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Updated: Nov 7, 2025

Construction of Cyclic Cell-Penetrating Peptides for Enhanced Penetration of Biological Barriers
Published on: September 19, 2022
Progress in tumour-targeted drug delivery based on cell-penetrating peptides
Xinru Kong1, Jiangkang Xu1, Xiaoye Yang1
1Key Laboratory of Chemical Biology, Department of Pharmaceutics, School of Pharmaceutical Sciences, Ministry of Education, Shandong University, Jinan, China.
Abstract:
Since the discovery of cell-penetrating peptides (CPP) in the 1980s, they have played a unique role in various fields owing to their excellent and unique cell membrane penetration function. In particular, in the treatment of tumours, CPPS have been used to deliver several types of 'cargos' to cancer cells. To address the insufficient targeting ability, non-selectivity, and blood instability, activatable cell-penetrating peptides, which can achieve targeted drug delivery in tumour treatment, enhance curative effects, and reduce toxicity have been developed. This study reviews the application of different cell-penetrating peptides in tumour-targeted delivery, overcoming multidrug resistance, organelle targeting, tumour imaging, and diagnosis, and summarises the different mechanisms of activatable cell-penetrating peptides in detail.
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