Co-encapsulation of dexamethasone 21-acetate and SPIONs into biodegradable polymeric microparticles designed for intra-articular delivery
Co-encapsulation of dexamethasone 21-acetate and SPIONs into biodegradable polymeric microparticles designed for intra-articular delivery
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DOI：
10.1080/02652040801999551
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发表时间：
2008-01-01
影响因子：
3.9
通讯作者：
Doelker, Eric
中科院分区：
文献类型：
--
作者：
Butoescu, Nicoleta;Jordan, Olivier;Doelker, Eric
目的：关节内给药系统仍然存在药效持续时间过短的问题。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物的局部释放。方法：采用复乳法制备包埋超顺磁性氧化铁纳米粒（SPIONs）和地塞米松21-醋酸酯（DXM）的聚（D，L-丙交酯-乙交酯）微球。处方优化分两步进行，筛选设计和全析因设计，针对10-m粒径和高DXM包封efficiency.Results：最显着的参数是聚合物浓度，溶剂提取过程中的搅拌速度和提取体积。将聚合物浓度从200 mg ml（-1）增加到300 mg ml（-1），微粒平均直径和DXM包封效率分别增加到12 μ m和90%。微粒可以保留与外部磁铁0.8 T放置在3 mm。更快的DXM释放获得较小的microparticles.Conclusion：实验设置提供的工具，用于定制一个配方的磁保留性能和DXM释放模式对应于所需的规格为关节内给药。
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-m 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 m 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.