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首页> 外文期刊>Biomacromolecules >Poly(2-methyl-2-oxazoline)-b-poly(tetrahydrofuran)-b-poly(2-methyl-2-oxazoline) Amphiphilic Triblock Copolymers: Synthesis, Physicochemical Characterizations, and Hydrosolubilizing Properties
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Poly(2-methyl-2-oxazoline)-b-poly(tetrahydrofuran)-b-poly(2-methyl-2-oxazoline) Amphiphilic Triblock Copolymers: Synthesis, Physicochemical Characterizations, and Hydrosolubilizing Properties

机译：聚（2-甲基-2-恶唑啉）-b-聚（四氢呋喃）-b-聚（2-甲基-2-恶唑啉）两亲性三嵌段共聚物：合成，理化性质和加氢性能

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Block copolymers assembled into micelles have gained a lot of attention to improve drug delivery. The recent drawbacks of the poly(ethylene oxide) blocks (PEO) contained in amphiphilic pluronics derivatives made of a central poly(propylene oxide) block surrounded by two PEO blocks were recently revealed, opening the way to the design of new amphiphilic block copolymers able to self-assemble in water and to entrap molecules of interest. Here, a family of p(methyloxazoline)-b-p(tetrahydrofuran)-b-p(methyloxazoline) triblock copolymers (called TBCP) is synthesized using cationic ring opening polymerization. Studies of micelle formation using dynamic light scattering, isothermal titration calorimetry (ITC), NMR diffusion-ordered spectroscopy (DOSY), and fluorescence experiments lead us to draw a relationship between copolymer structure and the physicochemical properties of the block copolymers (critical micellar concentration (CMC), Nagg, core diameter, shell thickness, etc.). The packing parameter of the block copolymers indicates the formation of a core-corona structure. Hydrosolubilizing properties of TBCPs were exemplified with curcumin selected as a highly insoluble drug model. Curcumin, a natural polyphenolic compound, has shown a large spectrum of biological and pharmacological activity, including anti-inflammatory, antimicrobial, antioxidant, and anticarcinogenic activities. An optimized formulation process reveals that the aggregation number is the parameter affecting drug encapsulation. Patch clamp experiments carried out to study the interaction of TBCP with the cell membrane demonstrate their permeation property suitable to promote the cellular internalization of curcumin.
机译：组装成胶束的嵌段共聚物已引起人们的广泛关注，以改善药物的递送。最近发现了由两片PEO嵌段包围的中心聚环氧丙烷嵌段制成的两亲性pluronics衍生物中包含的聚环氧乙烷嵌段（PEO）的最新缺陷，这为设计新型的两亲嵌段共聚物开辟了道路在水中自组装并捕获感兴趣的分子。在此，使用阳离子开环聚合法合成了对（甲基恶唑啉）-b-p（四氢呋喃）-b-p（甲基恶唑啉）三嵌段共聚物（称为TBCP）。使用动态光散射，等温滴定量热（ITC），NMR扩散有序光谱法（DOSY）和荧光实验研究胶束形成，使我们得出了共聚物结构与嵌段共聚物的理化性质之间的关系（临界胶束浓度（ CMC），纳格，芯直径，壳厚度等）。嵌段共聚物的填充参数表明形成了芯-电晕结构。 TBCP的增溶剂性能以姜黄素为高不溶性药物模型为例。姜黄素是一种天然的多酚化合物，已显示出广泛的生物学和药理活性，包括抗炎，抗微生物，抗氧化剂和抗癌活性。优化的配方过程表明，聚集数是影响药物封装的参数。进行膜片钳实验以研究TBCP与细胞膜的相互作用，证明它们的渗透特性适合促进姜黄素的细胞内在化。

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