---
title: "Cell-penetrating peptides for tumor drug delivery: classifications, mechanisms, and nanoplatform s"
id: "pubmed-42920212"
canonical_url: "https://medichelpline.com/clinical-feed/pubmed-42920212"
content_type: "clinical_feed_article"
specialty: "Pharmacology"
source_name: "PubMed / NCBI"
source_url: "https://pubmed.ncbi.nlm.nih.gov/42920212/"
doi: "10.13345/j.cjb.260296"
published_at: "2026-10-25T00:00:00.000Z"
evidence_level: "Journal Article"
license: "CC-BY-NC-4.0 / Informational Use"
---
# Cell-penetrating peptides for tumor drug delivery: classifications, mechanisms, and nanoplatform s
## Provenance & Clinical Metadata
- **Canonical URL:** https://medichelpline.com/clinical-feed/pubmed-42920212
- **Specialty:** [Pharmacology](https://medichelpline.com/clinical-feed/pharmacology.md)
- **Primary Source:** PubMed / NCBI
- **Source URL:** [Original Journal Publication](https://pubmed.ncbi.nlm.nih.gov/42920212/)
- **DOI:** [10.13345/j.cjb.260296](https://doi.org/10.13345%2Fj.cjb.260296)
- **Published At:** 2026-10-25T00:00:00.000Z
- **Evidence Rating:** Journal Article
## Executive GIST (TL;DR)
- The review examined **cell-penetrating peptides (CPPs)** as short peptides that efficiently cross biological membranes and serve as carriers for **tumor**-targeted drug delivery. - Authors grouped CPPs by charge and hydrophobicity into cationic, amphipathic, and hydrophobic classes, noting charge governs interaction with cell membranes. - The manuscript described two principal cellular entry routes: direct membrane penetration and endocytic uptake; molecular details and pathway distinctions were summarized by the study team. - Investigators surveyed combinations of CPPs with diverse delivery platforms, reporting development of multifunctional nanoplatforms that pair CPPs with carriers to improve intracellular delivery of antineoplastic agents. - Data indicated CPP modification enables cargo internalization via membrane translocation or endocytosis, but the abstract did not report quantitative efficacy measures, dosing, or specific clinical trial outcomes. - The review provided an overview of recent advances and suggested directions for CPP-based antitumor delivery, while not reporting translational or regulatory status of individual CPP constructs. - Keywords listed by the authors included cell-penetrating peptide, delivery system, targeted delivery, transcytosis, and tumor therapy. - The paper is a review article and includes an English abstract and 84 references supporting classifications, mechanisms, and nanoplatform applications.
## Clinical Analysis & Structured Key Points
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Affiliations Expand ### Affiliations * 1 Qinghai Key Laboratory of Phytochemistry in the Qinghai-Xizang Plateau, Qinghai Engineering Research Center of Modern Tibetan Medicine Development, College of Pharmacy, Qinghai Minzu University, Xining 810007, Qinghai, China. * 2 Beijing Key Laboratory of Drug Delivery Technology and Novel Formulation, Institute of Materia Medica, Chinese Academy of Medical Sciences & Peking Union Medical College, Beijing 100050, China. * 3 Qinghai Key Laboratory of Phytochemistry in the Qinghai-Xizang Plateau, Qinghai Engineering Research Center of Modern Tibetan Medicine Development, College of Pharmacy, Qinghai Minzu University, Xining 810007, Qinghai, China. yuhuama612@163.com. * 4 State Key Laboratory of Bioactive