ArticleAAPS PharmSciTech2014
Development and characterization of siRNA lipoplexes: Effect of different lipids, in vitro evaluation in cancerous cell lines and in vivo toxicity study.
Article in AAPS PharmSciTech, 2014. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 21 papers.
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Who cites it
21 citing papers in PubMed, 61 citations in OpenAlex.
- Cationic lipid-based nanoparticles for therapeutic delivery in cancer treatment: physicochemical characteristics, therapeutic cargos, and clinical potential.Applied microscopy · 2026Review
- Preclinical testing of antiviral siRNA therapeutics delivered in lipid nanoparticles in animal models - a comprehensive review.Drug delivery and translational research · 2025Review
- Multi-Step Assembly of an RNA-Liposome Nanoparticle Formulation Revealed by Real-Time, Single-Particle Quantitative Imaging.Advanced science (Weinheim, Baden-Wurttemberg, Germany) · 2025Article
- Lipoplexes' Structure, Preparation, and Role in Managing Different Diseases.AAPS PharmSciTech · 2024Review
- Plasmid DNA ionisable lipid nanoparticles as non-inert carriers and potent immune activators for cancer immunotherapy.Journal of controlled release : official journal of the Controlled Release Society · 2024Article
- Oligonucleotide-Based Therapeutics for STAT3 Targeting in Cancer-Drug Carriers Matter.Cancers · 2023Review
- Targeting the RNA-Binding Protein HuR in Cancer.Cancer research · 2023Review
- Liposome-polyethylenimine complexes for the effective delivery of HuR siRNA in the treatment of diabetic retinopathy.Drug delivery and translational research · 2023Article
- The role of lipid components in lipid nanoparticles for vaccines and gene therapy.Advanced drug delivery reviews · 2022Review
- Recent advances in mRNA-LNP therapeutics: immunological and pharmacological aspects.Journal of nanobiotechnology · 2022Review
- Anti-Biomedicines · 2020Review
- Plasma polymerized nanoparticles effectively deliver dual siRNA and drug therapy in vivo.Scientific reports · 2020Article
- Targeted Delivery of siRNA Lipoplexes to Cancer Cells Using Macrophage Transient Horizontal Gene Transfer.Advanced science (Weinheim, Baden-Wurttemberg, Germany) · 2019Article
- Preparation and Evaluation of A Novel Liposomal Nano-Formulation in Metastatic Cancer Treatment Studies.Cell journal · 2019Article
- Luminescent/magnetic PLGA-based hybrid nanocomposites: a smart nanocarrier system for targeted codelivery and dual-modality imaging in cancer theranostics.International journal of nanomedicine · 2017Article
- Achieving long-term stability of lipid nanoparticles: examining the effect of pH, temperature, and lyophilization.International journal of nanomedicine · 2017Article
- Cellular Delivery of RNA Nanoparticles.ACS combinatorial science · 2016Review
- Lipid Nanovectors to Deliver RNA Oligonucleotides in Cancer.Nanomaterials (Basel, Switzerland) · 2016Review
- Bolaamphiphiles as carriers for siRNA delivery: From chemical syntheses to practical applications.Journal of controlled release : official journal of the Controlled Release Society · 2015Article
- Translational application of nano delivery systems: emerging cancer therapy.AAPS PharmSciTech · 2015Article
Corrections and comments
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Authors and funding
5 authors at 1 institution in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Cationic liposomes have long been used as non-viral vectors for small interfering RNA (siRNA) delivery but are associated with high toxicity, less transfection efficiency, and in vivo instability. In this investigation, we have developed siRNA targeted to RRM1 that is responsible for development of resistance to gemcitabine in cancer cells. Effect of different lipid compositions has been evaluated on formation of stable and less toxic lipoplexes. Optimized cationic lipoplex (D2CH) system was comprised of dioleoyl-trimethylammoniumpropane (DOTAP), dioleoyl-sn-glycero-3-phosphoethanolamine (DOPE), hydrogenated soya phosphocholine (HSPC), cholesterol, and methoxy(polyethyleneglycol)2000-1,2-distearoyl-sn-glycero-3-phosphoethanolamine (mPEG2000-DSPE). D2CH lipoplexes have shown particle size (147.5 ± 2.89 nm) and zeta potential (12.26 ± 0.54 mV) characteristics essential for their in vivo use. In vitro cytotoxicity study has shown low toxicity of developed lipoplexes as compared with lipofectamine-2000 up to N/P ratio as high as 7.5. Cell uptake studies and gene expression studies have confirmed intracellular availability of siRNA. In addition, developed lipoplexes also showed ~3 times less hemolytic potential as compared with DOTAP/DOPE lipoplexes at lipid concentration of 5 mg/mL. Lipoplexes also maintained particle size less than 200 nm on exposure to high electrolyte concentration and showed >70% siRNA retention in presence of serum showing siRNA protection conferred by lipoplexes. Furthermore, in vivo acute toxicity studies in mice showed that formulation was non-toxic up to a dosage of 0.75 mg of siRNA/kg as lipoplexes and 300 mg lipid/kg as blank liposomes indicating tolerability of lipoplexes at a dose much higher than required for therapeutic use. Promising results of this study warrant further investigation of developed siRNA lipoplexes for cancer treatment.
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Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.