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Specialty: Drugs & Pharmacology

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Total 3220 results found since Jan 2013.

An Amphipathic Structure of a Dipropylglycine-Containing Helical Peptide with Sufficient Length Enables Safe and Effective Intracellular siRNA Delivery
Chem Pharm Bull (Tokyo). 2023;71(3):250-256. doi: 10.1248/cpb.c22-00852.ABSTRACTAmphipathic peptides composed of cationic amino acids and hydrophobic amino acids have cell-penetrating ability and are often used as a delivery tool for membrane-impermeable compounds. Small interfering RNA (siRNAs) are one of the delivery targets for such cell-penetrating peptides (CPPs). Cationic CPPs can associate with anionic siRNAs by electrostatic interactions resulting in the formation of nano-sized complexes, which can deliver siRNAs intracellularly. CPPs containing unnatural amino acids offer promising tools to siRNA delivery. However...
Source: Chemical and Pharmaceutical Bulletin - March 1, 2023 Category: Drugs & Pharmacology Authors: Makoto Oba Mika Shibuya Yuto Yamaberi Hidetomo Yokoo Satoshi Uchida Atsushi Ueda Masakazu Tanaka Source Type: research

Ultrasound-Mediated PLGA-PEI Nanobubbles Carrying STAT6 SiRNA Enhances NSCLC Treatment via Repolarizing Tumor-associated Macrophages from M2 to M1 Phenotypes
CONCLUSION: UMND enhanced PLGA-PEI NBs-STAT6 siRNA to repolarize TAMs from the M2 to the M1 phenotype, thus treating NSCLC. These findings provide a promising therapeutic approach for enhancing NSCLC immunotherapy.PMID:37491853 | DOI:10.2174/1567201820666230724151545
Source: Current Drug Delivery - July 26, 2023 Category: Drugs & Pharmacology Authors: Hong Shu Wenhao Lv Zhi-Jian Ren Hui Li Tiantian Dong Yao Zhang Fang Nie Source Type: research

A holistic analysis of the intrinsic and delivery-mediated toxicity of siRNA therapeutics
Adv Drug Deliv Rev. 2023 Aug 9:115052. doi: 10.1016/j.addr.2023.115052. Online ahead of print.ABSTRACTSmall interfering RNAs (siRNAs) are among the most promising therapeutic platforms in many life-threatening diseases. Owing to the significant advances in siRNA design, many challenges in the stability, specificity and delivery of siRNA have been addressed. However, safety concerns and dose-limiting toxicities still stand among the reasons for the failure of clinical trials of potent siRNA therapies, calling for a need of more comprehensive understanding of their potential mechanisms of toxicity. This review delves into th...
Source: Advanced Drug Delivery Reviews - August 11, 2023 Category: Drugs & Pharmacology Authors: Sheyda Ranjbar Xiao-Bo Zhong Jos é Manautou Xiuling Lu Source Type: research

Improvement of therapeutic efficacy of PLGA nanoformulation of siRNA targeting anti-apoptotic Bcl-2 through chitosan coating.
Abstract Potential use of siRNA as therapeutic agent has elicited a great deal of interest. However, insufficient cellular uptake and poor stability limited its application in therapeutics. In our earlier study, we prepared PLGA nanoparticles for effective delivery of siRNA targeting Bcl-2 gene to block its expression. Purpose of the present study was to improve effectiveness of PLGA nanoformulation of siRNA targeting anti-apoptotic Bcl-2 gene through chitosan coating. We prepared chitosan coated PLGA nanoparticles by using the double emulsion solvent diffusion (DESE) method. Characterization of prepared chitosan ...
Source: European Journal of Pharmaceutical Sciences - January 3, 2013 Category: Drugs & Pharmacology Authors: Jagani HV, Josyula VR, Palanimuthu VR, Hariharapura RC, Gang SS Tags: Eur J Pharm Sci Source Type: research

