Water-free microencapsulation of proteins within PLGA microparticles by spray drying using PEG-assisted protein solubilization technique in organic solvent

Water-free microencapsulation of proteins within PLGA microparticles by spray drying using PEG-assisted protein solubilization technique in organic solvent
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DOI:
10.1016/j.ejpb.2008.04.006
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发表时间:
2008-09-01
影响因子:
4.9
通讯作者:
Park, Tae Gwan
Park, Tae Gwan
中科院分区:
医学2区
文献类型:
--
作者:
Mok, Hyejung;Park, Tae Gwan

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在无水条件下制备了包封治疗性蛋白的聚(D, l -乳酸-羟基乙酸)(PLGA)微颗粒。以聚乙二醇(PEG)为络合物形成剂,将牛血清白蛋白(BSA)和重组人生长激素(rhGH)在二氯甲烷相中均匀溶解为纳米级络合物。将含有溶解的PLGA和PEG/蛋白复合物的有机相直接喷雾干燥,得到包封蛋白的PLGA微粒。它们表现出长达30天的BSA和rhGH的持续释放特征,初始爆发减少。从微颗粒中释放的蛋白质分子保持了结构的完整性而没有聚集,这表明目前不用水的单步蛋白质微胶囊化方法有可能应用于持续递送一系列不溶于有机溶剂的治疗性蛋白质药物。(c) 2008 Elsevier B.V.版权所有
Poly(D,L-lactic-co-glycolic acid) (PLGA) microparticles encapsulating therapeutic proteins were prepared under a water-free formulation condition. Bovine serum albumin (BSA) and recombinant human growth hormone (rhGH) were homogeneously solubilized as nano-scale complexes in methylene chloride phase by using polyethylene glycol (PEG) as a complex-forming agent. The organic phase containing dissolved PLGA and PEG/protein complexes was directly spray dried to obtain PLGA microparticles encapsulating proteins. They exhibited sustained release profiles of BSA and rhGH up to 30 days with reduced initial bursts. The released protein molecules from the microparticles maintained structural integrity without aggregation, suggesting that the current single-step protein microencapsulation method without using water could be potentially applied for sustained delivery of a wide range of therapeutic protein drugs that are not soluble in organic solvents. (c) 2008 Elsevier B.V. All rights reserved.