National Engineering Research Center for Biomaterials, Sichuan University, 29 Wangjiang Road, Chengdu 610064, China.
Theranostics. 2019 Aug 27;9(22):6618-6630. doi: 10.7150/thno.33901. eCollection 2019.
Intelligent polymeric micelles with fluorescence imaging feature have been emerged as promising tools for theranostics. However, conventional fluorescent dyes are limited by short wavelength excitation, interference of tissue autofluorescence, limited imaging depth and quenched emission in aggregation state. : We synthesized a novel mPEG-SS-Poly (AEMA--TBIS) (mPEATss) copolymer to develop multifunctional polymeric micelles with great AIE feature for cancer therapy and AIE active two-photon bioimaging. The stimuli-responsive behavior and AIE active two-photon cell and tissue imaging as well as and antitumor ability of DOX-loaded mPEATss were studied. : mPEATss micelles showed excellent AIE active two-photon cell imaging ability and deep tissue imaging ability. Antitumor drug DOX could be encapsulated to form a drug-loaded micellar system with a small diameter of 65 nm. The disassembly and charge-conversion of mPEATss micelles could be triggered by acidic environment, resulting in accelerated drug release and great antitumor efficacy. , imaging and pharmacokinetic study demonstrated that mPEATss micelles could efficiently accumulate in tumor sites, which ensured ideal anticancer effect. : This pH and redox dual responsive and AIE active two-photon imaging polymeric micelles would be a promising candidate for theranostics.
具有荧光成像特性的智能聚合物胶束已成为治疗和诊断一体化的有前途的工具。然而,传统的荧光染料受到短波长激发、组织自发荧光干扰、有限的成像深度和聚集状态下的荧光猝灭的限制。我们合成了一种新型的 mPEG-SS-Poly (AEMA-TBIS) (mPEATss) 共聚物,用于开发具有出色聚集诱导发光 (AIE) 特性的多功能聚合物胶束,用于癌症治疗和 AIE 活性双光子生物成像。研究了载药 mPEATss 的刺激响应行为和 AIE 活性双光子细胞和组织成像以及 DOX 的抗肿瘤能力。mPEATss 胶束表现出优异的 AIE 活性双光子细胞成像能力和深层组织成像能力。抗肿瘤药物 DOX 可以被包裹形成直径为 65nm 的载药胶束系统。mPEATss 胶束的解组装和电荷转换可以被酸性环境触发,导致药物的加速释放和强大的抗肿瘤功效。体内成像和药代动力学研究表明,mPEATss 胶束可以有效地在肿瘤部位积累,从而确保理想的抗癌效果。这种 pH 和氧化还原双重响应和 AIE 活性双光子成像聚合物胶束将是治疗和诊断一体化的有前途的候选物。