文獻：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

文獻鏈接：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.

合成了具有約32個臂的多臂星形兩親嵌段共聚物（SABC），并對其進行了表征，以用于藥物輸送應用。使用超支化聚酯bolten_H40（H40）作為s-己內酯（ε-CL）開環聚合的大分子引發劑。

使所得的多臂H40-聚（ε-己內酯）（H40-PCL-OH）進一步與羧基封端的甲氧基聚（乙二醇）（MPEG-COOH）反應以形成H40-PCL-b-MPEG共聚物。所得的SABC通過1H NMR光譜和凝膠滲透色譜（GPC）進行表征。

通過熒光分光光度法測定，H40-PCL-b-MPEG的臨界聚集濃度（CAC）為3.8 mg / L。在CAC下方，形成穩定的單分子膠束，通過TEM測量其平均直徑為18nm。

在CAC上方，單分子膠束表現出團聚，平均直徑為98 nm。通過動態光散射（DLS）測量，發現這些附聚物的流體力學直徑為122nm。 

H40-PCL-b-MPEG膠束的載藥效率為26重量％。藥物釋放研究表明，最初的爆發是隨后在9-140小時內持續釋放所包裹的疏水模型藥物5-氟尿嘧啶。

這些結果表明，H40-PCL-b-MPEG膠束具有作為疏水藥物遞送載體的潛力。

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