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Preparation, Characterization, and Biological Evaluation of Poly(Glutamic Acid)- b -Polyphenylalanine Polymersomes

机译:聚谷氨酸-b-聚苯丙氨酸多聚体的制备,表征及生物学评价

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Different types of amphiphilic macromolecular structures have been developed within recent decades to prepare the polymer particles considered as drug delivery systems. In the present research the series of amphiphilic block-copolymers containing poly(glutamatic acid) as hydrophilic, and polyphenylalanine as hydrophobic blocks was synthesized and characterized. Molecular weights for homo- and copolymers were determined by gel-permeation chromatography (GPC) and amino acid analysis, respectively. The copolymers obtained were applied for preparation of polymer particles. The specific morphology of prepared polymerosomes was proved using transmission electron microscopy (TEM). The influence on particle size of polymer concentration and pH used for self-assembly, as well as on the length of hydrophobic and hydrophilic blocks of applied copolymers, was studied by dynamic light scattering (DLS). Depending on different experimental conditions, the formation of nanoparticles with sizes from 60 to 350 nm was observed. The surface of polymersomes was modified with model protein (enzyme). No loss in biocatalytic activity was detected. Additionally, the process of encapsulation of model dyes was developed and the possibility of intracellular delivery of the dye-loaded nanoparticles was proved. Thus, the nanoparticles discussed can be considered for the creation of modern drug delivery systems.
机译:在最近的几十年中,已经开发出不同类型的两亲大分子结构以制备被认为是药物递送系统的聚合物颗粒。在本研究中,合成并表征了一系列以聚谷氨酸为亲水性和聚苯丙氨酸为疏水性嵌段的两亲嵌段共聚物。均聚物和共聚物的分子量分别通过凝胶渗透色谱法(GPC)和氨基酸分析确定。将获得的共聚物用于制备聚合物颗粒。使用透射电子显微镜(TEM)证明了所制备的聚合物小体的特定形态。通过动态光散射(DLS)研究了自组装所用聚合物浓度和pH值的粒径以及所用共聚物的疏水性和亲水性嵌段长度的影响。取决于不同的实验条件,观察到尺寸为60至350 nm的纳米颗粒的形成。用模型蛋白(酶)修饰聚合物囊泡的表面。没有检测到生物催化活性的损失。另外,开发了模型染料的包封过程,并证明了染料负载的纳米颗粒在细胞内递送的可能性。因此,可以考虑将所讨论的纳米颗粒用于创建现代药物递送系统。

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