文獻(xiàn)：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

 文獻(xiàn)鏈接：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.

負(fù)載PTX的Bi（mPEG-S-S）-TPE膠束的表征

Bi（mPEG-S-S）-TPE的兩親性使其傾向于自組裝成膠束，TPE聚集成核，mPEG形成殼。由于疏水相互作用，PTX可以被加載到膠束中。對(duì)于優(yōu)化的PTX負(fù)載膠束，粒徑為96±3.9nm，PDI為0.358。

這種尺寸有助于顆粒通過(guò)EPR效應(yīng)在腫瘤中自發(fā)聚集，保持RES的低攝取水平，并最大限度地減少腎臟排泄。Zeta電位測(cè)量顯示，負(fù)載PTX的膠束帶負(fù)電位，其值高達(dá)-39.9 mV，這意味著顆粒之間存在排斥力，膠束將表現(xiàn)出優(yōu)異的穩(wěn)定性。此外，負(fù)電荷將保護(hù)膠束免受RES的識(shí)別。載藥量和包封率分別為6.8%和74.8%。

為了確認(rèn)PTX在Bi（mPEG-S-S）-TPE膠束中的存在狀態(tài)，進(jìn)行了XRD分析。PTX在5°至30°的2θ范圍內(nèi)顯示出衍射峰。物理混合物的模式是空白膠束和PTX圖的簡(jiǎn)單疊加。相比之下，載藥膠束的圖與未檢測(cè)到任何PTX結(jié)晶峰的裸膠束相似，這意味著PTX被裝載在膠束中。

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