Bender Lena, Preis Eduard, Engelhardt Konrad H, Amin Muhammad Umair, Ayoub Abdallah M, Librizzi Damiano, Roschenko Valeri, Schulze Jan, Yousefi Behrooz H, Schaefer Jens, Bakowsky Udo
Department of Pharmaceutics and Biopharmaceutics, University of Marburg, Robert-Koch-Str. 4, Marburg 35037, Germany.
Center for Tumor Biology and Immunology (ZTI), Core Facility Molecular Imaging, Department of Nuclear Medicine, University of Marburg, Hans-Meerwein-Str. 3, Marburg 35043, Germany.
Eur J Pharm Sci. 2024 May 1;196:106748. doi: 10.1016/j.ejps.2024.106748. Epub 2024 Mar 11.
Lung cancer is one of the most common causes of high mortality worldwide. Current treatment strategies, e.g., surgery, radiotherapy, chemotherapy, and immunotherapy, insufficiently affect the overall outcome. In this study, we used curcumin as a natural photosensitizer in photodynamic therapy and encapsulated it in liposomes consisting of stabilizing tetraether lipids aiming for a pulmonary drug delivery system against lung cancer. The liposomes with either hydrolyzed glycerol-dialkyl-glycerol tetraether (hGDGT) in different ratios or hydrolyzed glycerol-dialkyl-nonitol tetraether (hGDNT) were prepared by dual centrifugation (DC), an innovative method for liposome preparation. The liposomes' physicochemical characteristics before and after nebulization and other nebulization characteristics confirmed their suitability. Morphological characterization using atomic force and transmission electron microscopy showed proper vesicular structures indicative of liposomes. Qualitative and quantitative uptake of the curcumin-loaded liposomes in lung adenocarcinoma (A549) cells was visualized and proven. Phototoxic effects of the liposomes were detected on A549 cells, showing decreased cell viability. The generation of reactive oxygen species required for PDT and disruption of mitochondrial membrane potential were confirmed. Moreover, the chorioallantoic membrane (CAM) model was used to further evaluate biocompatibility and photodynamic efficacy in a 3D cell culture context. Photodynamic efficacy was assessed by PET/CT after nebulization of the liposomes onto the xenografted tumors on the CAM with subsequent irradiation. The physicochemical properties and the efficacy of tetraether lipid liposomes encapsulating curcumin, especially liposomes containing hGDNT, in 2D and 3D cell cultures seem promising for future PDT usage against lung cancer.
肺癌是全球死亡率最高的常见病因之一。目前的治疗策略,如手术、放疗、化疗和免疫疗法,对总体治疗效果的影响并不充分。在本研究中,我们将姜黄素用作光动力疗法中的天然光敏剂,并将其包裹在由稳定四醚脂质组成的脂质体中,旨在构建一种针对肺癌的肺部给药系统。通过双离心法(一种创新的脂质体制备方法)制备了含有不同比例水解甘油二烷基甘油四醚(hGDGT)或水解甘油二烷基壬醇四醚(hGDNT)的脂质体。雾化前后脂质体的物理化学特性及其他雾化特性证实了它们的适用性。使用原子力显微镜和透射电子显微镜进行的形态学表征显示出脂质体典型的囊泡结构。可视化并证实了负载姜黄素的脂质体在肺腺癌(A549)细胞中的定性和定量摄取。检测到脂质体对A549细胞具有光毒性作用,细胞活力下降。证实了光动力疗法所需的活性氧的产生以及线粒体膜电位的破坏。此外,采用鸡胚绒毛尿囊膜(CAM)模型在三维细胞培养环境中进一步评估生物相容性和光动力疗效。将脂质体雾化到CAM上的异种移植肿瘤上并随后进行照射后,通过PET/CT评估光动力疗效。在二维和三维细胞培养中封装姜黄素的四醚脂质体的物理化学性质和疗效,尤其是含有hGDNT的脂质体,对于未来用于对抗肺癌的光动力疗法似乎很有前景。