Bordignon Nicolò, Köber Mariana, Chinigò Giorgia, Pontremoli Carlotta, Sansone Ettore, Vargas-Nadal Guillem, Moran Plata Maria Jesus, Fiorio Pla Alessandra, Barbero Nadia, Morla-Folch Judit, Ventosa Nora
Institut de Ciència de Materials de Barcelona, ICMAB-CSIC, Campus UAB, Bellaterra, 08193 Catalonia, Spain.
Department of Life Sciences and Systems Biology, University of Torino, Via Accademia Albertina 13, 10123 Turin, Italy.
Pharmaceutics. 2023 Mar 10;15(3):902. doi: 10.3390/pharmaceutics15030902.
Photodynamic therapy is a non-invasive therapeutic strategy that combines external light with a photosensitizer (PS) to destroy abnormal cells. Despite the great progress in the development of new photosensitizers with improved efficacy, the PS's photosensitivity, high hydrophobicity, and tumor target avidity still represent the main challenges. Herein, newly synthesized brominated squaraine, exhibiting intense absorption in the red/near-infrared region, has been successfully incorporated into Quatsome (QS) nanovesicles at different loadings. The formulations under study have been characterized and interrogated in vitro for cytotoxicity, cellular uptake, and PDT efficiency in a breast cancer cell line. The nanoencapsulation of brominated squaraine into QS overcomes the non-water solubility limitation of the brominated squaraine without compromising its ability to generate ROS rapidly. In addition, PDT effectiveness is maximized due to the highly localized PS loadings in the QS. This strategy allows using a therapeutic squaraine concentration that is 100 times lower than the concentration of free squaraine usually employed in PDT. Taken together, our results reveal the benefits of the incorporation of brominated squaraine into QS to optimize their photoactive properties and support their applicability as photosensitizer agents for PDT.
光动力疗法是一种非侵入性治疗策略,它将外部光与光敏剂(PS)结合起来以破坏异常细胞。尽管在开发具有更高疗效的新型光敏剂方面取得了巨大进展,但光敏剂的光敏性、高疏水性和肿瘤靶向亲和力仍然是主要挑战。在此,新合成的在红/近红外区域表现出强烈吸收的溴化方酸菁已成功以不同载量掺入Quatsome(QS)纳米囊泡中。所研究的制剂已在体外对乳腺癌细胞系的细胞毒性、细胞摄取和光动力疗法效率进行了表征和研究。将溴化方酸菁纳米包封到QS中克服了溴化方酸菁的非水溶性限制,同时不影响其快速产生活性氧的能力。此外,由于QS中高度局部化的PS载量,光动力疗法的有效性得以最大化。这种策略允许使用比光动力疗法中通常使用的游离方酸菁浓度低100倍的治疗性方酸菁浓度。综上所述,我们的结果揭示了将溴化方酸菁掺入QS以优化其光活性特性并支持其作为光动力疗法光敏剂的适用性的益处。