首页> 外文期刊>Journal of Microencapsulation: Microcapsules Liposomes Nanoparticles Microcells Microspheres >Long-circulating polyethylene glycol)-coated poly(lactid-co-glycolid) microcapsules as potential carriers for intravenously administered drugs
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Long-circulating polyethylene glycol)-coated poly(lactid-co-glycolid) microcapsules as potential carriers for intravenously administered drugs

机译:长循环聚乙二醇)包衣的聚(乳酸-共-糖脂)微胶囊作为静脉内给药药物的潜在载体

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摘要

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 perfluorpdecalin (PFD)-filled PEG-PLGA microcapsules (1.5 urn diameter) were manufactured by using a modified solvent evaporation method with either 1% polyvinyl 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.
机译:关于纳米胶囊作为静脉内药物载体系统,微胶囊的固有优势仍未得到充分利用。特别地,在需要在血管系统内长期释放药物的临床情况下,如果必须施用大量药物或如果发生毛细血管渗漏,则长循环的微粒可能显示出优于纳米颗粒的替代方案。在此,合成了微胶囊,并研究了诸如体外聚集的趋势,蛋白质吸附和体内性能等参数。使用生物相容性聚乙二醇(PEG)涂层的聚(DL-丙交酯-乙交酯)(PLGA)作为墙体材料,并通过以下方法制造固体和全氟萘烷(PFD)填充的PEG-PLGA微胶囊(直径1.5 n)。改进的溶剂蒸发方法,使用1%的聚乙烯醇(PVA)或1.5%的胆酸盐作为乳化剂。与使用胆酸盐生产的微胶囊相比,当使用PVA时,蛋白质的吸附(白蛋白和IgG)明显降低,并且防止了胶囊的团聚。将这些固体和PFD填充的微胶囊静脉内给药成功,并显示出约1 h的循环半衰期。我们的数据清楚地表明,使用PVA制造的PEG-PLGA微胶囊是适合生物相容的长循环药物载体,适用于静脉内给药。

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