Carboranes have emerged as one of the most promising boron agents in boron neutron capture therapy (BNCT). In this context, in vivo studies are particularly relevant, since they provide qualitative and quantitative information about the biodistribution of these molecules, which is of the utmost importance to determine the efficacy of BNCT, defining their localization and (bio)accumulation, as well as their pharmacokinetics and pharmacodynamics. First, we gathered a detailed list of the carboranes used for in vivo studies, considering the synthesis of carborane derivatives or the use of delivery system such as liposomes, micelles and nanoparticles. Then, the formulation employed and the cancer model used in each of these studies were identified. Finally, we examined the analytical aspects concerning carborane detection, identifying the main methodologies applied in the literature for ex vivo and in vivo analysis. The present work aims to identify the current strengths and weakness of the use of carboranes in BNCT, establishing the bottlenecks and the best strategies for future applications.
碳硼烷已成为硼中子俘获疗法中最具前景的硼剂之一。在此背景下,体内研究尤为重要,因为它们能提供关于这些分子生物分布的定性和定量信息,这对于确定BNCT疗效、明确其定位与(生物)累积特性以及药代动力学和药效学至关重要。首先,我们系统梳理了用于体内研究的碳硼烷清单,涵盖碳硼烷衍生物的合成及脂质体、胶束和纳米颗粒等递送系统的应用。随后,我们详细分析了各项研究中采用的制剂配方与癌症模型。最后,我们考察了碳硼烷检测相关的分析技术,明确了现有文献中离体与体内分析的主要方法学。本研究旨在系统评估碳硼烷在BNCT应用中的优势与局限,厘清当前技术瓶颈,并为未来应用确立最优策略。