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首页> 外文期刊>Journal of Microencapsulation: Microcapsules Liposomes Nanoparticles Microcells Microspheres >Co-encapsulation of dexamethasone 21-acetate and SPIONs into biodegradable polymeric microparticles designed for intra-articular delivery
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Co-encapsulation of dexamethasone 21-acetate and SPIONs into biodegradable polymeric microparticles designed for intra-articular delivery

机译：将地塞米松21-乙酸盐和SPIONs共包裹到可生物降解的聚合物微粒中，用于关节内递送

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Objective: Intra-articular drug delivery systems still suffer from too short-lasting effects. Magnetic particles retained in the joint using an external magnetic field might prolong the local release of an anti-inflammatory drug. For the purpose, superparamagnetic iron oxide nanoparticles (SPIONs) and dexamethasone 21-acetate (DXM) were co-encapsulated into biodegradable microparticles. Methods: Poly(D,L-lactide-co-glycolide) microparticles embedding both SPIONs and DXM were prepared by a double emulsion technique. The formulation was optimized in two steps, a screening design and a full factorial design, aiming at 10-μm particle diameter and high DXM encapsulation efficacy. Results: The most significant parameters were the polymer concentration, the stirring speed during solvent extraction and the extractive volume. Increasing the polymer concentration from 200 to 300 mg ml~(-1), both the microparticle mean diameter and the DXM encapsulation efficacy increased up to 12 μm and 90%, respectively. The microparticles could be retained with an external magnet of 0.8 T placed at 3 mm. Faster DXM release was obtained for smaller microparticles. Conclusion: The experimental set-up offered the tools for tailoring a formulation with magnetic retention properties and DXM release patterns corresponding to the required specifications for intra-articular administration.
机译：目的：关节内药物输送系统仍然具有持续时间太短的作用。使用外部磁场保留在关节中的磁性颗粒可能会延长抗炎药的局部释放。为此，将超顺磁性氧化铁纳米粒子（SPIONs）和地塞米松21醋酸酯（DXM）共囊化为可生物降解的微粒。方法：采用双乳化技术制备同时包埋SPIONs和DXM的聚（D，L-丙交酯-乙交酯）微粒。针对10μm粒径和高DXM封装功效，以筛选设计和全因子设计这两个步骤对配方进行了优化。结果：最重要的参数是聚合物浓度，溶剂萃取过程中的搅拌速度和萃取量。将聚合物浓度从200 mg / ml（-1）增加到123μm和90％时，微粒平均直径和DXM包封效率均增加。可以用放置在3 mm处的0.8 T的外部磁体来保留微粒。对于较小的微粒，DXM释放速度更快。结论：实验设置为定制具有磁保持特性和DXM释放模式的制剂提供了工具，这些制剂与关节内给药所需的规格相对应。

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