光动力疗法
超声
Zeta电位
光敏剂
金丝桃素
分散性
生物利用度
细胞毒性
化学
纳米颗粒
材料科学
共焦显微镜
生物物理学
色谱法
核化学
体外
纳米技术
药理学
有机化学
生物化学
医学
细胞生物学
生物
作者
Hui Ling,Laudemir Carlos Varanda,Janice Rodrigues Perussi,Emanuel Carrilho
标识
DOI:10.1016/j.jphotobiol.2021.112303
摘要
Hypericin (Hy) is a hydrophobic photosensitizer used in photodynamic therapy for cancer therapeutic. In this study, Hy-loaded oil-in-water (O/W) nanoemulsions (NEs) were produced by the ultrasonication method combing different biocompatible oils and surfactants to enhance Hy aqueous solubility and bioavailability. Experimental parameters were optimized by the characterization of droplet size, zeta potential, and physicochemical properties. In vitro studies based on the release profile, cytotoxicity, cell morphology, and Hy intracellular accumulation were assayed. Hy at 100 mg L−1 was incorporated into the low viscosity (~0.005 Pa s) NEs with spherical droplets averaging 20–40 nm in size and polydispersity index <0.02. Hy release from the NE was significantly higher (4-fold) than its suspension (p < 0.001). The NEs demonstrated good physical stability during storage at 5 °C for at least six months. The Hy-loaded NEs exhibited an IC50 value 6-fold lower than Hy suspension during PDT against breast cancer cell lines (MCF-7). Cell microscopy imaging confirmed the increased cytotoxic effects of Hy-loaded NEs, showing damaged and apoptotic cells. Confocal laser scanning microscopy evidenced greater Hy delivery through NE into MCF-7 cells followed by improved intracellular ROS generation. Our results suggest that the Hy-loaded NEs can improve hypericin efficacy and assist Hy-PDT's preclinical development as a cancer treatment.
科研通智能强力驱动
Strongly Powered by AbleSci AI