期刊
ADVANCED DRUG DELIVERY REVIEWS
卷 65, 期 10, 页码 1299-1315出版社
ELSEVIER SCIENCE BV
DOI: 10.1016/j.addr.2012.11.007
关键词
Cell-penetrating peptide (CPP); Drug delivery system; Prodrug; Targeted delivery; In vivo
资金
- NSFC, China [91029743, 81172996]
- National Basic Research Program of China (973 Program) [2013CB932503]
- Shanghai Pu-jiang Scholar Program
- School of Pharmacy, Fudan University
- Key Lab of Smart Drug Delivery (Fudan University)
- MOE PLA, China [SDD2011-02]
- NIH [CA114612]
- World Class University (WCU) project of the MEST [R31-2008-000-10103-01]
- NRF of South Korea
Cell-penetrating peptide (CPP)-mediated intracellular drug delivery system, often specifically termed as the Trojan horse approach, has become the holy grail in achieving effective delivery of macromolecular compounds such as proteins, DNA, siRNAs, and drug carriers. It is characterized by the unique cell(or receptor-), temperature-, and payload-independent mechanisms, therefore offering potent means to improve poor cellular uptake of a variety of macromolecular drugs. Nevertheless, this Trojan horse approach also acts like a double-edged sword, causing serious safety and toxicity concerns to normal tissues or organs for in vivo application, due to lack of target selectivity of the powerful cell penetrating activity. To overcome this problem of potent yet non-selective penetration vs. targeting delivery, a number of smart strategies have been developed in recent years, including controllable CPP-based drug delivery systems based on various stimuli-responsive mechanisms. This review article provides a fundamental understanding of these smart systems, as well as a discussion of their real-time in vivo applicability. (C) 2013 Elsevier B.V. All rights reserved.
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