Nanoparticles (NPs)‐based diagnosis and phototherapy are emerging as the cutting‐edge technologies for detection and treatment of cancer but their applications are still limited since insufficient and heterogeneous NPs accumulation in cancer often causes recurrence. To overcome these limitations, multifunctional microbubbles (MBs) were constructed with 1, 1‐dioctadecyl‐3, 3, 3, 3‐tetramethylindotricarbocyanine iodide (DiR) and porphyrin grafted lipid (PGL). Both DiR and PGL self‐assembled as microbubbles, the as‐designed PGL‐DiR MBs possess remarkably high drug loading contents (5.8% PGL and 10.38% DiR) and stable co‐delivery drug combinations. In vivo experiments showed PGL‐DiR MBs could serve as an excellent ultrasound contrast agent to enhance ultrasound imaging greatly for identifying the location and size of the tumors. Upon exposure to ultrasound, in situ conversion of PGL‐DiR MBs into nanoparticles resulted in a remarkable increase in fluorescence intensity (~5 folds) in tumor compared with PGL‐DiR NPs, validating the enhanced tumor accumulation and cellular uptake of therapeutic agents. PGL‐DiR MBs showed complete tumor ablation without recurrence in vivo, while PGL‐DiR NPs showed only 72.6% tumor growth inhibition at the same dose. We believe that PGL‐DiR MBs will soon reach their full potential as an important class of phototherapeutic formulations and will contribute to remarkable advances in cancer treatments.

中文翻译：

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通过超声介导的近红外花菁/卟啉微气泡原位转化为纳米粒子，提高联合癌症光疗的治疗效果

基于纳米颗粒（NPs）的诊断和光疗已成为检测和治疗癌症的前沿技术，但由于在癌症中积累的不足而异质的NPs通常会导致复发，因此其应用仍然受到限制。为了克服这些限制，多功能微泡（MBs）分别由1、1-二十八烷基-3、3、3、3-四甲基吲哚环花青碘化物（DiR）和卟啉接枝脂质（PGL）构成。DiR和PGL自组装成微泡，设计好的PGL-DiR MB具有很高的载药量（5.8％PGL和10.38％DiR）和稳定的共递送药物组合。体内实验表明，PGL-DiR MBs可以作为出色的超声造影剂，极大地增强超声成像，从而确定肿瘤的位置和大小。与PGL-DiR NPs相比，超声暴露后，PGL-DiR MBs原位转化为纳米颗粒导致肿瘤中荧光强度显着增加（〜5倍），证实了肿瘤积累和治疗药物的细胞吸收增加。PGL-DiR MBs在体内完全消融而无复发，而PGL-DiR NPs在相同剂量下仅显示72.6％的肿瘤生长抑制作用。我们相信，PGL-DiR MBs将很快成为一类重要的光疗制剂，充分发挥其潜力，并将为癌症治疗方面的显着进步做出贡献。PGL-DiR MBs在体内完全消融而无复发，而PGL-DiR NPs在相同剂量下仅显示72.6％的肿瘤生长抑制作用。我们相信，PGL-DiR MBs将很快成为一类重要的光疗制剂，充分发挥其潜力，并将为癌症治疗方面的显着进步做出贡献。PGL-DiR MBs在体内完全消融而无复发，而PGL-DiR NPs在相同剂量下仅显示72.6％的肿瘤生长抑制作用。我们相信，PGL-DiR MBs将很快成为一类重要的光疗制剂，充分发挥其潜力，并将为癌症治疗方面的显着进步做出贡献。