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首页> 外文期刊>Journal of Applied Polymer Science >Fabrication of size-controllable mPEG-decorated microparticles conjugating optically active ketoprofen based on self-assembly of amphiphilic random copolymers
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Fabrication of size-controllable mPEG-decorated microparticles conjugating optically active ketoprofen based on self-assembly of amphiphilic random copolymers

机译：基于两亲无规共聚物的自组装，制备尺寸可控制的mPEG修饰的微粒，该微粒缀合光学活性酮洛芬

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摘要

Novel size-controllable mPEG-decorated polymeric microparticles binding optically active ketoprofen were successfully fabricated based on chemoenzymatic synthesis and self-assembly of amphiphilic random polymer-ketoprofen conjugates with mPEG and (S)-ketoprofen as pendants. A series of mPEG_(350)- or mPEG_(1000)-functionalized amphiphilic random polymer-ketoprofen conjugates with drug loading capacity from 16.5% to 73.2% were easily prepared by combining enzymatic resolution with radical polymerization and characterized by Fourier Transform Infrared spectroscopy, ~1H-NMR, and gel permeation chromatography. The formation of aggregates from the amphiphilic random polymer-ketoprofen conjugates was investigated by ultraviolet-visible absorption spectra using pyrene as the guest molecule. Transmission electron microscopy measurement revealed that the self-assemblies were well dispersed as spherical microparticles. The size of the self-assemblies could be widely tuned by varying the length of mPEG chains and the content of ketoprofen in the synthetic polymer-ketoprofen conjugates, and a series of mPEG-decorated (S)-ketoprofen-bound polymeric microparticles with average radius from 70 nm to 1.1 μm were obtained. The successful preparation of the microparticles containing (S)-ketoprofen provided a new strategy for the design and fabrication of optically active drug delivery systems.
机译：基于化学酶法合成和两亲性随机聚合物-酮洛芬共轭物的自组装，以mPEG和（S）-酮洛芬为侧基，成功地制备了结合光学活性酮洛芬的新型可控大小的mPEG装饰的聚合物微粒。通过将酶拆分与自由基聚合相结合，并通过傅里叶变换红外光谱进行表征，可以轻松制备一系列载药量为16.5％至73.2％的mPEG_（350）-或mPEG_（1000）-官能化的两亲无规聚合物-酮洛芬共轭物，〜 1 H-NMR和凝胶渗透色谱。通过使用as作为客体分子的紫外-可见吸收光谱研究了由两亲无规聚合物-酮洛芬共轭物形成的聚集体。透射电子显微镜测量显示自组装体很好地分散为球形微粒。通过改变合成聚合物-酮洛芬缀合物中mPEG链的长度和酮洛芬的含量以及一系列平均半径为mPEG修饰的（S）-酮洛芬结合的聚合物微粒，可以广泛地调节自组装体的大小获得了70nm至1.1μm的光。含（S）-酮洛芬的微粒的成功制备为光学活性药物传递系统的设计和制造提供了新的策略。

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