醉剂的作用时间。

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