siRNA Delivery: From Lipids to Cell‐penetrating Peptides and Their Mimics

Citations Over TimeTop 10% of 2012 papers

Abstract

To deliver siRNA for therapeutic use, several hurdles must be addressed. Metabolic degradation must be blocked, and the RNAi cellular machinery is located in the cytoplasm, while double-stranded siRNA is large, highly charged and impermeable to cell membranes. To date, the solutions to the delivery issues have mostly involved different forms of lipid particle encapsulation. Cell-penetrating peptides and their mimics or analogues offer a different approach and this is an emerging field with the first in vivo examples now reported. Recent reports point to lipid receptors being involved in the cellular uptake of both types of transporter. This review examines the delivery of siRNA with a focus on cell-penetrating peptides and their small molecule and oligomeric mimics. The current status of siRNA delivery methods in clinical trials is examined. It now seems that the goal of delivering siRNA therapeutically is achievable but will they form part of a sustainable healthcare portfolio for the future.

Related Papers

• → Visualizing a Correlation between siRNA Localization, Cellular Uptake, and RNAi in Living Cells(2004)378 cited
• → A Non-Covalent Peptide-Based Strategy for siRNA Delivery(2010)37 cited
• → Short Interfering RNA (siRNA)—Mediated RNA Interference (RNAi) in Human Cells(2003)82 cited
• → Can siRNA Technology Provide the Tools for Gene Therapy of the Future?(2006)34 cited
• → Abstract 2057: Dual peptide-mediated targeted delivery of siRNAs for the treatment of oral cancer(2016)