Abstract
Background: RNA interference is a promising therapeutic tool for the treatment of a variety of diseases, with great potential for cancer therapy. Small interfering RNA (siRNA), however, presents several drawbacks that hamper its therapeutic application. Lipid nanoparticles, including liposomes, are delivery systems with great potential for siRNA delivery, protecting it from degradation, enhancing its cell uptake with the ability of controlled release. However, non-specific delivery and side effects could potentially limit the in vivo application. Therefore, targeting lipid nanoparticles to overexpressed receptors of cancer cells represents a strategy for better therapeutic outcome, with improved efficacy and reduced toxicity. For this purpose, lipid nanoparticles could be functionalized with several moieties that can be recognized by cancer cells more than by normal cells. These ligands include folate, transferrin, peptides, oligosaccharides, monoclonal antibodies and aptamers.
Methods: In this paper, we reviewed functionalization strategies and addressed the major in vitro and in vivo findings in the field of cancer treatment with siRNA.
Results: Many papers showed enhanced siRNA delivery by targeted liposomes, resulting in enhanced drug uptake and better cytotoxicity, with consequent better tumor growth control in xenograft studies.
Conclusion: siRNA delivery mediated by functionalized liposomes is promising, but clinical trials need to be conducted.
Keywords: siRNA, targeting, lipid nanoparticle, liposomes, cancer therapy, toxicity.
Current Pharmaceutical Design
Title:Targeted Liposomes for siRNA Delivery to Cancer
Volume: 24 Issue: 23
Author(s): Josimar O. Eloy, Raquel Petrilli, Giovanni Loureiro Raspantini and Robert J. Lee*
Affiliation:
- Division of Pharmaceutics and Pharmaceutical Chemistry, College of Pharmacy, The Ohio State University, Columbus, Ohio,United States
Keywords: siRNA, targeting, lipid nanoparticle, liposomes, cancer therapy, toxicity.
Abstract: Background: RNA interference is a promising therapeutic tool for the treatment of a variety of diseases, with great potential for cancer therapy. Small interfering RNA (siRNA), however, presents several drawbacks that hamper its therapeutic application. Lipid nanoparticles, including liposomes, are delivery systems with great potential for siRNA delivery, protecting it from degradation, enhancing its cell uptake with the ability of controlled release. However, non-specific delivery and side effects could potentially limit the in vivo application. Therefore, targeting lipid nanoparticles to overexpressed receptors of cancer cells represents a strategy for better therapeutic outcome, with improved efficacy and reduced toxicity. For this purpose, lipid nanoparticles could be functionalized with several moieties that can be recognized by cancer cells more than by normal cells. These ligands include folate, transferrin, peptides, oligosaccharides, monoclonal antibodies and aptamers.
Methods: In this paper, we reviewed functionalization strategies and addressed the major in vitro and in vivo findings in the field of cancer treatment with siRNA.
Results: Many papers showed enhanced siRNA delivery by targeted liposomes, resulting in enhanced drug uptake and better cytotoxicity, with consequent better tumor growth control in xenograft studies.
Conclusion: siRNA delivery mediated by functionalized liposomes is promising, but clinical trials need to be conducted.