Substances and Functions of Natural Medicines, Institute of Materia Medica, Chinese Academy of Medical Sciences & Peking Union Medical College, Beijing 100050, China. fanwufa@imm.ac.cn. * 5 Beijing Key Laboratory of Drug Delivery Technology and Novel Formulation, Institute of Materia Medica, Chinese Academy of Medical Sciences & Peking Union Medical College, Beijing 100050, China. fanwufa@imm.ac.cn. * PMID: **42920212** * DOI: [ 10.13345/j.cjb.260296 ](https://doi.org/10.13345/j.cjb.260296) Item in Clipboard Review # [Application of cell-penetrating peptides in tumor therapy] [Article in Chinese] Xin Xin et al. Sheng Wu Gong Cheng Xue Bao. 2026. Show details Display options Display options Format Abstract PubMed PMID Sheng Wu Gong Cheng Xue Bao Actions * [ Search in PubMed ](https://pubmed.ncbi.nlm.nih.gov/?term=%22Sheng+Wu+Gong+Cheng+Xue+Bao%22%5Bjour%5D&sort=date&sort_order=desc) * [ Search in NLM Catalog ](https://www.ncbi.nlm.nih.gov/nlmcatalog?term=%22Sheng+Wu+Gong+Cheng+Xue+Bao%22%5BTitle+Abbreviation%5D) * [ Add to Search ](https://pubmed.ncbi.nlm.nih.gov/42920212/) . 2026 Oct 25;42(10):4355-4370. doi: 10.13345/j.cjb.260296. ### Authors [Xin Xin](https://pubmed.ncbi.nlm.nih.gov/?term=Xin+X&cauthor_id=42920212)[ 1 ](https://pubmed.ncbi.nlm.nih.gov/42920212/#short-view-affiliation-1 "Qinghai Key Laboratory of Phytochemistry in the Qinghai-Xizang Plateau, Qinghai Engineering Research Center of Modern Tibetan Medicine Development, College of Pharmacy, Qinghai Minzu University, Xining 810007, Qinghai, China.")[ 2 ](https://pubmed.ncbi.nlm.nih.gov/42920212/#short-view-affiliation-2 "Beijing Key Laboratory of Drug Delivery Technology and Novel Formulation, Institute of Materia Medica, Chinese Academy of Medical Sciences & Peking Union Medical College, Beijing 100050, China."), [Jinfeng Zhang](https://pubmed.ncbi.nlm.nih.gov/?term=Zhang+J&cauthor_id=42920212)[ 1 ](https://pubmed.ncbi.nlm.nih.gov/42920212/#short-view-affiliation-1 "Qinghai Key Laboratory of Phytochemistry in the Qinghai-Xizang Plateau, Qinghai Engineering Research Center of Modern Tibetan Medicine Development, College of Pharmacy, Qinghai Minzu University, Xining 810007, Qinghai, China.")[ 2 ](https://pubmed.ncbi.nlm.nih.gov/42920212/#short-view-affiliation-2 "Beijing Key Laboratory of Drug Delivery Technology and Novel Formulation, Institute of Materia Medica, Chinese Academy of Medical Sciences & Peking Union Medical College, Beijing 100050, China."), [Yuhua Ma](https://pubmed.ncbi.nlm.nih.gov/?term=Ma+Y&cauthor_id=42920212)[ 3 ](https://pubmed.ncbi.nlm.nih.gov/42920212/#short-view-affiliation-3 "Qinghai Key Laboratory of Phytochemistry in the Qinghai-Xizang Plateau, Qinghai Engineering Research Center of Modern Tibetan Medicine Development, College of Pharmacy, Qinghai Minzu University, Xining 810007, Qinghai, China. yuhuama612@163.com."), [Wufa Fan](https://pubmed.ncbi.nlm.nih.gov/?term=Fan+W&cauthor_id=42920212)[ 4 ](https://pubmed.ncbi.nlm.nih.gov/42920212/#short-view-affiliation-4 "State Key Laboratory of Bioactive Substances and Functions of Natural Medicines, Institute of Materia Medica, Chinese Academy of Medical Sciences & Peking Union Medical College, Beijing 100050, China. fanwufa@imm.ac.cn.")