Micro/Nanomotors Actively Penetrate Physiological Barriers: Basic Nanoarchitectonics to Practical Application

Abstract Micro/nano technology offers advantages such as higher adsorption efficiency and lower toxicity in drug delivery; however, passive systems that depend on passive distribution face challenges in penetrating physiological barriers. In contrast, micro/nanomotors (MNMs) with self‐propulsion capabilities powered by energy sources like chemical reactions and physical fields show great potential for enhancing barrier penetration. Their active motion facilitates stronger tissue interaction and improves efficiency in crossing strict physiological barriers designed to protect vital areas but hinder drug delivery under abnormal conditions. This manuscript provides a critical introduction to MNMs‐based drug delivery systems, reviews recent advances in overcoming physiological barriers and targeted drug delivery, and summarizes the challenges and future research priorities, aiming to offer guidelines for further development. With continuous innovation, MNMs represent a promising strategy to enhance targeted drug delivery efficiency across physiological barriers.