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新型温敏性胶束由两亲性羟丙基甲基纤维素嵌段- JEFFAMINE 共聚物制备而成。

Novel thermo-responsive micelles prepared from amphiphilic hydroxypropyl methyl cellulose-block-JEFFAMINE copolymers.

机构信息

Institut Européen des Membranes, UMR 5635 CNRS-UM-ENSCM, Université de Montpellier, Place Eugene Bataillon, 34095 Montpellier Cedex 5, France.

Institut Européen des Membranes, UMR 5635 CNRS-UM-ENSCM, Université de Montpellier, Place Eugene Bataillon, 34095 Montpellier Cedex 5, France.

出版信息

Int J Biol Macromol. 2019 Aug 15;135:38-45. doi: 10.1016/j.ijbiomac.2019.05.087. Epub 2019 May 20.

Abstract

A series of amphiphilic and thermo-responsive block copolymers were synthesized by reductive amination between the aldehyde endgroup of hydrophilic HPMC and the amine group of monoamine, diamine, or triamine JEFFAMINE as hydrophobic block. The resulting diblock, triblock and three-armed copolymers with different hydrophilic/hydrophobic ratios and block lengths were characterized by NMR, FT-IR, DOSY-NMR and SEC. The cloud point (CP) of copolymers was determined by UV-visible spectrometer. Data show that both the geometrical structure and the molar mass of HPMC affect the CP of HPMC-JEF copolymers. The higher the hydrophilic/hydrophobic ratio, the higher the CP of copolymers which is lower than that of HPMC homopolymers. The self-assembly behavior of the copolymers was investigated from dynamic light scattering, transmission electron microscopy, and critical micelle concentration (CMC) measurements. Spherical nano-micelles are obtained by self-assembly of copolymers in aqueous solution, and the micelle size can be tailored by varying the block length of HPMC and the geometrical structure. Three-armed HPMC-JEF copolymers present lower CMC and smaller micelle size as compared to linear diblock and triblock ones. MTT assay evidenced the cytocompatibility of HPMC-JEF copolymers, indicating that they could be promising as drug carrier in drug delivery systems.

摘要

一系列两亲性和温敏性嵌段共聚物通过亲水性 HPMC 的醛端基与单胺、二胺或三胺 JEFFAMINE 的氨基之间的还原胺化反应合成。所得的具有不同亲水/亲水平衡比和嵌段长度的二嵌段、三嵌段和三臂共聚物通过 NMR、FT-IR、DOSY-NMR 和 SEC 进行了表征。通过紫外可见分光光度计测定共聚物的浊点(CP)。数据表明,HPMC 的几何结构和摩尔质量都影响 HPMC-JEF 共聚物的 CP。亲水/亲水平衡比越高,共聚物的 CP 越高,低于 HPMC 均聚物的 CP。通过动态光散射、透射电子显微镜和临界胶束浓度(CMC)测量研究了共聚物的自组装行为。共聚物在水溶液中自组装形成球形纳米胶束,通过改变 HPMC 的嵌段长度和几何结构可以调整胶束的尺寸。与线性二嵌段和三嵌段共聚物相比,三臂 HPMC-JEF 共聚物具有更低的 CMC 和更小的胶束尺寸。MTT 试验证明了 HPMC-JEF 共聚物的细胞相容性,表明它们有望作为药物传递系统中的药物载体。

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