In this two-part review we present an up-to-date description of different imaging methods available to map the localization of drugs on skin as a complement of established ex-vivo absorption studies. This first part deals with invasive methods which are grouped in two classes according to their underlying principles: i) methods using radioactivity such as autoradiography and ii) mass spectrometry methods such as MALDI and SIMS. For each method, a description of the principle is given along with example applications of imaging and quantifying drug delivery in human skin. Thanks to these techniques a better assessment of the fate of drugs is obtained: its localization on a particular skin structure, its potential accumulation, etc. A critical comparison in terms of capabilities, sensitivity and practical applicability is included that will help the reader to select the most appropriate technique depending on the particular problem to be solved.

在这篇由两部分组成的综述中，我们提供了可用于绘制药物在皮肤上的定位的不同成像方法的最新描述，作为已建立的离体吸收研究的补充。第一部分涉及侵入性方法，根据其基本原理分为两类：i) 使用放射性的方法，如放射自显影和 ii) 质谱方法，如 MALDI 和 SIMS。对于每种方法，都给出了原理描述以及在人体皮肤中成像和量化药物递送的示例应用。由于这些技术，可以获得对药物命运的更好评估：它在特定皮肤结构上的定位、其潜在的积累等。 包括在能力、灵敏度和实际适用性方面的关键比较，这将帮助读者根据要解决的特定问题选择最合适的技术。