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Total 3220 results found since Jan 2013.

Current Development of siRNA Bioconjugates: From Research to the Clinic
In this study, it was shown that the main factor determining the nature of the biodistribution of conjugates is their lipophilicity. Conjugates of siRNA with lower lipophilicity; i.e., derivatives of retinoic acid, lithocholic acid, and docosahexanoic acid with greater efficiency than cholesterol conjugates accumulated in the kidneys, bladder, and lungs of the mouse after subcutaneous injection (Biscans et al., 2018). This fact is consistent with previous data that showed that more lipophilic conjugates bind more efficiently to serum components, and thus are not excreted by the kidneys (Wolfrum et al., 2007; Osborn et al.,...
Source: Frontiers in Pharmacology - April 25, 2019 Category: Drugs & Pharmacology Source Type: research

Functionalized selenium nanoparticles for targeted siRNA delivery silence Derlin1 and promote antitumor efficacy against cervical cancer.
In this study, biocompatible selenium nanoparticles (SeNPs) were loaded with RGDfC peptide to fabricate tumor-targeting gene delivery vehicle RGDfC-SeNPs. Subsequently, RGDfC-SeNPs were loaded with Derlin1-siRNA to fabricate RGDfC-Se@siRNA, which are functionalized selenium nanoparticles. RGDfC-Se@siRNA showed greater uptake in HeLa cervical cancer cells in comparison with that in human umbilical vein endothelial cells (HUVECs), verifying the RGDfC-mediated specific uptake of RGDfC-Se@siRNA. RGDfC-Se@siRNA was capable of entering HeLa cells via clathrin-associated endocytosis, and showed faster siRNA release in a cancer ce...
Source: Drug Delivery - December 14, 2019 Category: Drugs & Pharmacology Tags: Drug Deliv Source Type: research

Design of a Novel PEGylated Liposomal Vector for Systemic Delivery of siRNA to Solid Tumors.
Abstract A small interfering RNA (siRNA) delivery system using dioleylphosphate-diethylenetriamine conjugate (DOP-DETA)-based liposomes (DL) was assessed for systemic delivery of siRNA to tumors. DL carrying siRNA capable of inducing efficient gene silencing with low doses of siRNA were modified with polyethylene glycol (PEG-DL/siRNA) for systemic injection of siRNA. The biodistribution of DL and siRNA in the PEG-DL/siRNA was studied by using radiolabeled DL and fluorescence-labeled siRNA, respectively. DL in the PEG-DL/siRNA showed a high retention in the plasma, accumulation in the tumor, and low accumulation in...
Source: Biological and Pharmaceutical Bulletin - June 4, 2019 Category: Drugs & Pharmacology Authors: Song F, Sakurai N, Okamoto A, Koide H, Oku N, Dewa T, Asai T Tags: Biol Pharm Bull Source Type: research

One-step scalable preparation method for non-cationic liposomes with high siRNA content
Publication date: 25 July 2015 Source:International Journal of Pharmaceutics, Volume 490, Issues 1–2 Author(s): Masaharu Somiya , Kotomi Yamaguchi , Qiushi Liu , Tomoaki Niimi , Andrés Daniel Maturana , Masumi Iijima , Nobuo Yoshimoto , Shun’ichi Kuroda Cationic liposomes (LPs) have been utilized for short interfering RNA (siRNA) delivery in vitro and in vivo owing to their high affinity for siRNA via electrostatic binding. However, both cytotoxicity and non-specific adsorption of cationic LPs in the body have prevented clinical siRNA applications. These situations have led to siRNA encapsulation in non-cationic LPs...
Source: International Journal of Pharmaceutics - June 8, 2015 Category: Drugs & Pharmacology Source Type: research

Inhalation Properties and Stability of Nebulized Naked siRNA Solution for Pulmonary Therapy.
Abstract The use of naked unmodified small interfering RNA (N-siRNA) without vector has previously been investigated as a pulmonary therapy. However, little is known regarding stabilities and aerodynamic particle sizes of N-siRNA-containing droplets; nebulizers have not yet been optimized for N-siRNA solutions. Thus, in this study, we investigated the feasibility of inhaled N-siRNA solutions for pulmonary therapy using nebulization. Various nebulizers and N-siRNA concentrations were assessed in terms of siRNA integrity after nebulization, and inhalation properties including aerodynamic particle size were examined....
Source: Chemical and Pharmaceutical Bulletin - January 13, 2016 Category: Drugs & Pharmacology Authors: Tahara K, Hashimoto W, Takeuchi H Tags: Chem Pharm Bull (Tokyo) Source Type: research

Dual stimulus of hyperthermia and intracellular redox environment triggered release of siRNA for tumor-specific therapy
This study demonstrates that the constructed vesicle in combination with hyperthermia could greatly improve the in vivo stability of siRNA-CPPs and synergistically enhance its cancer therapy efficiency. Graphical abstract
Source: International Journal of Pharmaceutics - April 27, 2016 Category: Drugs & Pharmacology Source Type: research

Treatment of acute lung inflammation by pulmonary delivery of anti-TNF- α siRNA with PAMAM dendrimers in a murine model.
In this study, commercially available generation 3 poly(amidoamine) (PAMAM) dendrimer was investigated for pulmonary delivery of siRNA directed against tumor necrosis factor (TNF) α for the treatment of acute lung inflammation. Delivery efficiency was assessed in vitro in the RAW264.7 macrophage cell line activated with lipopolysaccharide (LPS), and efficacy was evaluated in vivo in a murine model of LPS-induced lung inflammation upon pre-treatment with TNF-α siRNA. The PAMAM dendrimer-siRNA complexes (dendriplexes) displayed strong siRNA condensation and high cellular uptake in macrophages compared with non-complexed si...
Source: European Journal of Pharmaceutics and Biopharmaceutics - August 12, 2020 Category: Drugs & Pharmacology Authors: Bohr A, Tsapis N, Foged C, Andreana I, Yang M, Fattal E Tags: Eur J Pharm Biopharm Source Type: research

