Department of Pharmaceutics, School of Pharmacy, Qingdao University, Qingdao, People's Republic of China.
Department of Pharmaceutics, School of Biomedical Science and Pharmacy, University of Newcastle, Newcastle, New South Wales, Australia.
Int J Nanomedicine. 2019 Jul 8;14:4931-4947. doi: 10.2147/IJN.S203171. eCollection 2019.
Phototherapy, including photothermal therapy (PTT) and photodynamic therapy (PDT), is a promising noninvasive strategy in the treatment of cancers due to its highly localized specificity to tumors and minimal side effects to normal tissues. However, single phototherapy often causes tumor recurrence which hinders its clinical applications. Therefore, developing a NIR-guided dendritic nanoplatform for improving the phototherapy effect and reducing the recurrence of tumors by synergistic chemotherapy and phototherapy is essential.
A fluorescent targeting ligand, insisting of ICG derivative cypate and a tumor penetration peptide iRGD (CRGDKGPDC), was covalently combined with PAMAM dendrimer to prepare a single agent-based dendritic theranostic nanoplatform iRGD-cypate-PAMAM-DTX (RCPD).
Compared with free cypate, the resulted RCPD could generate enhanced singlet oxygen species while maintaining its fluorescence intensity and heat generation ability when subjected to NIR irradiation. Furthermore, our in vitro and in vivo therapeutic studies demonstrated that compared with phototherapy or chemotherapy alone, the combinatorial chemo-photo treatment of RCPD with the local exposure of NIR light can significantly improve anti-tumor efficiency and reduce the risk of recurrence of tumors.
The multifunctional theranostic platform (RCPD) could be used as a promising method for NIR fluorescence image-guided combinatorial treatment of tumor cancers.
光疗，包括光热疗法（PTT）和光动力疗法（PDT），是一种很有前途的非侵入性治疗癌症的策略，因为它对肿瘤具有高度的局部特异性，对正常组织的副作用极小。然而，单一的光疗往往会导致肿瘤复发，这阻碍了它的临床应用。因此，开发一种近红外（NIR）引导的树枝状纳米平台，通过协同化学疗法和光疗来提高光疗效果和降低肿瘤复发率是至关重要的。
将一种荧光靶向配体，由吲哚菁绿（ICG）衍生物 cypate 和肿瘤穿透肽 iRGD（CRGDKGPDC）组成，共价结合到 PAMAM 树枝状大分子上，制备了一种基于单药的树枝状治疗性纳米平台 iRGD-cypate-PAMAM-DTX（RCPD）。
与游离的 cypate 相比，所得的 RCPD 在接受近红外辐射时可以产生增强的单线态氧，同时保持其荧光强度和发热能力。此外，我们的体外和体内治疗研究表明，与光疗或单独化疗相比，RCPD 与近红外光局部照射的联合化疗-光疗治疗可以显著提高抗肿瘤效率，并降低肿瘤复发的风险。
多功能治疗平台（RCPD）可以作为一种有前途的近红外荧光成像引导的肿瘤联合治疗方法。
