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Specialty: Drugs & Pharmacology

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Total 3220 results found since Jan 2013.

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

5'-triphosphate-siRNA activates RIG-I-dependent type I interferon production and enhances inhibition of hepatitis B virus replication in HepG2.2.15 cells.
In conclusion, our findings suggest that 3p-siRNA could act as a powerful bifunctional antiviral molecule with potential for developing a promising therapeutic against chronic HBV infection. PMID: 24099962 [PubMed - as supplied by publisher]
Source: European Journal of Pharmacology - October 4, 2013 Category: Drugs & Pharmacology Authors: Chen X, Qian Y, Yan F, Tu J, Yang X, Xing Y, Chen Z Tags: Eur J Pharmacol Source Type: research

Evaluation of multimeric siRNA conjugates for efficient protamine-based delivery into breast cancer cells.
This study demonstrates that multi-siRNA conjugates greatly facilitate the formulation of nano-sized protamine-based carriers and significantly improve intracellular delivery in vitro compared to common siRNAs, and therefore may provide a platform for the design of peptide-based siRNA delivery systems for in vivo applications. PMID: 24687259 [PubMed - as supplied by publisher]
Source: Archives of Pharmacal Research - April 1, 2014 Category: Drugs & Pharmacology Authors: Yoo H, Mok H Tags: Arch Pharm Res Source Type: research

Efficient siRNA Delivery Using PEG-conjugated PAMAM Dendrimers Targeting Vascular Endothelial Growth Factor in a CoCl2-induced Neovascularization Model in Retinal Endothelial Cells.
Abstract Choroidal neovascularization (CNV), also known as subretinal neovascularization, causes serious damage to the central vision as it happens more commonly in macula. The most important factor involved in angiogenesis is vascular endothelial growth factor (VEGF). By an RNAi technique, VEGF gene knockdown can be used to treat CNV. PEG-conjugated poly (amidoamine) (PEG-PAMAM) dendrimers as a new type of synthetic polymers are very promisingto begene delivery carriers. To investigate siRNA delivery efficacy of PEG-PAMAM dendrimers, we prepared dendriplexes of PEG-PAMAM dendrimers with a fluorescence-labelled si...
Source: Current Drug Delivery - August 17, 2015 Category: Drugs & Pharmacology Authors: Xua L, Shena W, Wang B, Wang X, Liua G, Taoc Y, Qia R Tags: Curr Drug Deliv Source Type: research

Co-delivery of Epirubicin and siRNA Using Functionalized Mesoporous Silica Nanoparticles Enhances In vitro and In vivo Drug Efficacy.
Abstract Development of drug resistance to anticancer drugs is an important challenge for cancer treatment. Recent studies focus on co-delivery of anticancer drugs and siRNA to overcome this challenge. Mesoporous silica nanoparticles (MSNs) are one of the promising nanoparticles that enable the delivery of drugs and siRNA simultaneously. MSNs coated with copolymer that able for co-delivery of drug and siRNA were prepared and characterized. In the present study, MSNs functionalized with polyethylenimine-polyethylene glycol (PEI-PEG) copolymer were prepared. MSNs were characterized using dynamic light scattering (DL...
Source: Current Drug Delivery - December 30, 2015 Category: Drugs & Pharmacology Authors: YahyaHanafi-Bojd M, Jaafari MR, Ramezanian N, Abnous K, Malaekeh-Nikouei B Tags: Curr Drug Deliv Source Type: research

EGF-modified mPEG-PLGA-PLL nanoparticle for delivering doxorubicin combined with Bcl-2 siRNA as a potential treatment strategy for lung cancer.
CONCLUSION: We conclude that co-delivery of Dox and Bcl-2-siRNA by tumor-targeted EGF-PEAL NPs could significantly inhibit lung cancer growth. PMID: 26739487 [PubMed - as supplied by publisher]
Source: Drug Delivery - February 16, 2016 Category: Drugs & Pharmacology Tags: Drug Deliv 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

Conjugates of HA2 with octaarginine-grafted HPMA copolymer offer effective siRNA delivery and gene silencing in cancer cells.
Abstract The key for successful gene silencing is to design a safe and efficient siRNA delivery system for the transfer of therapeutic nucleic acids into the target cells. Here, we describe the design of hydrophilic N-(2-hydroxypropyl)methacrylamide (HPMA) copolymer displaying multiple copies of octaarginine (R8) and its use in promoting the effective delivery of small interfering RNA (siRNA) molecules intracellularly. Fluorescein-5-isothiocyanate (FITC)-labeled HPMA copolymer-bound R8 (P-R8-FITC) was synthesized with increasing R8 molar ratios (4 to 9.5 mol-%) to define the optimal R8 content that allowed the pol...
Source: European Journal of Pharmaceutics and Biopharmaceutics - September 30, 2016 Category: Drugs & Pharmacology Authors: Golan M, Feinshtein V, David A Tags: Eur J Pharm Biopharm 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

STAT3-siRNA induced B16.F10 melanoma cell death: Association with VEGF downregulation than p-STAT3 knockdown
Publication date: Available online 30 May 2018 Source:Saudi Pharmaceutical Journal Author(s): Aws Alshamsan STAT3 knockdown by small interfering RNA (siRNA) has been described to inhibit carcinogenic growth in various types of tumors. Earlier we have reported delivery of siRNA by oleic acid- and stearic acid-modified-polyethylenimine and enhancement of silencing of STAT3 by small interfering RNA (siRNA) in B16.F10 melanoma cell lines and consequent tumor suppression. Present investigation mainly focused on the downstream events involved in B16.F10 melanoma cell death and consequent tumor suppression following knockdown of...
Source: Saudi Pharmaceutical Journal - May 31, 2018 Category: Drugs & Pharmacology Source Type: research

STAT3-siRNA induced B16.F10 melanoma cell death: more association with VEGF downregulation than p-STAT3 knockdown
Publication date: Available online 30 May 2018 Source:Saudi Pharmaceutical Journal Author(s): Aws Alshamsan STAT3 knockdown by small interfering RNA (siRNA) has been described to inhibit carcinogenic growth in various types of tumors. Earlier we have reported delivery of siRNA by oleic acid- and stearic acid-modified-polyethylenimine and enhancement of silencing of STAT3 by small interfering RNA (siRNA) in B16.F10 melanoma cell lines and consequent tumor suppression. Present investigation mainly focused on the downstream events involved in B16.F10 melanoma cell death and consequent tumor suppression following knockdown of...
Source: Saudi Pharmaceutical Journal - June 6, 2018 Category: Drugs & Pharmacology Source Type: research