[ 5 ](https://pubmed.ncbi.nlm.nih.gov/42920212/#short-view-affiliation-5 "Beijing Key Laboratory of Drug Delivery Technology and Novel Formulation, Institute of Materia Medica, Chinese Academy of Medical Sciences & Peking Union Medical College, Beijing 100050, China. fanwufa@imm.ac.cn.") ### Affiliations * 1 Qinghai Key Laboratory of Phytochemistry in the Qinghai-Xizang Plateau, Qinghai Engineering Research Center of Modern Tibetan Medicine Development, College of Pharmacy, Qinghai Minzu University, Xining 810007, Qinghai, China. * 2 Beijing Key Laboratory of Drug Delivery Technology and Novel Formulation, Institute of Materia Medica, Chinese Academy of Medical Sciences & Peking Union Medical College, Beijing 100050, China. * 3 Qinghai Key Laboratory of Phytochemistry in the Qinghai-Xizang Plateau, Qinghai Engineering Research Center of Modern Tibetan Medicine Development, College of Pharmacy, Qinghai Minzu University, Xining 810007, Qinghai, China. yuhuama612@163.com. * 4 State Key Laboratory of Bioactive Substances and Functions of Natural Medicines, Institute of Materia Medica, Chinese Academy of Medical Sciences & Peking Union Medical College, Beijing 100050, China. fanwufa@imm.ac.cn. * 5 Beijing Key Laboratory of Drug Delivery Technology and Novel Formulation, Institute of Materia Medica, Chinese Academy of Medical Sciences & Peking Union Medical College, Beijing 100050, China. fanwufa@imm.ac.cn. * PMID: **42920212** * DOI: [ 10.13345/j.cjb.260296 ](https://doi.org/10.13345/j.cjb.260296) Item in Clipboard Cite Display options Display options Format Abstract PubMed PMID Linked Discoveries ## Abstract in [ English, ](https://pubmed.ncbi.nlm.nih.gov/42920212/#eng-abstract) [ Chinese ](https://pubmed.ncbi.nlm.nih.gov/42920212/#zho-abstract) Cell-penetrating peptides (CPPs) represent a class of short peptides capable of efficiently traversing biological membrane barriers, demonstrating substantial potential in tumor-targeted drug delivery. Drugs modified with CPPs can enter cells through direct membrane penetration or endocytic pathways, and CPPs have been extensively investigated in various antitumor drug delivery systems. This review initially categorizes CPPs into cationic peptides, amphipathic peptides, and hydrophobic peptides according to their charge characteristics, and subsequently elucidates the molecular mechanisms underlying CPP-mediated cellular entry. Furthermore, we comprehensively summarize the latest advances in multifunctional nanoplatforms constructed through the integration of CPPs with diverse delivery systems, thereby providing insights for the development of CPP-based antitumor delivery strategies. 细胞穿膜肽(cell-penetrating peptides, CPPs)是一类能够高效穿透生物膜屏障的短肽，在肿瘤靶向药物递送领域展现出巨大潜力。经CPPs修饰的药物可通过直接穿透或内吞方式进入细胞，并且已在多种抗肿瘤药物递送研究中得到应用。本文首先依据电荷特性将CPPs分为阳离子型肽、两亲性肽、疏水性肽，并剖析了CPPs进入细胞的分子机制。同时，详细综述了CPPs与不同递送系统结合所构建的多功能纳米平台及其最新应用进展，为CPPs抗肿瘤递送系统的研究提供了思路。. **Keywords:** cell-penetrating peptide; delivery system; targeted delivery; transcytosis; tumor therapy. [PubMed Disclaimer](https://pubmed.ncbi.nlm.nih.gov/disclaimer/) ## Conflict of interest statement 作者声明没有任何可能会影响本文所报告工作的已知经济利益或个人关系。 ## References 1. 1. BRAY F, LAVERSANNE M, SUNG H, FERLAY J, SIEGEL RL, SOERJOMATARAM I, JEMAL A. Global cancer statistics 2022:GLOBOCAN estimates of incidence and mortality worldwide for 36 cancers in 185 countries[J]. CA:A Cancer Journal for Clinicians, 2024, 74(3):229-263. 2. 1. GHEMRAWI R, ABUAMER L, KREMESH S, HUSSIEN G, AHMED R, MOUSA W, KHODER G, KHAIR M. Revolutionizing cancer treatment:recent advances in immunotherapy[J]. Biomedicines, 2024, 12(9):2158. 3. 