PD-1 siRNA-Encapsulated Solid Lipid Nanoparticles Downregulate PD-1 Expression by Macrophages and Inhibit Tumor Growth : PD-1 siRNA-Encapsulated Solid Lipid Nanoparticles.
In conclusion, the PD-1 siRNA-SLNs inhibited tumor growth, likely related to their ability to downregulate PD-1 expression by tumor-associated macrophage (TAMs). PMID: 33517490 [PubMed - in process]
Source: AAPS PharmSciTech - January 31, 2021 Category: Drugs & Pharmacology Authors: Hanafy MS, Hufnagel S, Trementozzi AN, Sakran W, Stachowiak JC, Koleng JJ, Cui Z Tags: AAPS PharmSciTech Source Type: research

PAMAM versus PEI complexation for siRNA delivery: interaction with model lipid membranes and cellular uptake
ConclusionComplexation of PAMAM dendrimer or bPEI with siRNA modified physicochemical properties of the parent polymer, however it did not impact on the mechanism of interaction with model lipid bilayers or how the polymer/siRNA complex interacted and was internalized by HeLa cells. Interaction of siRNA polymer complexes with cells is related to the action of the parent polymer.Graphical abstract
Source: Pharmaceutical Research - March 22, 2022 Category: Drugs & Pharmacology Source Type: research

Modified gold nanoparticles for intracellular delivery of anti-liver cancer siRNA
Publication date: 17 May 2016 Source:International Journal of Pharmaceutics, Volume 504, Issues 1–2 Author(s): Hanan Shaat, Amany Mostafa, Moustafa Moustafa, Amira Gamal-Eldeen, Ahmed Emam, Enas El-Hussieny, Mahmoud Elhefnawi To overcome the rapid enzymatic degradation and low transfection efficiency of siRNA, the delivery carriers for siRNA is a therapeutic demand to increase its stability. Gold nanoparticles (AuNPs) modified by branched polyethyleneimine (bPEI) were developed as an efficient and safe intracellular delivery carriers for siRNA. The current study implied that siRNA designed against an oncogene c-...
Source: International Journal of Pharmaceutics - April 2, 2016 Category: Drugs & Pharmacology Source Type: research

Counterion of Chitosan Influences Thermodynamics of Association of siRNA with a Chitosan-Based siRNA Carrier
ConclusionAssociation of siRNA with our siRNA carrier was influenced by the nature of counterions associated with chitosan. Driven by entropic phenomena including dehydration, interactions were favored by acetate counterion. Although more work would be needed to decipher the influence of the counterion of chitosan during association with siRNA, it was pointed out as a new critical attribute of chitosan to consider while formulating siRNA carrier with this polysaccharide.
Source: Pharmaceutical Research - January 1, 2020 Category: Drugs & Pharmacology Source Type: research

Novel siRNA Delivery System Using a Ternary Polymer Complex with Strong Silencing Effect and No Cytotoxicity.
Abstract We developed a novel small interfering RNA (siRNA) delivery system using a ternary complex with polyethyleneimine (PEI) and γ-polyglutamic acid (γ-PGA), which showed silencing effect and no cytotoxicity. The binary complexes of siRNA with PEI were approximately 73-102 nm in particle size and 45-52 mV in ζ-potential. The silencing effect of siRNA/PEI complexes increased with an increase of PEI, and siRNA/PEI complexes with a charge ratio greater than 16 showed significant luciferase knockdown in a mouse colon carcinoma cell line regularly expressing luciferase (Colon26/Luc cells). However, strong cy...
Source: Biological and Pharmaceutical Bulletin - August 9, 2014 Category: Drugs & Pharmacology Authors: Kodama Y, Shiokawa Y, Nakamura T, Kurosaki T, Aki K, Nakagawa H, Muro T, Kitahara T, Higuchi N, Sasaki H Tags: Biol Pharm Bull Source Type: research

TPX2 siRNA regulates growth and invasion of esophageal cancer cells
Conclusion siRNA could effectively inhibit the invasion and metastasis of EC9706 cells, promote the apoptosis of tumor cells and may become a new approach for treatment of esophageal carcinoma.
Source: Biomedicine and Pharmacotherapy - November 1, 2014 Category: Drugs & Pharmacology Source Type: research

In vivo siRNA delivery system for targeting to the liver by poly-l-glutamic acid-coated lipoplex
In this study, we developed anionic polymer-coated liposome/siRNA complexes (lipoplexes) with chondroitin sulfate C (CS), poly-l-glutamic acid (PGA) and poly-aspartic acid (PAA) for siRNA delivery by intravenous injection, and evaluated the biodistribution and gene silencing effect in mice. The sizes of CS-, PGA- and PAA-coated lipoplexes were about 200 nm and their ζ-potentials were negative. CS-, PGA- and PAA-coated lipoplexes did not induce agglutination after mixing with erythrocytes. In terms of biodistribution, siRNAs after intravenous administration of cationic lipoplexes were largely observed in the lungs, but t...
Source: Results in Pharma Sciences - October 12, 2014 Category: Drugs & Pharmacology Source Type: research