文献：Biodegradable and biocompatible multi-arm star amphiphilic block copolymer as a carrier for hydrophobic drug delivery

作者：S Aryal，M Prabaharan，S Pilla，S Gong

文献链接：https://xueshu.baidu.com/usercenter/paper/show?paperid=d61fdc2f0b9e8919635b549acaef41be&site=xueshu_se

摘要：

Multi-arm star amphiphilic block copolymers (SABCs) with approximately 32 arms were synthesized and characterized for drug delivery applications. A hyperbranched polyester, boltorn~_ H40 (H40), was used as the macroinitiator for the ring-opening polymerization of s-caprolactone (ε-CL). The result_ing multi-arm H40-poly(ε-caprolactone) (H40-PCL-OH) was further reacted with carboxyl terminated methoxy poly(ethylene glycol) (MPEG-COOH) to form H40-PCL-b-MPEG copolymers. The resulting SABCs were characterized by ~1H 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 spec_trophotometry. 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 aver_age 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.

合成了具有约32个臂的多臂星形两亲嵌段共聚物（SABC），并对其进行了表征，以用于药物输送应用。使用超支化聚酯bolten_H40（H40）作为s-己内酯（ε-CL）开环聚合的大分子引发剂。

使所得的多臂H40-聚（ε-己内酯）（H40-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-MPEG共聚物。所得的SABC通过1H NMR光谱和凝胶渗透色谱（GPC）进行表征。

通过荧光分光光度法测定，H40-PCL-b-MPEG的临界聚集浓度（CAC）为3.8 mg / L。在CAC下方，形成稳定的单分子胶束，通过TEM测量其平均直径为18nm。

在CAC上方，单分子胶束表现出团聚，平均直径为98 nm。通过动态光散射（DLS）测量，发现这些附聚物的流体力学直径为122nm。 

H40-PCL-b-MPEG胶束的载药效率为26重量％。药物释放研究表明，最初的爆发是随后在9-140小时内持续释放所包裹的疏水模型药物5-氟尿嘧啶。

这些结果表明，H40-PCL-b-MPEG胶束具有作为疏水药物递送载体的潜力。

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