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Specialty: Drugs & Pharmacology
Source: International Journal of Pharmaceutics
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Total 111 results found since Jan 2013.
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
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
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
Cationic polyaspartamide-based nanocomplexes mediate siRNA entry and down-regulation of the pro-inflammatory mediator high mobility group box 1 in airway epithelial cells
In conclusion, we have found optimal conditions for down-regulation of HMGB1 by siRNA delivery mediated by polyaminoacidic polymers in airway epithelial cells in the absence of cytotoxicity. Functional and in-vivo studies are warranted. Graphical abstract
Source: International Journal of Pharmaceutics - July 11, 2015 Category: Drugs & Pharmacology Source Type: research
The intracellular pharmacodynamics of siRNA is responsible for the low gene silencing activity of siRNA-loaded nanoparticles in dendritic cells
Publication date: 15 October 2015 Source:International Journal of Pharmaceutics, Volume 494, Issue 1 Author(s): Takashi Nakamura, Yuki Fujiwara, Shota Warashina, Hideyoshi Harashima The delivery of small interfering RNA (siRNA) to dendritic cells (DCs) is a challenging issue for siRNA-loaded lipid nanoparticles. The cause of this difficulty is unknown. The findings reported herein indicate that the rate-limiting step in gene silencing using siRNA-loaded lipid nanoparticles in DCs, as evidenced by a quantitative analysis of each process in siRNA delivery between mouse bone marrow derived DC (BMDC) and other cell lines...
Source: International Journal of Pharmaceutics - August 26, 2015 Category: Drugs & Pharmacology Source Type: research
Brain tumor-targeted therapy by systemic delivery of siRNA with Transferrin receptor-mediated core-shell nanoparticles
This study aims to investigate the therapeutic effects of intravenous administration of T7 peptide modified core-shell nanoparticles (named T7-LPC/siRNA NPs) on brain tumors. Layer-by-layer assembling of protamine/chondroitin sulfate/siRNA/cationic liposomes followed by T7 peptide modification has been carried out in order to obtain a targeted siRNA delivery system. In vitro cellular uptake experiments demonstrated a higher intracellular fluorescence intensity of siRNA in brain microvascular endothelial cells (BMVECs) and U87 glioma cells when treated with T7-LPC/siRNA NPs compared with PEG-LPC/siRNA NPs. In the co-culture...
Source: International Journal of Pharmaceutics - July 14, 2016 Category: Drugs & Pharmacology Source Type: research
Mechanisms of cellular uptake and endosomal escape of calcium-siRNA nanocomplexes
Publication date: 30 December 2016 Source:International Journal of Pharmaceutics, Volume 515, Issues 1–2 Author(s): Matan Goldshtein, Efrat Forti, Emil Ruvinov, Smadar Cohen Ca2+-siRNA nanocomplexes represent a simple yet an effective platform for siRNA delivery into the cell cytoplasm, with subsequent successful siRNA-induced target gene silencing. Herein, we aimed to elucidate the roles played by calcium ions in siRNA nanocomplex formation, cell uptake, and endosomal escape. We investigated whether the replacement of Ca2+in the nanocomplex by other bivalent cations would affect their cell entry and subsequent gene sil...
Source: International Journal of Pharmaceutics - October 9, 2016 Category: Drugs & Pharmacology Source Type: research
CXCR4-targeted modular peptide carriers for efficient anti-VEGF siRNA delivery
Publication date: 30 December 2016 Source:International Journal of Pharmaceutics, Volume 515, Issues 1–2 Author(s): Anna Egorova, Anastasia Shubina, Dmitriy Sokolov, Sergey Selkov, Vladislav Baranov, Anton Kiselev The application of small interfering RNA (siRNA) for specific gene inhibition is a promising strategy in gene therapy treatments. The efficient cellular delivery of therapeutic siRNA is a critical step in RNA interference (RNAi) application. Highly efficient siRNA carriers should be developed for specific cellular uptake, stable RNA-complexes formation and intracellular RNA release. To study these features, we...
Source: International Journal of Pharmaceutics - October 26, 2016 Category: Drugs & Pharmacology Source Type: research
Versatile electrostatically assembled polymeric siRNA nanovectors: can they overcome the limits of siRNA tumor delivery?
Publication date: Available online 11 June 2019Source: International Journal of PharmaceuticsAuthor(s): S. Ben Djemaa, E. Munnier, I. Chourpa, E. Allard-Vannier, S. DavidAbstractThe application of small interfering RNA (siRNA) cancer therapeutics is limited by several extra- and intracellular barriers including the presence of ribonucleases that degrade siRNA, the premature clearance, the impermeability of the cell membrane, or the difficulty to escape endo-lysosomal degradation. Therefore, several delivery systems have emerged to overcome these limitations and to successfully deliver siRNA to the tumor site. This review i...
