Department of intensive care unit, the Ninth People's Hospital of Chongqing, Chongqing, China.
Pharm Dev Technol. 2022 Jun;27(5):503-510. doi: 10.1080/10837450.2020.1871011. Epub 2022 Jun 2.
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.
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。
