Polymersome formation induced by encapsulation of water-insoluble molecules within ABC triblock terpolymers,Polymer Chemistry

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Polymersome formation induced by encapsulation of water-insoluble molecules within ABC triblock terpolymers
Polymer Chemistry ( IF 4.1 ) Pub Date : 2020-04-21 , DOI: 10.1039/d0py00426j
Rintaro Takahashi _{1,

2,

3,

4} , Shotaro Miwa _{1,

2,

3,

4} , Carsten Rössel _{5,

6,

7,

8} , Shota Fujii _{1,

2,

3,

4} , Ji Ha Lee _{1,

2,

3,

4} , Felix H. Schacher _{5,

6,

7,

8,

9} , Kazuo Sakurai _{1,

2,

3,

4}

Affiliation

Polymeric micelles have been extensively studied as nanoscale drug carriers. Knowing how the encapsulation of drugs alters the micellar structure is one of the most important issues for the biomedical application of amphiphilic block copolymers. However, little is known so far about the structural changes that micelles undergo upon loading with water-insoluble guests. Herein, we investigate the micellar morphology of ABC triblock terpolymers after loading with various water-insoluble molecules (naphthalene and its derivatives as drug-equivalent model molecules). The triblock terpolymer features a poly(ethylene oxide) (PEO) block, a poly(allyl glycidyl ether) segment which has been functionalized with carboxylic acid moieties (PAGE_COOH), and poly(tert-butyl glycidyl ether) (PtBGE) as a hydrophobic block. Structural analysis by small-angle X-ray scattering (SAXS) and cryogenic and conventional transmission electron microscopy (TEM) found that a morphological transition from spherical micelles to vesicles (polymersomes) was induced by loading the guest molecules at pH 4, whilst the spherical and prolate morphologies remained unchanged upon loading at pH 6 and 8. This study highlights the dynamics and morphological changes of polymeric micelles upon loading with guest molecules.

中文翻译：

通过将水不溶性分子包裹在ABC三嵌段三元共聚物中诱导的聚合物小体形成

高分子胶束已被广泛研究为纳米级药物载体。对于两亲性嵌段共聚物的生物医学应用而言，了解药物的封装如何改变胶束结构是最重要的问题之一。然而，到目前为止，关于胶束在负载水不溶性客体时发生的结构变化知之甚少。在本文中，我们研究了负载各种水不溶性分子（萘及其衍生物作为药物等效模型分子）后ABC三嵌段三元共聚物的胶束形态。三嵌段三元共聚物具有一个聚环氧乙烷（PEO）嵌段，一个已被羧酸部分（PAGE _COOH）官能化的聚（烯丙基缩水甘油醚）链段和一个聚（叔丁基缩水甘油醚）（Pt BGE）作为疏水性嵌段。通过小角X射线散射（SAXS），低温和常规透射电子显微镜（TEM）进行的结构分析发现，通过将客体分子加载到pH 4来诱导从球形胶束到囊泡（多聚体）的形态转变。 pH值为6和8时，胶束和扁长形的形态保持不变。该研究着重介绍了载有客体分子的聚合物胶束的动力学和形态变化。

更新日期：2020-04-21

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