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Co-assembly of block copolymers as a tool for developing novel micellar carriers of insulin for controlled drug delivery
European Polymer Journal ( IF 6 ) Pub Date : 2018-04-27
Katya Kamenova, Emi Haladjova, Georgy Grancharov, Mariya Kyulavska, Virginia Tzankova, Denitsa Aluani, Krassimira Yoncheva, Stergios Pispas, Petar Petrov

In this study the co-assembly of two amphiphilic block copolymers with tailored composition and molecular characteristics, poly(ethylene oxide)-poly(ε-caprolactone)-b-poly(ethylene oxide) (PEO113-b-PCL35-b-PEO113) and poly(2-(dimethylamino)ethyl methacrylate)-b-poly(ε-caprolactone)-b-poly(2-(dimethylamino)ethyl methacrylate) (PDMAEMA20-b-PCL70-b-PDMAEMA20), was employed for preparation of a novel micellar system for controlled delivery of insulin. Mixed block copolymer micelles (MBCMs) of three different compositions were prepared by blending the two copolymers at molar ratios of 7:3, 1:1 and 3:7. Next, the electrostatic complexation between insulin and MBCMs with a focus on particle size, morphology, zeta potential and colloid stability as a function of insulin concentration in the aqueous solution was investigated by dynamic and electrophoretic light scattering as well as atomic force microscopy. The properties of systems were proven to depend on MBCMs composition and protein concentration. In vitro cytotoxicity of blank and insulin-loaded carriers was assessed by standard MTT (3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide) test. The release profile of insulin from selected carriers in phosphate buffer (pH 7.4) was also studied.



中文翻译:

嵌段共聚物的共组装作为开发新型胰岛素胶束载体以控制药物输送的工具

在这项研究中,两种具有特定组成和分子特性的两亲嵌段共聚物,聚(环氧乙烷)-聚(ε-己内酯)-b-聚环氧乙烷(PEO 113 -b-PCL 35 -b- PEO 113)和聚(甲基丙烯酸2-(二甲基氨基)乙酯)-b-聚(ε-己内酯)-b-聚甲基丙烯酸2-(二甲基氨基)乙酯(PDMAEMA 20 -b-PCL 70 -b-PDMAEMA 20)被用于制备新的胶束系统以控制胰岛素的递送。通过以摩尔比为7:3、1:1和3:7的方式共混两种共聚物,制备了三种不同组成的混合嵌段共聚物胶束(MBCM)。接下来,通过动态和电泳光散射以及原子力显微镜研究了胰岛素和MBCM之间的静电络合,重点是粒径,形态,ζ电位和胶体稳定性与胰岛素浓度在水溶液中的关系。事实证明,系统的性能取决于MBCM的组成和蛋白质浓度。体外通过标准MTT(3-(4,5-二甲基噻唑-2-基)-2,5-二苯基四唑溴化物)测试评估空白和载有胰岛素的载体的细胞毒性。还研究了在磷酸盐缓冲液(pH 7.4)中胰岛素从选定载体的释放曲线。

更新日期:2018-04-27
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