University of São Paulo (USP), Chemical Insititut of São Carlos (IQSC), Sao Carlos, SP, Brazil.
São Paulo State University (UNESP), School of Pharmaceutical Sciences, Araraquara, SP, Brazil.
Photodiagnosis Photodyn Ther. 2023 Dec;44:103858. doi: 10.1016/j.pdpdt.2023.103858. Epub 2023 Oct 26.
Cyclodextrins (CDs) are molecules approved by the FDA and show promise in increasing the solubility of hydrophobic molecules and making them more available to the skin. These CDs have been used to form complexes with some photosensitizers for Photodynamic Therapy (PDT), such as Hypericin (HY). HY is a lipophilic photosensitizer known for its exceptional fluorescence and singlet oxygen quantum yield generation of over 20 % under 590 nm irradiation. In this study, we found a six-fold increase in the release of HY in vitro after complexation with β-CD. The β-CDHY assembly also demonstrated better skin retention, which is crucial for the topical application of this photosensitizer. Furthermore, the β-CD complexation led to a significant increase in the phototoxicity of HY at three different light doses (3, 6, and 10 J cm) due to its improved water solubility and higher in vitro accumulation (approximately two times compared with free HY) in HeLa and Vero cell lines.
环糊精（CDs）是 FDA 批准的物质，在提高疏水分子的溶解度并使其更易被皮肤吸收方面显示出潜力。这些 CDs 已被用于与一些光动力治疗（PDT）的光敏剂形成复合物，如金丝桃素（HY）。HY 是一种亲脂性光敏剂，以其在 590nm 照射下超过 20%的单重态氧量子产率生成的出色荧光而闻名。在这项研究中，我们发现 HY 与β-CD 络合后，体外释放增加了六倍。β-CDHY 组装体还表现出更好的皮肤保留性，这对于这种光敏剂的局部应用至关重要。此外，由于其水溶性提高和 HeLa 和 Vero 细胞系中体外积累（与游离 HY 相比约增加两倍）更高，β-CD 络合导致 HY 在三种不同光剂量（3、6 和 10 J cm）下的光毒性显著增加。
