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Specialty: Drugs & Pharmacology

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Total 3220 results found since Jan 2013.

siRNA-Based Novel Therapeutic Strategies to Improve Effectiveness of Antivirals: An Insight
AAPS PharmSciTech. 2023 Aug 11;24(6):170. doi: 10.1208/s12249-023-02629-1.ABSTRACTSince the ground-breaking discovery of RNA interference (RNAi), scientists have made significant progress in the field of small interfering RNA (siRNA) treatments. Due to severe barriers to the therapeutic application of siRNA, nanoparticle technologies for siRNA delivery have been designed. For pathological circumstances such as viral infection, toxic RNA abnormalities, malignancies, and hereditary diseases, siRNAs are potential therapeutic agents. However, systemic administration of siRNAs in vivo remains a substantial issue due to a lack o...
Source: AAPS PharmSciTech - August 11, 2023 Category: Drugs & Pharmacology Authors: Krittika Chatterjee Sagheerah Lakdawala Sheikh Shahnawaz Quadir Dinesh Puri Dinesh Kumar Mishra Garima Joshi Sanjay Sharma Deepak Choudhary Source Type: research

siRNA-Mediated Knockdown of P450 Oxidoreductase in Rats: A Tool to Reduce Metabolism by CYPs and Increase Exposure of High Clearance Compounds
Conclusions Anti-POR siRNA can be used to significantly reduce hepatic metabolism by various CYPs as well as greatly increase the bioavailability of high clearance compounds following an oral dose, thus enabling it to be used as a tool to increase drug exposure in vivo.
Source: Pharmaceutical Research - November 14, 2014 Category: Drugs & Pharmacology Source Type: research

Polyene-based cationic lipids as visually traceable siRNA transfer reagents.
Abstract Cationic lipids are promising non-viral vectors for the cellular delivery of nucleic acids. Important considerations for the development of new delivery vectors are enhanced uptake efficiency, low toxicity and traceability. Traceable gene transfer systems however typically require the inclusion of a labeled excipient, and highly sensitive imaging instrumentation to detect the presence of the label. Recently, we reported the synthesis and characterization of colored, polyene cationic phospholipidoids composed of a rigid, polyeneoic acid of predetermined dimension (C20:5 and C30:9) paired with flexible satu...
Source: European Journal of Pharmaceutics and Biopharmaceutics - December 20, 2014 Category: Drugs & Pharmacology Authors: Jubeli E, Raju L, Khalique NA, Bilchuk N, Zegel C, Chen A, Lou HH, Øpstad CL, Zeeshan M, Sliwka H, Partali V, Leopold PL, Pungente MD Tags: Eur J Pharm Biopharm Source Type: research

Anticancer siRNA cocktails as a novel tool to treat cancer cells. Part (B). Efficiency of pharmacological action
Publication date: 15 May 2015 Source:International Journal of Pharmaceutics, Volume 485, Issues 1–2 Author(s): Volha Dzmitruk , Aleksandra Szulc , Dzmitry Shcharbin , Anna Janaszewska , Natallia Shcharbina , Joanna Lazniewska , Darya Novopashina , Marina Buyanova , Maksim Ionov , Barbara Klajnert-Maculewicz , Rafael Gómez-Ramirez , Serge Mignani , Jean-Pierre Majoral , Maria Angeles Muñoz-Fernández , Maria Bryszewska This paper examines a perspective to use newly engineered nanomaterials as effective and safe carriers for gene therapy of cancer. Three different groups of cationic dendrimers (PAMAM, phosphorus, and c...
Source: International Journal of Pharmaceutics - March 27, 2015 Category: Drugs & Pharmacology Source Type: research

Suppression of tumor growth in lung cancer xenograft model mice by poly(sorbitol-co-PEI)-mediated delivery of osteopontin siRNA.
Abstract Small interfering RNA (siRNA)-mediated gene silencing represents a promising strategy for treating diseases such as cancer; however, specific gene silencing requires an effective delivery system to overcome the instability and low transfection efficiency of siRNAs. To address this issue, a polysorbitol-based transporter (PSOT) was prepared by low molecular-weight branched polyethylenimine (bPEI) crosslinked with sorbitol diacrylate (SDA). Osteopontin (OPN) gene, which is highly associated with non-small cell lung cancer (NSCLC) was targeted by siRNA therapy using siRNA targeting OPN (siOPN). Characterizat...
Source: European Journal of Pharmaceutics and Biopharmaceutics - June 30, 2015 Category: Drugs & Pharmacology Authors: Cho WY, Hong SH, Singh B, Islam MA, Lee S, Lee AY, Gankhuyag N, Kim JE, Yu KN, Kim KH, Park YC, Cho CS, Cho MH Tags: Eur J Pharm Biopharm Source Type: research

siRNA Delivery by Stimuli-Sensitive Nanocarriers.
Abstract Since its discovery in the late 1990, small interfering RNA (siRNA) have quickly crept into the biopharmaceutical research as a new and powerful tool for the treatment of different human diseases based on altered gene-expression. Despite promising data from many pre-clinical studies, concrete hurdles still need to be overcome to bring therapeutic siRNAs in clinic. The design of stimuli-sensitive nanopreparations for gene therapy is a lively area of the current research. Compared to conventional systems for siRNA delivery, this type of platform can respond to local stimuli that are characteristics of the p...
Source: Current Pharmaceutical Design - October 23, 2015 Category: Drugs & Pharmacology Authors: Salzano G, Costa DF, Torchilin VP Tags: Curr Pharm Des Source Type: research

