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用超临界二氧化碳从附着在固体上的 PLGA 微球中释放药物。

Drug release from PLGA microspheres attached to solids using supercritical CO₂.

机构信息

Chemical Engineering Department, University of Indonesia, Depok 16424, Indonesia.

出版信息

J Biomater Appl. 2011 Jan;25(5):401-12. doi: 10.1177/0885328209354365. Epub 2009 Dec 30.

Abstract

Functionalization of a porous orthopedic implant with dexamethasone, a widely used anti-inflammatory drug, encapsulated within a biodegradable polymer for controlled release could help reduce or eliminate the inflammation response by the local tissue. In this research, we investigated the possibility of using supercritical carbon dioxide (CO₂) for attaching dexamethasone-loaded PLGA (polylactic-co-glycolic acid) microspheres to porous CoCrMo alloy for continuous delivery of dexamethasone. Supercritical CO₂ has been shown to be effective for attachment of PLGA microspheres to glass plates and porous CoCrMo alloy. Attached microspheres showed similar dexamethasone release profiles but different magnitude of burst release. Microspheres attached to the porous alloy samples using supercritical CO₂ at 10 bar and 40 °C for 30 min showed a release profile similar to that of the nonattached microspheres. The microsphere morphology and the release profiles of microspheres attached to the glass plates and to the porous alloy samples suggest that dexamethasone burst release is enhanced by PLGA swelling at higher CO₂ pressures and better dispersion of microspheres. This study shows that microspheres can be incorporated into porous solids using supercritical CO₂, allowing for a wide variety of drug-biodegradable polymer formulations prepared using the proven emulsion/solvent evaporation method to be tested.

摘要

将一种广泛应用于抗炎的药物地塞米松通过包裹在可生物降解聚合物中的方式固定在多孔骨科植入物上,通过控制药物的释放,有助于减轻或消除局部组织的炎症反应。在这项研究中,我们探索了使用超临界二氧化碳(CO₂)将载有地塞米松的 PLGA(聚乳酸-共-羟基乙酸)微球附着在多孔 CoCrMo 合金上来连续递送地塞米松的可能性。超临界 CO₂ 已被证明可有效将 PLGA 微球附着在玻璃片和多孔 CoCrMo 合金上。附着的微球显示出相似的地塞米松释放曲线,但突释程度不同。在 10 巴和 40°C 的超临界 CO₂ 下作用 30 分钟,附着在多孔合金样品上的微球显示出与非附着微球相似的释放曲线。微球形态和附着在玻璃片和多孔合金样品上的微球的释放曲线表明,在较高的 CO₂压力下,PLGA 溶胀和微球更好的分散增强了地塞米松的突释。这项研究表明,可以使用超临界 CO₂ 将微球掺入多孔固体中,允许使用经过验证的乳液/溶剂蒸发方法制备的各种药物-可生物降解聚合物制剂进行测试。

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