Current research is mainly trending toward addressing the development of multifunctional nanocarriers that could precisely reach disease sites, release drugs in a controlled-manner, and act as an imaging agent for both diagnosis and targeted therapy. In this study, a pH-sensitive theranostic nanoplatform as a promising dual-functional nanovector for tumor therapy and computed tomography (CT) imaging was developed. The 21-arm star-like triblock polymer of β-cyclodextrin-{poly(ε-caprolactone)-poly(2-aminoethyl methacrylate)-poly[poly(ethylene glycol) methyl ether methacrylate]}₂₁ [β-CD-(PCL-PAEMA-PPEGMA)₂₁] with stable unimolecular micelles formed in aqueous solution was first synthesized by combined ROP with ARGET ATRP techniques and then was used as a template for fabricating gold nanoparticles (AuNPs) with uniform sizes and excellent colloidal stability in situ followed by the encapsulation of doxorubicin (DOX) with maximum entrapment efficiency up to 60% to generate the final product β-CD-(PCL-PAEMA-PPEGMA)₂₁/AuNPs/DOX. Furthermore, dissipative particle dynamics (DPD) simulations revealed further details of the formation process of unimolecular micelles and the morphologies and distributions of AuNPs and DOX. Almost 80% of DOX was released in 120 h in an acidic tumoral environment in an in vitro drug release experiment, and the experiments both in vitro and in vivo demonstrated the fact that β-CD-(PCL-PAEMA-PPEGMA)₂₁/AuNPs/DOX exhibited similar antitumor efficacy to free DOX and effective CT imaging performance. Therefore, we believe this structurally stable unimolecular micelle-based nanoplatform synergistically integrated with anticancer drug delivery and CT imaging capabilities hold great promise for future cancer theranostics.

中文翻译：

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阿霉素负载的单分子胶束稳定的金纳米颗粒作为治疗肿瘤靶向化学疗法和计算机断层扫描成像的治疗诊断纳米平台。

当前的研究主要趋向于解决多功能纳米载体的发展，这些载体可以精确地到达疾病部位，以可控的方式释放药物，并充当诊断和靶向治疗的成像剂。在这项研究中，开发了一种pH敏感的治疗药物纳米平台，作为一种有望用于肿瘤治疗和计算机断层扫描（CT）成像的双功能纳米载体。β-环糊精-{聚（ε-己内酯）-聚（甲基丙烯酸2-氨基乙酯）-聚[聚（乙二醇）甲基丙烯酸甲酯]} ₂₁ [ ₂₁ -CD-（PCL ）的21臂星形三嵌段聚合物-PAEMA-PPEGMA）₂₁首先通过结合ROP和ARGET ATRP技术合成在水溶液中形成稳定的单分子胶束，然后将其用作制备原位均匀且具有良好胶体稳定性的金纳米颗粒（AuNP）的模板，然后将阿霉素（DOX）包封）的最大包封率高达60％，以生成最终产物β-CD-（PCL-PAEMA-PPEGMA）₂₁/ AuNPs / DOX。此外，耗散粒子动力学（DPD）模拟揭示了单分子胶束的形成过程以及AuNPs和DOX的形态和分布的更多细节。在体外药物释放实验中，在酸性肿瘤环境中在120小时内释放了近80％的DOX，并且该实验在体外和体内实验均证明了β-CD-（PCL-PAEMA-PPEGMA）₂₁ / AuNPs的存在。 / DOX表现出与游离DOX相似的抗肿瘤功效和有效的CT成像性能。因此，我们认为，这种结构稳定，基于单分子胶束的纳米平台与抗癌药物的递送和CT成像功能协同集成，对未来的癌症治疗学具有广阔的前景。