Source: International Journal of Pharmaceutics - June 21, 2019 Category: Drugs & Pharmacology Source Type: research
High siRNA loading powder for inhalation prepared by co-spray drying with human serum albumin
This study aimed to prepare inhalable siRNA powder formulations that contained high siRNA loading of over 6% w/w by spray drying, with human serum albumin (HSA) investigated as a dispersion enhancer to improve the aerosol performance. The effect of siRNA, HSA and solute concentrations in the formulations were evaluated systemically using factorial analyses. All the spray dried siRNA powders exhibited excellent aerosol performance with fine particle fraction (FPF) consistently over 50% in all the formulations. An enrichment of HSA on the particle surface was observed. Surface corrugation was more prominent as the HSA compos...
Source: International Journal of Pharmaceutics - November 1, 2019 Category: Drugs & Pharmacology Source Type: research
TPP-dendrimer nanocarriers for siRNA delivery to the pulmonary epithelium and their dry powder and metered-dose inhaler formulations
Publication date: 15 July 2017 Source:International Journal of Pharmaceutics, Volume 527, Issues 1–2 Author(s): Elizabeth Bielski, Qian Zhong, Hamad Mirza, Matthew Brown, Ashura Molla, Teresa Carvajal, Sandro R.P. da Rocha The regulation of genes utilizing the RNA interference (RNAi) mechanism via the delivery of synthetic siRNA has great potential in the treatment of a variety of lung diseases. However, the delivery of siRNA to the lungs is challenging due to the poor bioavailability of siRNA when delivered intraveneously, and difficulty in formulating and maintaining the activity of free siRNA when delivered directly ...
Source: International Journal of Pharmaceutics - June 1, 2017 Category: Drugs & Pharmacology Source Type: research
Oral siRNA Delivery Using Dual Transporting Systems to Efficiently Treat Colorectal Liver Metastasis
Publication date: Available online 3 November 2018Source: International Journal of PharmaceuticsAuthor(s): Eun-Ju Hyun, Mohammad Nazmul Hasan, Sung Hun Kang, Sungpil Cho, Yong-Kyu LeeAbstractOral siRNA delivery is an ideal way to translate siRNA therapeutic effects in the clinic due to its ability to be administered in convenient and multiple dosages. However, an effective oral delivery system requires overcoming both a hostile gastrointestinal (GI) environment and non-specific targeting. Here, an HTsRP-NC system is a new oral siRNA delivery system consisting of a siRNA/protamine (sRP) nano-complex protected by a multi-fun...
Source: International Journal of Pharmaceutics - November 4, 2018 Category: Drugs & Pharmacology Source Type: research
Effect of thermal and shear stresses in the spray drying process on the stability of siRNA dry powders
In conclusion, stable siRNA based particles for inhalation purposes could be produced using the spray drying technology.Graphical abstract
Source: International Journal of Pharmaceutics - May 9, 2019 Category: Drugs & Pharmacology Source Type: research
Key determinants of siRNA delivery mediated by unique pH-responsive lipid-based liposomes
Publication date: Available online 12 August 2019Source: International Journal of PharmaceuticsAuthor(s): Mariko Sako, Furan Song, Ayaka Okamoto, Hiroyuki Koide, Takehisa Dewa, Naoto Oku, Tomohiro AsaiAbstractLipid-based nanoparticles, a potential nonviral vector due to their good biocompatibility and biodegradability, have been extensively developed for the delivery of small interfering RNA (siRNA). We designed a unique pH-responsive lipid derivative, a dioleylphosphate-diethylenetriamine conjugate (DOP-DETA). DOP-DETA consists of a pH-responsive triamine and unsaturated fatty acids that accelerate membrane fusion. Our re...
Source: International Journal of Pharmaceutics - August 13, 2019 Category: Drugs & Pharmacology Source Type: research
Biokinetic studies of non-complexed siRNA versus nano-sized PEI F25-LMW/siRNA polyplexes following intratracheal instillation into mice
Publication date: 16 March 2016 Source:International Journal of Pharmaceutics, Volume 500, Issues 1–2 Author(s): Jens Lipka, Manuela Semmler-Behnke, Alexander Wenk, Jana Burkhardt, Achim Aigner, Wolfgang Kreyling Successful gene therapy requires stability and sufficient bioavailability of the applied drug at the site of action. In the case of RNA interference (RNAi), non-viral vectors play a promising role for delivering intact siRNA molecules. We selected a low molecular weight polyethyleneimine (PEI F25-LMW) and investigated the biokinetics of PEI F25-LMW/siRNA polyplexes in comparison to non-complexed siRNA mo...
Source: International Journal of Pharmaceutics - January 31, 2016 Category: Drugs & Pharmacology Source Type: research
