Nanophotosensitizers for Folate Receptor-Targeted and Redox-Sensitive Delivery of Chlorin E6 against Cancer Cells

Materials

Chang-Min Lee¹  Young-Il Jeong¹  Byung-Hoon Kim¹  Min-Suk Kook² 

[1] Department of Dental Materials, School of Dentistry, Chosun University, Gwangju 61452, Korea;Department of Oral and Maxillofacial Surgery, School of Dentistry, Chonnam National University, Gwangju 61186, Korea;

关键词: oral cancer;    photodynamic therapy;    chlorin e6;    nanophotosensitizers;   

DOI  :  10.3390/ma13122810

来源: DOAJ

【 摘 要 】

In this study, FA–PEG₃₅₀₀-ss-Ce6tri copolymer was synthesized to deliver photosensitizers via redox-sensitive and folate receptor-specific manner. Folic acid (FA) was attached to amine end of poly (ethylene glycol) (PEG₃₅₀₀) (FA–PEG₃₅₀₀ conjugates) and cystamine-conjugated chlorin e6 (Ce6) (Ce6-cystamine conjugates). FA–PEG₃₅₀₀ was further conjugated with Ce6-cystamine to produce FA–PEG₃₅₀₀-ss-Ce6 conjugates. To the remaining amine end group of Ce6-cystamine conjugates, Ce6 was attached to produce FA–PEG₃₅₀₀-ss-Ce6tri. Nanophotosensitizers of FA–PEG₃₅₀₀-ss-Ce6tri copolymer were smaller than 200 nm. Their shapes were disintegrated by treatment with GSH and then Ce6 released by GSH-dependent manner. Compared to Ce6 alone, FA–PEG₃₅₀₀-ss-Ce6tri copolymer nanophotosensitizers recorded higher Ce6 uptake ratio, reactive oxygen species (ROS) production and cellular cytotoxicity against KB and YD-38 cells. The in vitro and in vivo study approved that delivery of nanophotosensitizers is achieved by folate receptor-sensitive manner. These results indicated that FA–PEG₃₅₀₀-ss-Ce6tri copolymer nanophotosensitizers are superior candidate for treatment of oral cancer.

【 授权许可】

Unknown