Abstract
RNA interference (RNAi) is an evolutionary conserved highly specific gene-silencing mechanism initiated by small interfering RNA (siRNA) molecules. Fast-paced preclinical and clinical studies helped the siRNA technology become an efficient tool for undruggable targets in different diseases including genetic diseases, viral diseases and cancer. Despite great feature of siRNAs that can down-regulate any protein in the cells, the full potential and the success of the preclinical studies could not be translated into largely successful clinical outcomes. It has become clear that the possibility of overcoming the pitfalls for in vivo siRNA therapy fully depends on delivery systems. In this review, we start with the challenges and barriers for in vivo siRNA delivery. Then we briefly discuss the recent developments in siRNA modification technology. We specifically focused on siRNA lipidation and delivery approaches with special emphasis on the lipid based hybrid systems. Here we summarize the journey of lipid-based micelle-like nanoparticle systems that combine longevity in blood, effective cellular uptake and endosomal escape for successful siRNA delivery and discuss the multifunctional stimuli-sensitive systems based on lipids as the next generation smart systems.
Keywords: siRNA, lipid-based delivery, micelle-like nanoparticles, stimuli-sensitive carriers, multifunctional carriers, polyethyleneimine.
Current Pharmaceutical Biotechnology
Title:Lipid-based siRNA Delivery Systems: Challenges, Promises and Solutions Along the Long Journey
Volume: 17 Issue: 8
Author(s): Can Sarisozen, Giuseppina Salzano and Vladimir P. Torchilin
Affiliation:
Keywords: siRNA, lipid-based delivery, micelle-like nanoparticles, stimuli-sensitive carriers, multifunctional carriers, polyethyleneimine.
Abstract: RNA interference (RNAi) is an evolutionary conserved highly specific gene-silencing mechanism initiated by small interfering RNA (siRNA) molecules. Fast-paced preclinical and clinical studies helped the siRNA technology become an efficient tool for undruggable targets in different diseases including genetic diseases, viral diseases and cancer. Despite great feature of siRNAs that can down-regulate any protein in the cells, the full potential and the success of the preclinical studies could not be translated into largely successful clinical outcomes. It has become clear that the possibility of overcoming the pitfalls for in vivo siRNA therapy fully depends on delivery systems. In this review, we start with the challenges and barriers for in vivo siRNA delivery. Then we briefly discuss the recent developments in siRNA modification technology. We specifically focused on siRNA lipidation and delivery approaches with special emphasis on the lipid based hybrid systems. Here we summarize the journey of lipid-based micelle-like nanoparticle systems that combine longevity in blood, effective cellular uptake and endosomal escape for successful siRNA delivery and discuss the multifunctional stimuli-sensitive systems based on lipids as the next generation smart systems.
Export Options
About this article
Cite this article as:
Sarisozen Can, Salzano Giuseppina and P. Torchilin Vladimir, Lipid-based siRNA Delivery Systems: Challenges, Promises and Solutions Along the Long Journey, Current Pharmaceutical Biotechnology 2016; 17 (8) . https://dx.doi.org/10.2174/1389201017666160401145319
DOI https://dx.doi.org/10.2174/1389201017666160401145319 |
Print ISSN 1389-2010 |
Publisher Name Bentham Science Publisher |
Online ISSN 1873-4316 |
Call for Papers in Thematic Issues
Artificial Intelligence in Bioinformatics
Bioinformatics is an interdisciplinary field that analyzes and explores biological data. This field combines biology and information system. Artificial Intelligence (AI) has attracted great attention as it tries to replicate human intelligence. It has become common technology for analyzing and solving complex data and problems and encompasses sub-fields of machine ...read more
- Author Guidelines
- Graphical Abstracts
- Fabricating and Stating False Information
- Research Misconduct
- Post Publication Discussions and Corrections
- Publishing Ethics and Rectitude
- Increase Visibility of Your Article
- Archiving Policies
- Peer Review Workflow
- Order Your Article Before Print
- Promote Your Article
- Manuscript Transfer Facility
- Editorial Policies
- Allegations from Whistleblowers
Related Articles
-
The Role of ABC and SLC Transporters in the Pharmacokinetics of Dietary and Herbal Phytochemicals and their Interactions with Xenobiotics
Current Drug Metabolism Eupatilin Inhibits the Proliferation and Migration of Prostate Cancer Cells through Modulation of PTEN and NF-κB Signaling
Anti-Cancer Agents in Medicinal Chemistry Effect of MRJF4 on C6 Glioma Cells Proliferation and Migration
Central Nervous System Agents in Medicinal Chemistry Drug Design Studies of the Novel Antitumor Targets Carbonic Anhydrase IX and XII
Current Medicinal Chemistry Apoptosis Induction by Erucylphosphohomocholine via the 18 kDa Mitochondrial Translocator Protein: Implications for Cancer Treatment
Anti-Cancer Agents in Medicinal Chemistry Upregulation of Cytoskeleton Protein and Extracellular Matrix Protein Induced by Stromal-Derived Nitric Oxide Promotes Lung Cancer Invasion and Metastasis
Current Molecular Medicine Dual Induction of Mitochondrial Apoptosis and Senescence in Chronic Myelogenous Leukemia by Myrtucommulone A
Anti-Cancer Agents in Medicinal Chemistry Anti-Genes: siRNA, Ribozymes and Antisense
Current Pharmaceutical Biotechnology Bioactive Metabolites from Pathogenic and Endophytic Fungi of Forest Trees
Current Medicinal Chemistry Rac-1 as a New Therapeutic Target in Cerebro- and Cardio-Vascular Diseases
Current Drug Targets Clinical Trials with Oncolytic Measles Virus: Current Status and Future Prospects
Current Cancer Drug Targets Optimal Saturated Neuropilin-1 Expression in Normal Tissue Maximizes Tumor Exposure to Anti-Neuropilin-1 Monoclonal Antibody
Anti-Cancer Agents in Medicinal Chemistry Toxicity and Efficacy of Benzamide Riboside in Cancer Chemotherapy Models
Current Medicinal Chemistry Cytotoxic and Anticancer Activities of Isatin and Its Derivatives: A Comprehensive Review from 2000-2008
Anti-Cancer Agents in Medicinal Chemistry Natural Polyphenols in the Treatment of Alzheimer’s Disease
Current Drug Targets Biologically Active Peptides Interacting with the G Protein-Coupled Formylpeptide Receptors
Protein & Peptide Letters Application of Metabolomics in Drug Discovery, Development and Theranostics
Current Metabolomics MYC-Mediated Synthetic Lethality for Treating Tumors
Current Cancer Drug Targets Microarray Technologies for Intracellular Kinome Analysis
Current Medicinal Chemistry The Interactions of the 5-HT3 Receptor with Quipazine-Like Arylpiperazine Ligands. The Journey Track at the End of the First Decade of the Third Millennium
Current Topics in Medicinal Chemistry