体内
肺表面活性物质
荧光
原卟啉IX
化学
溶解度
增溶
体外
细胞毒性
光动力疗法
水溶液
荧光计
生物物理学
色谱法
生物化学
生物
有机化学
生物技术
物理
量子力学
作者
Lirong Ma,Xuanlin Yang,Xiuzhong Yao,Weiyu Weng
摘要
Abstract 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® 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 .
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