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Specialty: Drugs & Pharmacology

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Total 3220 results found since Jan 2013.

Effective Skin Cancer Treatment by Topical Co-delivery of Curcumin and STAT3 siRNA Using Cationic Liposomes.
Abstract The aim of the present study was to evaluate the effectiveness of iontophoretic co-delivery of curcumin and anti-STAT3 siRNA using cationic liposomes against skin cancer. Curcumin was encapsulated in DOTAP-based cationic liposomes and then complexed with STAT3 siRNA. This nanocomplex was characterized for the average particle size, zeta-potential, and encapsulation efficiency. The cell viability studies in B16F10 mouse melanoma cells have shown that the co-delivery of curcumin and STAT3 siRNA significantly (p < 0.05) inhibited the cancer cell growth compared with either liposomal curcumin or STAT3 si...
Source: AAPS PharmSciTech - June 21, 2017 Category: Drugs & Pharmacology Authors: Jose A, Labala S, Ninave KM, Gade SK, Venuganti VVK Tags: AAPS PharmSciTech 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

siRNA-mediated protein knockdown in precision-cut lung slices.
Abstract Small interfering RNA (siRNA) can induce RNA interference, which leads to the knockdown of messenger RNA (mRNA) and protein. As a result, siRNA is often used in vitro and in vivo to unravel the function of genes and as a therapeutic agent to disrupt excessive expression of disease-related genes. However, there is a large gap between in vitro and in vivo models in terms of simplicity, flexibility, throughput, and translatability. This gap could be bridged by using precision-cut tissue slices, which represent viable explants prepared from animal or human tissue that can be cultured ex vivo. Previously, we d...
Source: European Journal of Pharmaceutics and Biopharmaceutics - November 7, 2018 Category: Drugs & Pharmacology Authors: Ruigrok MJR, Xian JL, Frijlink HW, Melgert BN, Hinrichs WLJ, Olinga P Tags: Eur J Pharm Biopharm Source Type: research

Let-7 miRNA and CDK4 siRNA co-encapsulated in Herceptin-conjugated liposome for breast cancer stem cells
In conclusion, an efficient liposomal delivery system for the combination of miRNA and siRNA to target the BCSCs was developed and could be used as an efficacious therapeutic modality for breast cancer.Graphical AbstractHerceptin-conjugated cationic liposome can enhance the cellular uptake of let-7 miRNA and CDK4 siRNA toward the HER-2 expressing breast cancer stem cells.
Source: Asian Journal of Pharmaceutical Sciences - May 8, 2019 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

Transmigration of Tetraspanin 2 (Tspan2) siRNA Via Microglia Derived Exosomes across the Blood Brain Barrier Modifies the Production of Immune Mediators by Microglia Cells
AbstractMicroglia are implicated in the neuropathogenesis of HIV. Tetraspanin 2 (Tspan2) is closely related to CD9 and CD81 proteins, and are expressed on microglia cells. They have been implicated in cell fusion and adhesion and in the immune response, and neuroinflammation. Developing therapeutics that target microglia remains a challenge as these therapeutics must cross the Blood-Brain Barrier (BBB). Our goal was to use microglia derived exosomes as a vehicle to deliver siRNA across the BBB to target human telomerase reverse transcriptase immortalized human microglial cells (HTHU) latently infected by HIV (HTHU-HIV) and...
Source: Journal of NeuroImmune Pharmacology - December 9, 2019 Category: Drugs & Pharmacology Source Type: research

Development of a carrier system containing hyaluronic acid and protamine for siRNA delivery in the treatment of melanoma
SummaryThe use of small interfering RNA (siRNA) in melanoma treatment remains limited owing to its biological properties. Herein, we developed a carrier system containing hyaluronic acid and protamine for siRNA delivery. Considering zeta potential and particle size as standards, the ratio of each component in liposome nanoparticles prepared was screened using the control variable method, and siRNA cationic liposome nanoparticles were prepared based on the optimal results obtained. The encapsulation rate of the cationic liposome nanoparticles was measured, and particle morphology was observed. B16F10 cells were treated with...
Source: Investigational New Drugs - August 12, 2020 Category: Drugs & Pharmacology Source Type: research

