College of Chemistry, Beijing Normal University, Beijing 100875, PR China.
China National Institute for Food and Drug Control, Institute of Chemical Drug Control, TianTanXiLi 2, Beijing 100050, PR China.
Bioorg Chem. 2022 Feb;119:105559. doi: 10.1016/j.bioorg.2021.105559. Epub 2021 Dec 15.
Stimuli-responsive drug delivery systems (DDSs) based on amphiphilic polymers have attracted much attention. In this study, we reported an innovative HO-responsive amphiphilic polymer (TBP), bearing a HO-sensitive phenylboronic ester, AIE fluorophore tetraphenylethene (TPE) hydrophobic, and polyethylene glycol hydrophilic (PEG) moieties. TBP could self-assemble into micelles with an encapsulation efficiency as high as 74.9% for doxorubicin (DOX) in aqueous solution. In the presence of HO, TBP micelles was decomposed by oxidation, hydrolysis and rearrangement, leading to almost 80% DOX release from TBP@DOX micelles. TBP and the corresponding degradation products were biocompatible, while TBP@DOX micelles only displayed obvious toxicity toward cancer cells. Drug delivery process was clearly monitored by confocal laser scanning microscopic (CLSM) and flow cytometry (FCM) analysis. Moreover, in vivo anticancer study showed that TBP@DOX micelles were accumulated in tumor region of nude mice and effectively inhibited tumor growth. The results suggested that the reported HO-responsive amphiphilic polymer displayed great potential in drug delivery and tumor therapy.
基于两亲聚合物的刺激响应型药物传递系统（DDS）引起了广泛关注。在本研究中，我们报道了一种创新的 HO 响应性两亲聚合物（TBP），其具有 HO 敏感的苯硼酸酯、AIE 荧光团四苯乙烯（TPE）疏水性和亲水性聚乙二醇（PEG）部分。TBP 可以在水溶液中自组装成胶束，对阿霉素（DOX）的包封效率高达 74.9%。在 HO 的存在下，TBP 胶束通过氧化、水解和重排分解，导致 TBP@DOX 胶束中约 80%的 DOX 释放。TBP 和相应的降解产物具有生物相容性，而 TBP@DOX 胶束仅对癌细胞表现出明显的毒性。通过共聚焦激光扫描显微镜（CLSM）和流式细胞术（FCM）分析清楚地监测了药物传递过程。此外，体内抗癌研究表明，TBP@DOX 胶束在裸鼠的肿瘤区域聚集，并有效抑制肿瘤生长。结果表明，所报道的 HO 响应性两亲聚合物在药物传递和肿瘤治疗中具有巨大的潜力。
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