Western Blot Evaluation of siRNA Delivery by pH-Responsive Peptides
Gene silencing, via RNA interference (RNAi) technologies using small interfering RNA (siRNA), has been developed as an important tool for target identification and validation in drug discovery and has huge therapeutic potential. However, effective delivery into cells presents a major challenge to the use of siRNA. pH-responsive cell-penetrating peptides have attracted considerable attention in recent years as delivery vectors due to their ability to transport their cargos across the biological membrane and/or to promote endosomal escape and prevent lysosomal degradation. To evaluate the in vitro transfection efficiency of ...
Source: Springer protocols feed by Pharmacology/Toxicology - February 26, 2013 Category: Drugs & Pharmacology Source Type: news

Impact of anti-PLK1 siRNA-containing F3-targeted liposomes on the viability of both cancer and endothelial cells.
Abstract We have previously described the development of novel sterically stabilized F3-targeted pH-sensitive liposomes, which exhibited the ability to target both cancer and endothelial cells. Herein, the therapeutic potential of those liposomes was assessed upon encapsulation of a siRNA against a well-validated molecular target, PLK1. Treatment of prostate cancer (PC3) and angiogenic endothelial (HMEC-1) cells with F3-targeted liposomes containing anti-PLK1 siRNA resulted in a significant decrease in cell viability, which was mediated by a marked PLK1 silencing, both at the mRNA and protein levels. Furthermore, ...
Source: European Journal of Pharmaceutics and Biopharmaceutics - May 7, 2013 Category: Drugs & Pharmacology Authors: Gomes-da-Silva LC, Ramalho JS, Pedroso de Lima MC, Simões S, Moreira JN Tags: Eur J Pharm Biopharm Source Type: research

Hsp70 silencing with siRNA in nanocarriers enhances cancer cell death induced by the inhibitor of Hsp90.
The objective of this in vitro study was to silence inducible Hsp70 and to promote celastrol-induced tumor cell death. Hsp70 siRNA loaded chitosan-TPP carriers were prepared by ionic gelation and characterized by photon correlation spectroscopy and asymmetric flow field-flow fractionation combined with dynamic light scattering. Viability of human leukemia and glioblastoma cells and Hsp70 silencing was determined following treatment with chitosan-TPP-Hsp70 siRNA particles. The results showed that silencing of Hsp70 by chitosan-TPP-Hsp70 siRNA treatment significantly reduced cell viability, and enhanced antiproliferative eff...
Source: European Journal of Pharmaceutical Sciences - April 10, 2013 Category: Drugs & Pharmacology Authors: Matokanovic M, Barisic K, Filipovic-Grcic J, Maysinger D Tags: Eur J Pharm Sci Source Type: research

Self-assembling gelling formulation based on a crystalline-phase liquid as a non-viral vector for siRNA delivery.
Abstract Liquid crystalline systems (LCSs) form interesting drug delivery systems. These include in situ gelling delivery systems, which present several advantages for use as self-assembling systems for local drug delivery. The aim of this study was to develop and characterize in situ gelling delivery systems for local siRNA delivery. The influence of the components that form the systems was investigated, and the systems were characterized by polarized light microscopy, small angle X-ray scattering (SAXS), swelling studies, assays of their ability to form a complex with genes and of the stability of the genes in t...
Source: European Journal of Pharmaceutical Sciences - April 8, 2014 Category: Drugs & Pharmacology Authors: Borgheti-Cardoso LN, Depieri LV, Diniz H, Calzzani RA, Fantini MC, Iyomasa MM, Vicentini FT, Bentley MV Tags: Eur J Pharm Sci Source Type: research

siRNA nanotherapeutics: a Trojan horse approach against HIV.
Abstract The concept of RNA interference (RNAi) is gaining popularity for the better management of various diseases, including HIV. Currently, the successful biomedical utilization of siRNA therapeutics is hampered, both in vivo and in vitro, mainly by the inherent inability of naked siRNA to cross the cell membrane. RNAi can potentially improve the weakness of current highly active antiretroviral therapy (HAART) by diminishing the chances of the appearance of antiHIV-resistant strains. Here, we discuss the nanocarrier-mediated delivery of siRNA delivery as well as highlighted the scope of siRNA-mediated gene-sile...
Source: Drug Discovery Today - October 2, 2014 Category: Drugs & Pharmacology Authors: Mishra V, Kesharwani P, Jain NK Tags: Drug Discov Today Source Type: research