1. GUIDOTTI G, BRAMBILLA L, ROSSI D. Cell-penetrating peptides:from basic research to clinics[J]. Trends in Pharmacological Sciences, 2017, 38(4):406-424. 4. 1. SILVA S, ALMEIDA A, VALE N. Combination of cell-penetrating peptides with nanoparticles for therapeutic application:a review[J]. Biomolecules, 2019, 9(1):22. 5. 1. FUTAKI S, SUZUKI T, OHASHI W, YAGAMI T, TANAKA S, UEDA K, SUGIURA Y. Arginine-rich peptides. An abundant source of membrane-permeable peptides having potential as carriers for intracellular protein delivery[J]. The Journal of Biological Chemistry, 276(8):5836-5840. Show all 84 references ## Publication types * Review Actions * [ Search in PubMed ](https://pubmed.ncbi.nlm.nih.gov/?term=%22Review%22%5Bpt%5D&sort=date&sort_order=desc) * [ Search in MeSH ](https://www.ncbi.nlm.nih.gov/mesh?term=Review) * [ Add to Search ](https://pubmed.ncbi.nlm.nih.gov/42920212/) * English Abstract Actions * [ Search in PubMed ](https://pubmed.ncbi.nlm.nih.gov/?term=%22English+Abstract%22%5Bpt%5D&sort=date&sort_order=desc) * [ Search in MeSH ](https://www.ncbi.nlm.nih.gov/mesh?term=English+Abstract) * [ Add to Search ](https://pubmed.ncbi.nlm.nih.gov/42920212/) ## MeSH terms * Animals Actions * [ Search in PubMed ](https://pubmed.ncbi.nlm.nih.gov/?term=%22Animals%22%5BMeSH%5D&sort=date&sort_order=desc) * [ Search in MeSH ](https://www.ncbi.nlm.nih.gov/mesh?term=Animals) * [ Add to Search ](https://pubmed.ncbi.nlm.nih.gov/42920212/) * Antineoplastic Agents* / administration & dosage Actions * [ Search in PubMed ](https://pubmed.ncbi.nlm.nih.gov/?term=%22Antineoplastic+Agents%2Fadministration+and+dosage%22%5BMAJR%5D&sort=date&sort_order=desc) * [ Search in MeSH ](https://www.ncbi.nlm.nih.gov/mesh?term=Antineoplastic+Agents) * [ Add to Search ](https://pubmed.ncbi.nlm.nih.gov/42920212/) * Cell-Penetrating Peptides* / chemistry Actions * [ Search in PubMed ](https://pubmed.ncbi.nlm.nih.gov/?term=%22Cell-Penetrating+Peptides%2Fchemistry%22%5BMAJR%5D&sort=date&sort_order=desc) * [ Search in MeSH ](https://www.ncbi.nlm.nih.gov/mesh?term=Cell-Penetrating+Peptides) * [ Add to Search ](https://pubmed.ncbi.nlm.nih.gov/42920212/) * Drug Delivery Systems* / methods Actions * [ Search in PubMed ](https://pubmed.ncbi.nlm.nih.gov/?term=%22Drug+Delivery+Systems%2Fmethods%22%5BMAJR%5D&sort=date&sort_order=desc) * [ Search in MeSH ](https://www.ncbi.nlm.nih.gov/mesh?term=Drug+Delivery+Systems) * [ Add to Search ](https://pubmed.ncbi.nlm.nih.gov/42920212/) * Humans Actions * [ Search in PubMed ](https://pubmed.ncbi.nlm.nih.gov/?term=%22Humans%22%5BMeSH%5D&sort=date&sort_order=desc) * [ Search in MeSH ](https://www.ncbi.nlm.nih.gov/mesh?term=Humans) * [ Add to Search ](https://pubmed.ncbi.nlm.nih.gov/42920212/) * Neoplasms* / drug therapy Actions * [ Search in PubMed ](https://pubmed.ncbi.nlm.nih.gov/?term=%22Neoplasms%2Fdrug+therapy%22%5BMAJR%5D&sort=date&sort_order=desc) * [ Search in MeSH ](https://www.ncbi.nlm.nih.gov/mesh?term=Neoplasms) * [ Add to Search ](https://pubmed.ncbi.nlm.nih.gov/42920212/) ## Substances * Cell-Penetrating Peptides Actions * [ Search in PubMed ](https://pubmed.ncbi.nlm.nih.gov/?term=%22Cell-Penetrating+Peptides%22%5Bnm%5D&sort=date&sort_order=desc) * [ Search in MeSH ](https://www.ncbi.nlm.nih.gov/mesh?term=%22Cell-Penetrating+Peptides%22) * [ Add to Search ](https://pubmed.ncbi.nlm.nih.gov/42920212/) * Antineoplastic Agents Actions * [
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