在vivo中通过positron发射断层扫描对[60]基于烯的分子球体核酸进行成像
Antti Äärelä1,2, Tatsiana Auchynnikava1,3, Olli Moisio3
1Department of Chemistry, University of Turku, FI-20500 Turku, Finland.
Molecular pharmaceutics
|August 2, 2023
概括
标有-18的富勒基分子球形核酸 (MSNA) 是为癌症成像开发的. 酸的骨干增强了稳定性,并显示出有希望的生物分布,用于有针对性的输送.
科学领域:
- 纳米医学是一种纳米医学.
- 分子成像学分子成像学
- 氧核酸治疗药物 治疗药物
背景情况:
- 人类表皮生长因子受体2 (HER2) 是癌症治疗的目标.
- 分子球状核酸 (MSNA) 提供了针对药物输送和成像的潜力.
- 开发稳定和可追溯的MSNA对于体内应用至关重要.
研究的目的:
- 为了合成和表征18F标记的MSNAs用于HER2阳性瘤成像.
- 评估具有不同脊柱的MSNAs的体内生物分布和稳定性.
- 评估MSNA在HER2表达瘤中的向输送潜力.
主要方法:
- 用基 (MSNA-PO) 和基酸 (MSNA-PS) 骨架合成18F标记的MSNA.
- 在HER2表达型HCC1954瘤携带小鼠体内PET/CT成像.
- 分析MSNA生物分布,稳定性和瘤与肌肉的比率.
主要成果:
- MSNA-PO显示出快速降解,而MSNA-PS显示出更好的酶稳定性.
- 在注射后一小时,MSNA-PS在脏,肝脏和血液中显示出显著的积累.
- 观察到平均瘤与肌肉的比率为2,MSNA-PS.的血液循环持续时间长.
结论:
- 酸的骨干增强了18F标记的MSNA在体内应用中的稳定性.
- MSNAs显示了针对 HER2 表达瘤的向传递和成像的潜力.
- 对MSNA流通时间的进一步研究可以优化目标交付策略.
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