Long-circulating poly(ethylene glycol)-coated poly(lactid-co-glycolid) microcapsules as potential carriers for intravenously administered drugs
Long-circulating poly(ethylene glycol)-coated poly(lactid-co-glycolid) microcapsules as potential carriers for intravenously administered drugs
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DOI：
10.3109/02652048.2013.770098
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发表时间：
2013-01-01
影响因子：
3.9
通讯作者：
Kirsch, Michael
中科院分区：
文献类型：
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作者：
Ferenz, Katja B.;Waack, Indra N.;Kirsch, Michael
微胶囊作为静脉药物载体系统的内在优势尚未得到充分利用。特别地，在需要在血管系统内长期药物释放的临床情况下，如果必须施用大量药物或者如果发生毛细血管渗漏，则长循环微粒可以显示出纳米颗粒的上级替代物。在这里，微胶囊的合成和参数，如在体外团聚的趋势，蛋白质吸附和在体内的性能进行了研究。以聚乙二醇（PEG）包覆的聚（DL-丙交酯-共-乙交酯）（PLGA）为壁材，采用改进的溶剂蒸发法，以1%聚乙烯醇（PVA）或1.5%胆酸盐为乳化剂，制备了PEG-PLGA（直径1.5 μ m）固体微胶囊和全氟萘烷（PFD）填充微胶囊。与用胆酸盐制造的微胶囊相比，当使用PVA时，蛋白质吸附（白蛋白和IgG）明显降低，并且防止了胶囊的团聚。在大鼠中静脉内施用这些微胶囊（固体和填充有PFD的）是成功的，并且表现出约1小时的循环半衰期。我们的数据清楚地表明，PEG-PLGA微囊，通过使用PVA制造，是合适的生物相容性，长循环药物载体，适用于静脉给药。
The intrinsic advantages of microcapsules with regard to nanocapsules as intravenous drug carrier systems are still not fully exploited. Especially, in clinical situations where a long-term drug release within the vascular system is desired, if large amounts of drug have to be administered or if capillary leakage occurs, long-circulating microparticles may display a superior alternative to nanoparticles. Here, microcapsules were synthesised and parameters such as in vitro tendency of agglomeration, protein adsorption and in vivo performance were investigated. Biocompatible poly(ethylene glycol) (PEG)-coated poly(DL-lactide-co-glycolide) (PLGA) as wall material, solid and perfluorodecalin (PFD)-filled PEG-PLGA microcapsules (1.5 mu m diameter) were manufactured by using a modified solvent evaporation method with either 1% poly(vinyl alcohol) (PVA) or 1.5% cholate as emulsifying agents. Compared to microcapsules manufactured with cholate, the protein adsorption (albumin and IgG) was clearly decreased and agglomeration of capsules was prevented, when PVA was used. The intravenous administration of these microcapsules, both solid and PFD-filled, in rats was successful and exhibited a circulatory half-life of about 1 h. Our data clearly demonstrate that PEG-PLGA microcapsules, manufactured by using PVA, are suitable biocompatible, long-circulating drug carriers, applicable for intravenous administration.