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Polymer-Drug Encapsulation using Various PEG- and Polypeptide-Based Block Copolymer Micelles

机译:使用各种基于PEG和多肽的嵌段共聚物胶束包封的聚合物 - 药物包封

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Various novel di-or tri-block copolymers with hydrophilic PEG and/or polylysine in association with hydrophobic polycaprolactone segments namely PEGb- PolyLys and PEG-b-PolyLys-b-PCL, have been synthesized and characterized. Poly(Lys-g-Glu)-b-PCL has been successfully synthesized where D-gluconolactone was grafted on the -NH2 group of PolyLys. These copolymers self-assemble in water to form micelles in the size range 165 to 365 nm and CMC from 0.1 mg/ml to 2 mg/ml. Both micelle size and CMC showed a strong dependency on the hydrophobic chain length. The encapsulation of Ketoprofen and Rifampicin in the different copolymer families was assessed and encapsulation efficiency determined using UV Spectroscopy. The % drug loaded was found to depend on the interaction between drug and copolymer system. Both drugs showed chemical conjugation with PolyLys segment and physical entrapment in the PCL hydrophobic core. Higher encapsulation efficiency was obtained with Rifampicin (17-70%).
机译:已经合成并表征了与疏水性聚己内酯段与亲水PEG和/或聚赖氨酸相关联的各种新型二或三嵌段共聚物,即PEGB-多种和PEG-B-聚层-B-PCL。已经成功地合成了聚(Lys-G-Glu)-B-PCL,其中将D-葡聚糖内酯接枝在-NH 2的聚层上。这些共聚物在水中自组装以形成165至365nm和CMC的胶束,从0.1mg / ml到2mg / ml。胶束尺寸和CMC都显示出对疏水链长度的强烈依赖。评估酮洛芬和利福平素的包封,并评估使用紫外光谱测定的包封效率。发现%药物依赖于药物和共聚物体系之间的相互作用。两种药物表现出与PCL疏水芯中的多层段和物理夹带的化学缀合。用利福平(17-70%)获得较高的封装效率。

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