文献：AIE-Featured Redox-Sensitive Micelles for Bioimaging and Efficient Anticancer Drug Delivery

作者：by Wei Zhao 1,†,Zixue Li 1,†,Na Liang 2,*,Jiyang Liu 1,Pengfei Yan 1 andShaoping Sun

 文献链接：https://www.mdpi.com/1422-0067/23/18/10801

The amphiphilicity of Bi(mPEG-S-S)-TPE makes it trend to self-assemble into micelles, with TPE aggregated to serve as the core and mPEG formed the shell. PTX could be loaded into the micelles due to the hydrophobic interaction. For the optimized PTX-loaded micelles, the particle size was 96 ± 3.9 nm, and PDI was 0.358. Notably, such size facilitates the particles to spontaneously aggregate in the tumor via the EPR effect, keep a low level of uptake by the RES, and minimize renal excretion [32]. Zeta potential measurement revealed the PTX-loaded micelles charged negative potential, with a value as high as −39.9 mV, which implied that there was repulsive force among the particles, and the micelles would exhibit excellent stability. Moreover, the negative charge would protect the micelles from recognition by the RES [33]. The drug loading and encapsulation efficiency were determined to be 6.8% and 74.8%, respectively.

To confirm the existing state of PTX in Bi(mPEG-S-S)-TPE micelles, XRD analysis was conducted. As observed from Figure 3A, PTX showed diffraction peaks in the 2θ range of 5° to 30°. The pattern of the physical mixture was the simple superposition of the diagrams of blank micelles and PTX. In contrast, the diagram of drug-loaded micelles was similar as the bare micelles without any crystalline peaks of PTX detected, which implied that PTX was loaded in the micelles.

负载PTX的Bi（mPEG-S-S）-TPE胶束的表征

Bi（mPEG-S-S）-TPE的两亲性使其倾向于自组装成胶束，TPE聚集成核，mPEG形成壳。由于疏水相互作用，PTX可以被加载到胶束中。对于优化的PTX负载胶束，粒径为96±3.9nm，PDI为0.358。

这种尺寸有助于颗粒通过EPR效应在肿瘤中自发聚集，保持RES的低摄取水平，并最大限度地减少肾脏排泄。Zeta电位测量显示，负载PTX的胶束带负电位，其值高达-39.9 mV，这意味着颗粒之间存在排斥力，胶束将表现出优异的稳定性。此外，负电荷将保护胶束免受RES的识别。载药量和包封率分别为6.8%和74.8%。

为了确认PTX在Bi（mPEG-S-S）-TPE胶束中的存在状态，进行了XRD分析。PTX在5°至30°的2θ范围内显示出衍射峰。物理混合物的模式是空白胶束和PTX图的简单叠加。相比之下，载药胶束的图与未检测到任何PTX结晶峰的裸胶束相似，这意味着PTX被装载在胶束中。

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