A novel folic acid-conjugated TiO2–SiO2 photosensitizer for cancer targeting in photodynamic therapy

• Published in: Colloids and surfaces, B, Biointerfaces B, Biointerfaces, 2015-01, Vol.125, p.197-205
• Main Authors: Feng, Xiaohui, Zhang, Shaokun, Wu, Hong, Lou, Xia
• Format: Article
• Language: English
• Subjects: Animals; Biological Transport; Cancer; Cell Line; Fibroblasts; Fibroblasts - cytology; Fibroblasts - drug effects; Fibroblasts - radiation effects; Folic acid; Folic Acid - chemistry; Human; Humans; KB Cells; Mathematical analysis; Mice; Nanoparticles; Nanoparticles - chemistry; Nanoparticles - ultrastructure; Photochemotherapy; Photodynamic therapy; Photosensitizer, Photo-killing; Photosensitizing Agents - chemical synthesis; Photosensitizing Agents - pharmacology; Silicon Dioxide - chemistry; Targeting; Titanium - chemistry; Titanium dioxide; Titanium dioxide nanoparticles; Ultraviolet Rays
• ISSN: 0927-7765; 1873-4367
• DOI: 10.1016/j.colsurfb.2014.11.035

•A novel folic acid-conjugated TiO2–SiO2 nano-photosensitizer was synthesized for targeted photo-killing of cancer cells.•High photodynamic reactivity, improved cell internalization and cellular and blood compatibility were well demonstrated.•A strong photo-killing effect on the human nasopharyngeal epidermoid cancer (KB) cells was achieved. In this paper, a novel folic acid-conjugated silica-coated titanium dioxide (TiO2–SiO2) photosensitizer was synthesized and characterized using various analytical instruments. The photosensitizer was further assessed with regards to its photoreactivity, cellular and hemocompatibility, cell internalization, and phototoxicity. Conjugating folic acid with TiO2–SiO2 has shown a significantly improved compatibility of the nanoparticles with the mouse fibroblast cells (L929) at 24h. An improved compatibility with the human nasopharyngeal epidermoid cancer (KB) cells was also demonstrated, but to a slightly reduced degree. Enhanced cell internalization was well demonstrated in the TiO2–SiO2 folate nanoparticles. Upon exposure to UV light, TiO2–SiO2 folate nanoparticles maintained a high level photodynamic reactivity and yielded a 38–43% photo-killing of KB cells. The photo-killing effect increased with increasing dosage in the investigated concentration range of 50–100μgml−1.