4.5 Review

Progress in tumour-targeted drug delivery based on cell-penetrating peptides

Journal

JOURNAL OF DRUG TARGETING
Volume 30, Issue 1, Pages 46-60

Publisher

TAYLOR & FRANCIS LTD
DOI: 10.1080/1061186X.2021.1920026

Keywords

Cell-penetrating peptides; cancer therapy; activatable cell-penetrating peptides; targeted drug delivery; cell membrane

Funding

  1. National Science and Technology Major Special Project-Major New Drug Creation [2019ZX09301-112]
  2. Shandong Provincial Major Science &Technology Innovation Project, P. R. China [2018CXGC1411]
  3. Shandong Provincial Program of Taishan Industrial Experts

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Cell-penetrating peptides have shown unique applications in tumor treatment, delivering drugs with enhanced efficacy and reduced toxicity through targeted delivery.
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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