Heparin conjugated polymeric micelle for long-terin delivery of basic fibroblast growth factor
Heparin conjugated polymeric micelle for long-terin delivery of basic fibroblast growth factor
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DOI：
10.1016/j.jconrel.2006.11.004
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发表时间：
2007-02-12
影响因子：
10.8
通讯作者：
Park, Ki Dong
中科院分区：
文献类型：
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作者：
Lee, Jung Seok;Go, Dong Hyun;Park, Ki Dong
开发了肝素偶联的两亲嵌段共聚物Tetronic(R)-PCL-Heparin(TCH)，并制备了其聚合物胶束(Pms)，作为肝素结合生长因子(HBGF)之一的bFGF的长期注射载体。采用单一乳液和溶剂挥发法制备了TCH膜。用核磁共振氢谱、傅立叶变换红外光谱和凝胶渗透色谱确证了TCH的结构。与游离肝素相比，结合肝素的含量为0.44微克/微克，APTT测定的肝素活性为43.6%。TCH-PMs的临界胶束浓度约为0.11g/L，TC胶束的直径约为25 nm，与肝素偶联后胶束的大小因胶束壳层上的肝素分子而增大到114 nm。肝素与碱性成纤维细胞生长因子的特异性相互作用使TCH-PM的碱性成纤维细胞生长因子负载量明显高于TC。体外实验中，碱性成纤维细胞生长因子从TCH PM中以控制的方式释放超过2个月。结果表明，TCH微球可作为组织工程中多种生长因子与肝素结合区长期输送的候选材料。(C)2006爱思唯尔B.V.保留所有权利。
Heparin conjugated amphiphilic block copolymer, Tetronic (R)-PCL-heparin (TCH), was developed and its polymeric micelles (PMs) were prepared as an injectable vehicle for long-term delivery of bFGF, which is one of the heparin-binding growth factors (HBGF). TCH PMs were fabricated by a single emulsion and solvent evaporation method. The structural properties of TCH were confirmed by H-1 NMR, FT-IR and GPC. The contents of bound heparin were 0.44 mu g/mu g and the heparin activity by APTT assay was 43.6% when compared to free heparin. The critical micelle concentration (CMC) of TCH PMs was approximately 0.11 g/l. The diameter of TC micelle was approximately 25 nm and its size after conjugation of heparin was increased to 114 nm due to the heparin molecules on the shell of the micelle. The bFGF loading amount of TCH PMs was considerably higher than that of TC, caused by specific interactions between heparin and bFGF. In vitro study, bFGF was released from TCH PMs in a controlled manner over 2 months. The results demonstrated that TCH PMs become a novel candidate for the long-term delivery of various growth factors with heparin-binding domain in tissue engineering. (c) 2006 Elsevier B.V. All rights reserved.