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首页> 外文期刊>Acta biomaterialia >Comparison of PEG chain length and density on amphiphilic macromolecular nanocarriers: self-assembled and unimolecular micelles.
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Comparison of PEG chain length and density on amphiphilic macromolecular nanocarriers: self-assembled and unimolecular micelles.

机译：两亲大分子纳米载体上PEG链长和密度的比较：自组装和单分子胶束。

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摘要

Two classes of amphiphilic macromolecules were evaluated for drug delivery applications: those that exist as unimolecular micelles and those that self-assemble in aqueous solution to form micelles. This study compares the poly(ethylene glycol) (PEG) chain length and density that constitute the corona of both classes. In particular, the effect of PEG branching on micellar size, water-solubility, resolubilization rate, drug loading efficiency and drug release rate were analyzed. Pluronic P85 and Cremophor EL, commonly used in pharmaceutical applications, were used as controls. Indomethacin (IMC) was used as the drug for encapsulation, release and resolubilization experiments. Results indicated that smaller micellar sizes, higher water solubilities and faster resolubilization rates were achieved from higher PEG densities compared to linear PEG analog of similar mass. Further, micellar sizes of both higher density PEG and linear PEG macromolecules were constant over a wide temperature range (2-70 degrees C). In contrast, Cremophor EL formed aggregates at 15 degrees C and Pluronic P85 underwent a size transition at 45 degrees C. IMC loading efficiencies for all amphiphilic macromolecules were comparable to controls. However, faster resolubilization and slower drug release were observed for higher density PEG macromolecules compared to linear PEG analogs and controls.
机译：评价了两类两亲性大分子在药物递送方面的应用：以单分子胶束形式存在的两亲性大分子和在水溶液中自组装形成胶束的类两亲性大分子。这项研究比较了构成这两类电晕的聚乙二醇（PEG）链长和密度。特别地，分析了PEG支化对胶束大小，水溶性，再溶解速率，载药效率和药物释放速率的影响。药物应用中常用的Pluronic P85和Cremophor EL被用作对照。消炎痛（IMC）用作包囊，释放和再溶解实验的药物。结果表明，与类似质量的线性PEG类似物相比，更高的PEG密度可实现更小的胶束尺寸，更高的水溶性和更快的再溶解速率。此外，较高密度的PEG和线性PEG大分子的胶束尺寸在宽的温度范围（2-70℃）下是恒定的。相反，Cremophor EL在15摄氏度形成的聚集体，而Pluronic P85在45摄氏度经历了尺寸转变。所有两亲大分子的IMC负载效率均与对照相当。然而，与线性PEG类似物和对照相比，对于更高密度的PEG大分子观察到更快的再溶解和较慢的药物释放。

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