文献类型：期刊文献

英文题名：Solubilization of Hexyl Aminolevulinate by Surfactants for Tumor Fluorescence Detection

作者：Ma, Lirong[1];Yang, Xuanlin[1];Yao, Xiuzhong[2];Weng, Weiyu[1,3]

机构：[1]East China Univ Sci & Technol, Sch Pharm, Minist Educ, Engn Res Ctr Pharmaceut Proc Chem, Shanghai, Peoples R China;[2]Fudan Univ, Zhongshan Hosp, Dept Radiol, Shanghai, Peoples R China;[3]East China Univ Sci & Technol, Shanghai Key Lab New Drug Design, Shanghai, Peoples R China

年份：2020

卷号：96

期号：5

起止页码：1088

外文期刊名：PHOTOCHEMISTRY AND PHOTOBIOLOGY

收录：;WOS:【SCI-EXPANDED(收录号:WOS:000528938100001)】；

基金：This work was supported by the Shanghai Natural Science Foundation (16ZR1405900).

语种：英文

摘要：Hexyl aminolevulinate (HAL) is a lipophilic derivative of 5-aminolevulinic acid (5-ALA) and can induce more protoporphyrin IX (PpIX) formation and stronger fluorescence intensity (FI) than 5-ALA, which will greatly facilitate photodynamic diagnosis and therapy. The main drawback of HAL is its low solubility in neutral aqueous media. In this study, surfactants were used to increase HAL solubility in the cell culture medium and serum, followed by in vitro fluorescence formation measurement in human pancreatic cancer cells (SW1990) and in vivo fluorescence detection in tumor-bearing mice. The results showed that Tween 80 (TW80) and Kolliphor (R) HS 15 (HS15) increased the solubility of HAL in the selected media. Although TW80 and HS15 exhibited in vitro cytotoxicity at high concentrations (5 mg mL(-1)), they facilitated fluorescent signal formation at the early stage of cell incubation. When surfactants were used, the FI should be determined without the routine washing process because surfactant-containing culture medium caused the loss of synthesized PpIX during the washing process. When HAL dissolved in TW80 solution was injected intraperitoneally into pancreatic cancer-bearing mice at a dose of 50 mg kg(-1), the tumors exhibited red fluorescence, which indicated that systemic administration of surfactant-solubilized HAL might be applicable for tumor fluorescence detection in vivo.