Export Options
About this article
Cite this article as:
Eloy O. Josimar , Petrilli Raquel , Raspantini Loureiro Giovanni and Lee J. Robert *, Targeted Liposomes for siRNA Delivery to Cancer, Current Pharmaceutical Design 2018; 24 (23) . https://dx.doi.org/10.2174/1381612824666180807121935
DOI https://dx.doi.org/10.2174/1381612824666180807121935 |
Print ISSN 1381-6128 |
Publisher Name Bentham Science Publisher |
Online ISSN 1873-4286 |
Call for Papers in Thematic Issues
"Tuberculosis Prevention, Diagnosis and Drug Discovery"
The Nobel Prize-winning discoveries of Mycobacterium tuberculosis and streptomycin have enabled an appropriate diagnosis and an effective treatment of tuberculosis (TB). Since then, many newer diagnosis methods and drugs have been saving millions of lives. Despite advances in the past, TB is still a leading cause of infectious disease mortality ...read more
Current Pharmaceutical challenges in the treatment and diagnosis of neurological dysfunctions
Neurological dysfunctions (MND, ALS, MS, PD, AD, HD, ALS, Autism, OCD etc..) present significant challenges in both diagnosis and treatment, often necessitating innovative approaches and therapeutic interventions. This thematic issue aims to explore the current pharmaceutical landscape surrounding neurological disorders, shedding light on the challenges faced by researchers, clinicians, and ...read more
Emerging and re-emerging diseases
Faced with a possible endemic situation of COVID-19, the world has experienced two important phenomena, the emergence of new infectious diseases and/or the resurgence of previously eradicated infectious diseases. Furthermore, the geographic distribution of such diseases has also undergone changes. This context, in turn, may have a strong relationship with ...read more
Melanoma and Non-Melanoma Skin Cancer Treatment: Standard of Care and Recent Advances
In this thematic issue, we aim to provide a standard of care of the diagnosis and treatment of melanoma and non-melanoma skin cancer. The editor will invite authors from different countries who will write review articles of melanoma and non-melanoma skin cancers. The Diagnosis, Staging, Surgical Treatment, Non-Surgical Treatment all ...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
- Announcements
Related Articles
-
Patent Selections
Recent Patents on Biotechnology Editorial [Hot Topic: Cancer Genetics (Guest Editor: Anirban Maitra)]
Current Molecular Medicine Editorial (Thematic Issue: Immunophilins, Protein Chemistry and Cell Biology of a Promising New Class of Drug Targets – Part II)
Current Molecular Pharmacology Novel Monoclonal Antibodies for the Treatment of Chronic Lymphocytic Leukemia
Current Cancer Drug Targets Bridging the Gap Between Chemistry and Biotechnology - Large Molecules with Potential, How Could Biotechnology Complement Chemistry?
Current Organic Chemistry Characterization of Carbonic Anhydrase Isozyme Specific Inhibition by Sulfamated 2-Ethylestra Compounds
Letters in Drug Design & Discovery Pharmacodynamics and Pharmacokinetics of Antifungals for Treatment of Invasive Aspergillosis
Current Pharmaceutical Design Cinnamaldehyde-Induced Apoptosis in Human Hepatoma PLC/PRF/5 Cells Involves the Mitochondrial Death Pathway and is Sensitive to Inhibition by Cyclosporin A and z-VAD-fmk
Anti-Cancer Agents in Medicinal Chemistry Patent Selections:
Recent Patents on Biotechnology Silencing GPX3 Expression Promotes Tumor Metastasis in Human Thyroid Cancer
Current Protein & Peptide Science The AmpliChip: A Review of its Analytic and Clinical Validity and Clinical Utility
Current Drug Safety Macrocyclic Inhibitors of Hsp90
Current Topics in Medicinal Chemistry Clinical Trials Investigating Immune Checkpoint Inhibitors in Non-Small-Cell Lung Cancer
Reviews on Recent Clinical Trials Molecular Targeting of Breast Cancer: Molecular Imaging and Therapy
Current Pharmaceutical Biotechnology Vitamin D and the Adaptive Immune System with Special Emphasis to Allergic Reactions and Allograft Rejection
Inflammation & Allergy - Drug Targets (Discontinued) Editorial (Thematic Issue: Iron Chelation and Drug Resistance in Cancer and Tuberculosis)
Current Pharmaceutical Biotechnology Pharmaceutical and Biomedical Potential of PEGylated Dendrimers
Current Pharmaceutical Design Targeting Proteasomal Pathways by Dietary Curcumin for Cancer Prevention and Treatment
Current Medicinal Chemistry Cell Penetrating Peptides for In Vivo Molecular Imaging Applications
Current Pharmaceutical Design Targeting CCK Receptors in Human Cancers
Current Topics in Medicinal Chemistry