Journal
EUROPEAN JOURNAL OF PHARMACEUTICS AND BIOPHARMACEUTICS
Volume 85, Issue 1, Pages 5-11Publisher
ELSEVIER SCIENCE BV
DOI: 10.1016/j.ejpb.2013.03.021
Keywords
Oligonucleotide; siRNA; Cell-penetrating peptide; Endocytosis; Delivery
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Funding
- Gebert Ruf Foundation [GRS-041/11]
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Cell-penetrating peptides have been widely investigated as delivery vehicles for oligonucleotides (e.g., siRNA and antisense oligonucleotides). Different delivery strategies can be used, such as co-incubation, direct conjugation, non-covalent complex, and modification on the surface of liposome or polymer complexes. However, several challenges remain for their preclinical and clinical development. Endosomal escape, lack of cell/tissue specificity, and toxicity are major concerns in the design of cell-penetrating peptide-mediated delivery systems. In this commentary, we highlight recent reports of cell-penetrating peptide incorporation into oligonucleotide delivery systems and underline the remaining challenges, particularly for preclinical and clinical applications. (c) 2013 Elsevier B.V. All rights reserved.
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