Natural Carriers for siRNA Delivery.
Abstract This review is based on carriers of natural origin such as polysaccharides, proteins, and cell derived entities which have been used for delivery of siRNA. To realize the therapeutic potential of a delivery system, the role of the carrier is of utmost importance. Historical aspects of viral vectors, the first carriers of genes are briefly outlined. Chitosan, one of the extensively experimented carriers, alginates and other polysaccharides have shown success in siRNA delivery. Peptides of natural origin and mimics thereof have emerged as another versatile carrier. Exosomes and mini cells of cellular origin...
Source: Current Pharmaceutical Design - October 23, 2015 Category: Drugs & Pharmacology Authors: Karunaratne DN, Jafari M, Ranatunga RJ, Siriwardhana A Tags: Curr Pharm Des Source Type: research

High Sensitivity RT-qPCR Assay of Nonlabeled siRNA in Small Blood Volume for Pharmacokinetic Studies: Application to Survivin siRNA
Abstract RNAi therapeutics provide an opportunity to correct faulty genes, and several RNAi have entered clinical evaluation. The existing quantification methods typically use radioactivity- or fluorescence-labeled RNAi, require large blood volumes, and/or have a limited dynamic detection range. We established a quantitative reverse transcriptase real-time polymerase chain reaction (RT-qPCR) assay to measure RNAi; the model analyte was survivin siRNA (siSurvivin). A second siRNA was used as the internal standard. The three major steps were (a) extraction of the two siRNAs from blood or water, (b) synthesis of the...
Source: The AAPS Journal - October 24, 2015 Category: Drugs & Pharmacology Source Type: research

A novel, anisamide-targeted cyclodextrin nanoformulation for siRNA delivery to prostate cancer cells expressing the sigma-1 receptor
In this study, a cationic cyclodextrin derivative was synthesized to complex siRNA. The nanoparticle was then further modified by exploiting the ability of the β-cyclodextrin cavity to form an inclusion complex with the hydrophobic molecule adamantane. PEGylated adamantane derivatives were synthesized with and without the anisamide-targeting ligand on the terminal end of the PEG chain. Anisamide is known to bind specifically to the sigma receptor which is overexpressed on the surface of prostate cancer cells. The resulting nanocomplexes were slightly cationic and less than 300nm in size. They successfully protected siRNA ...
Source: International Journal of Pharmaceutics - January 12, 2016 Category: Drugs & Pharmacology Source Type: research

Highly stable polyglutamate derivatives/siRNA polyplex efficiently down-relegate survivin expression and augment the efficacy of cisplatin
In this study, we developed the polyglutamate derivative polymer brush, poly(ethyleneglycol) monomethyl ether-b-polyglutamate-g-spermine (mPEG-b-PG-g-spermine, PPGS), which could efficiently deliver survivin-siRNA under ultra-high dilution and in the presence of salt (NaCl 150mM) and serum (10% FBS), most likely due to its PEG-shelled polymer brush structure. On the contrary, aggregation occurred when PEI/siRNA polyplex dispersed in saline and serum-containing media and PEI polyplex dissociated after making a 256-fold dilution. PPGS/si-survivin polyplex exhibited high cellular uptake efficiency and efficiently down-regulat...
Source: International Journal of Pharmaceutics - April 4, 2016 Category: Drugs & Pharmacology Source Type: research

Structure, activity and uptake mechanism of siRNA-lipid nanoparticles with an asymmetric ionizable lipid
Publication date: 20 August 2016 Source:International Journal of Pharmaceutics, Volume 510, Issue 1 Author(s): Yuta Suzuki, Hiroshi Ishihara Lipid nanoparticles (LNPs) represent the most advanced platform for the systemic delivery of siRNA. We have previously reported the discovery of novel ionizable lipids with asymmetric lipid tails, enabling potent gene-silencing activity in hepatocytes in vivo; however, the structure and delivery mechanism had not been elucidated. Here, we report the structure, activity and uptake mechanism of LNPs with an asymmetric ionizable lipid. Zeta potential and hemolytic activity of LNPs sh...
Source: International Journal of Pharmaceutics - July 12, 2016 Category: Drugs & Pharmacology Source Type: research

BACH1 silencing by siRNA inhibits migration of HT-29 colon cancer cells through reduction of metastasis-related genes.
CONCLUSION: Our results indicated that BACH1 down-regulation in HT29 CRC cells had no effect on cell growth but did inhibit cell migration by decreasing metastasis-related genes expression. Collectively, these results suggest that BACH1 may function as an oncogenic driver in colon cancer and may represent as a potential target of gene therapy for CRC treatment. PMID: 27657827 [PubMed - as supplied by publisher]
Source: Biomedicine and pharmacotherapy = Biomedecine and pharmacotherapie - September 18, 2016 Category: Drugs & Pharmacology Authors: Davudian S, Shajari N, Kazemi T, Mansoori B, Salehi S, Mohammadi A, Shanehbandi D, Shahgoli VK, Asadi M, Baradaran B Tags: Biomed Pharmacother Source Type: research

Enhanced Anti-Tumor Efficacy of Lipid-Modified Platinum Derivatives in Combination with Survivin Silencing siRNA in Resistant Non-Small Cell Lung Cancer
ConclusionsCo-treatment of lipid-modified compounds andsurvivin-silencing siRNA can constitute a reliable alternative to cisplatin treatment for cisplatin-resistant lung tumors that merit further evaluation.
Source: Pharmaceutical Research - November 3, 2016 Category: Drugs & Pharmacology Source Type: research