Use of block copolymers of poly(ortho esters) and poly (ethylene glycol) micellar carriers as potential tumour targeting systems

Use of block copolymers of poly(ortho esters) and poly (ethylene glycol) micellar carriers as potential tumour targeting systems
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DOI:
10.1080/10611860310001633839
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发表时间:
2003-07-01
影响因子:
4.5
通讯作者:
Heller, J
Heller, J
中科院分区:
医学3区
文献类型:
--
作者:
Toncheva, V;Schacht, E;Heller, J

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以聚原酸酯和聚乙二醇制得了两亲性AB和ABA嵌段共聚物。这种嵌段共聚物很容易在水或缓冲液中形成胶束分散体。CMC在3×10(-4)-5×10(-4)g/L的范围内,这个值足够低,足以确保静脉注射时胶束的完整性。由动态光散射测定的尺寸在40-70 nm范围内。该胶束可在冻干状态下保存至少8个月,并容易恢复到原来的性质。胶束在pH 7.4和37℃的PBS溶液中稳定3天,在pH 5.5和37℃的柠檬酸盐缓冲液中稳定2 h。在牛血清白蛋白存在下的稳定性取决于嵌段共聚物的结构,特别是POE嵌段的长度。
Amphiphilic AB and ABA block copolymers have been prepared from poly (ortho esters) and poly (ethylene glycol). Such block copolymers readily form micellar dispersions in water, or buffers. The CMC is in the range of 3 x 10(-4)-5 x 10(-4) g/l which is a value low enough to assure retention of micelle integrity upon intravenous injection. The size, as determined by dynamic light scattering was in the 40-70 nm range. The micelles can be stored in lyophilized form for at lest 8 months and easily reconstituted to the original properties. The micelles are stable in PBS at pH 7.4 and 37degreesC for 3 days and in a citrate buffer at pH 5.5 and 37degreesC for 2 h. Stability in the presence of bovine serum albumin depends on the structure of the block copolymer and especially the length of the POE block.