Preparation of preformed porous PLGA microparticles and antisense oligonucleotides loading
Preparation of preformed porous PLGA microparticles and antisense oligonucleotides loading
复制标题
DOI：
10.1016/j.ejpb.2008.09.007
复制
发表时间：
2009-02-01
影响因子：
4.9
通讯作者：
Bodmeier, Roland
中科院分区：
文献类型：
--
作者：
Ahmed, Abid Riaz;Bodmeier, Roland
本研究的目的是用药物装载预先形成的高度多孔的微粒。通过添加成孔剂（NaCl到内部水相中或甘油单油酸酯到聚（丙交酯-共-乙交酯）（PLGA）聚合物相中）的改进的多重乳液（w/o/w）溶剂蒸发方法制备微粒。然后用水（对于NaCl）或己烷（对于甘油单油酸酯）洗涤不含药物的固化微粒以提取成孔剂。然后通过在药物水溶液中孵育，然后空气干燥或冷冻干燥，将药物加载到预先形成的多孔微粒中。药物与空气干燥的微粒牢固地结合到聚合物表面。具有初始快速释放相（突释效应）的双相药物释放之后是长达数周的较慢释放。初始突释取决于载药量，并且可以通过湿（非水）温度固化显著降低。(C)2008 Elsevier B.V.保留所有权利。
The objective of this study was to load preformed highly porous microparticles with drug. The microparticles were prepared by a modified multiple emulsion (w/o/w) solvent evaporation method with the addition of pore formers (NaCl into the internal aqueous phase or of glycerol monooleate to the poly(lactide-co-glycolide) (PLGA) polymer phase). The drug-free solidified microparticles were then washed with either water (for NaCl) or hexane (for glycerol monooleate) to extract the pore formers. The drug was then loaded into the preformed porous microparticles by incubation in aqueous drug solutions followed by air- or freeze-drying. The drug was strongly bound to the polymeric surface with air-dried microparticles. A biphasic drug release with an initial rapid release phase (burst effect) was followed by a slower release up to several weeks. The initial burst was dependent on the drug loading and could be significantly reduced by wet (non-aqueous) temperature curing. (C) 2008 Elsevier B.V. All rights reserved.