Lyophilization and nebulization of pulmonary surfactant-coated nanogels for siRNA inhalation therapy.
Abstract RNA interference (RNAi) enables highly specific silencing of potential target genes for treatment of pulmonary pathologies. The intracellular RNAi pathway can be activated by cytosolic delivery of small interfering RNA (siRNA), inducing sequence-specific gene knockdown on the post-transcriptional level. Although siRNA drugs hold many advantages over currently applied therapies, their clinical translation is hampered by inefficient delivery across cellular membranes. We previously developed hybrid nanoparticles consisting of an siRNA-loaded nanosized hydrogel core (nanogel) coated with Curosurf®, a clinic...
Source: European Journal of Pharmaceutics and Biopharmaceutics - October 2, 2020 Category: Drugs & Pharmacology Authors: Merckx P, Lammens J, Nuytten G, Bogaert B, Guagliardo R, Maes T, Vervaet C, De Beer T, De Smedt SC, Raemdonck K Tags: Eur J Pharm Biopharm Source Type: research

Targeted nanomedicine with anti-EGFR scFv for siRNA delivery into triple negative breast cancer cells.
Abstract A targeted nanomedicine with humanized anti-EGFR scFv (NM-scFv) was developed for siRNA delivery into triple negative breast cancer (TNBC) cells. NM-scFv consisted of i) targeted nanovector (NV-scFv): nano-cargo with targeting properties; ii) siRNA: pharmacological agent and iii) cationic polymers (chitosan, poly-L-arginine): for siRNA complexation and endosomal escape. NV-scFv was based on superparamagnetic nanoparticle (SPION) labeled with DylightTM680, a PEG layer and a humanized anti-EGFR scFv. The PEG density was optimized from 236±3 to 873±4 PEGs/NV-scFv and the number of targeting ligands per NV-...
Source: European Journal of Pharmaceutics and Biopharmaceutics - October 12, 2020 Category: Drugs & Pharmacology Authors: Vinh Nguyen P, Hervé-Aubert K, David S, Lautram N, Passirani C, Chourpa I, Aubrey N, Allard-Vannier E Tags: Eur J Pharm Biopharm Source Type: research

Therapeutic siRNA: State-of-the-Art and Future Perspectives
This article reviews the knowledge on siRNA design and chemical modification, as well as issues related to siRNA delivery that may be addressed using different delivery systems. Details on the mode of action and clinical status of the various siRNA therapeutics are provided, before giving an outlook on issues regarding the future of siRNA drugs and on their potential as one emerging standard modality in pharmacotherapy. Notably, this may also cover otherwise un-druggable diseases, the definition of non-coding RNAs as targets, and novel concepts of personalized and combination treatment regimens.
Source: BioDrugs - August 23, 2022 Category: Drugs & Pharmacology Source Type: research

Liposomal siRNA nanocarriers for cancer therapy.
Abstract Small interfering RNAs (siRNA) have recently emerged as a new class of therapeutics with a great potential to revolutionize the treatment of cancer and other diseases. A specifically designed siRNA binds and induces post-transcriptional silencing of target genes (mRNA). Clinical applications of siRNA-based therapeutics have been limited by their rapid degradation, poor cellular uptake, and rapid renal clearance following systemic administration. A variety of synthetic and natural nanoparticles composed of lipids, polymers, and metals have been developed for siRNA delivery, with different efficacy and safe...
Source: Advanced Drug Delivery Reviews - December 30, 2013 Category: Drugs & Pharmacology Authors: Ozpolat B, Sood AK, Lopez-Berestein G Tags: Adv Drug Deliv Rev Source Type: research

Development and Characterization of siRNA Lipoplexes: Effect of Different Lipids, In Vitro Evaluation in Cancerous Cell Lines and In Vivo Toxicity Study.
Abstract Cationic liposomes have long been used as non-viral vectors for small interfering RNA (siRNA) delivery but are associated with high toxicity, less transfection efficiency, and in vivo instability. In this investigation, we have developed siRNA targeted to RRM1 that is responsible for development of resistance to gemcitabine in cancer cells. Effect of different lipid compositions has been evaluated on formation of stable and less toxic lipoplexes. Optimized cationic lipoplex (D2CH) system was comprised of dioleoyl-trimethylammoniumpropane (DOTAP), dioleoyl-sn-glycero-3-phosphoethanolamine (DOPE), hydrogena...
Source: AAPS PharmSciTech - August 22, 2014 Category: Drugs & Pharmacology Authors: Khatri N, Baradia D, Vhora I, Rathi M, Misra A Tags: AAPS PharmSciTech Source Type: research

New Techniques to Assess In Vitro Release of siRNA from Nanoscale Polyplexes
Conclusions We introduce new methods for the efficient and informative characterization of siRNA polyplexes with special attention to stability. Comparing FRET-labeled siRNA in different polyplexes associates successful knockdown with intermediate siRNA stability in various steps from formulation to intracellular persistence.
Source: Pharmaceutical Research - December 9, 2014 Category: Drugs & Pharmacology Source Type: research