Biodegradable and biocompatible multi-arm star amphiphilic block copolymer as a carrier for hydrophobic drug delivery
Biodegradable and biocompatible multi-arm star amphiphilic block copolymer as a carrier for hydrophobic drug delivery
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DOI：
10.1016/j.ijbiomac.2009.01.007
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发表时间：
2009-05-01
影响因子：
8.2
通讯作者：
Gong, Shaoqin
中科院分区：
文献类型：
--
作者：
Aryal, Santosh;Prabaharan, Mani;Gong, Shaoqin
合成了具有约32个臂的多臂星星型两亲性嵌段共聚物（SABC），并表征其用于药物递送应用。超支化聚酯Boltorn（R）H40（H40）用作ε-己内酯（ε-CL）开环聚合的大分子引发剂。将所得多臂H40-聚（ε-己内酯）CH 40-PCL-OH）进一步与羧基封端的甲氧基聚（乙二醇）（MPEG-COOH）反应以形成H40-PCL-b-M PEG共聚物。用1H-1 NMR和凝胶渗透色谱（GPC）对SABC进行了表征。荧光分光光度法测定H40-PCL-b-MPEG的临界聚集浓度（CAC）为3.8mg/L。在CAC以下，形成稳定的单分子胶束，其平均直径为18 nm，通过TEM测量。在CAC以上，单分子胶束表现出团聚，平均直径为98 nm。发现这些附聚物的流体动力学直径为122 nm，如通过动态光散射（DLS）测量的。H40-PCL-b-MPEG胶束的载药效率为26wt%。药物释放研究表明，包封的疏水模型药物5-氟尿嘧啶在9-140 h内先突释，然后持续释放。这些结果表明，H40-PCL-b-MPEG胶束作为疏水性药物释放载体具有很大的潜力。(C)2009爱思唯尔有限公司版权所有。
Multi-arm star amphiphilic block copolymers (SABCs) with approximately 32 arms were synthesized and characterized for drug delivery applications. A hyperbranched polyester, boltorn (R) H40 (H40), was used as the macroinitiator for the ring-opening polymerization of epsilon-caprolactone (epsilon-CL). The resulting multi-arm H40-poly(epsilon-caprolactone) CH40-PCL-OH) was further reacted with carboxyl terminated methoxy poly(ethylene glycol) (MPEG-COOH) to form H40-PCL-b-M PEG copolymers. The resulting SABCs were characterized by H-1 NMR spectroscopy and gel permeation chromatography (GPC). The critical aggregation concentration (CAC) of H40-PCL-b-MPEG was 3.8 mg/L as determined by fluorescence spectrophotometry. Below the CAC, stable unimolecular micelles were formed with an average diameter of 18 nm as measured by TEM. Above the CAC, unimolecular micelles exhibited agglomeration with an average diameter of 98 nm. The hydrodynamic diameter of these agglomerates was found to be 122 nm, as measured by dynamic light scattering (DLS). The drug loading efficacy of the H40-PCL-b-MPEG micelles was 26 wt%. Drug release study showed an initial burst followed by a sustained release of the entrapped hydrophobic model drug, 5-fluorouracil, over a period of 9-140 h. These results indicate that the H40-PCL-b-MPEG micelles have great potential as hydrophobic drug delivery carriers. (C) 2009 Elsevier B.V. All rights reserved.