keyword
MENU ▼
Read by QxMD icon Read
search

drug stability

keyword
https://www.readbyqxmd.com/read/29779181/tailoring-acyclovir-prodrugs-with-enhanced-antiviral-activity-rational-design-synthesis-human-plasma-stability-and-in-vitro-evaluation
#1
Radoslav L Chayrov, Evgenios K Stylos, Maria V Chatziathanasiadou, Kiril N Chuchkov, Aleksandra I Tencheva, Androniki D Kostagianni, Tsenka S Milkova, Assia L Angelova, Angel S Galabov, Stoyan A Shishkov, Daniel G Todorov, Andreas G Tzakos, Ivanka G Stankova
Bile acid prodrugs have served as a viable strategy for refining the pharmaceutical profile of parent drugs through utilizing bile acid transporters. A series of three ester prodrugs of the antiherpetic drug acyclovir (ACV) with the bile acids cholic, chenodeoxycholic and deoxycholic were synthesized and evaluated along with valacyclovir for their in vitro antiviral activity against herpes simplex viruses type 1 and type 2 (HSV-1, HSV-2). The in vitro antiviral activity of the three bile acid prodrugs was also evaluated against Epstein-Barr virus (EBV)...
May 19, 2018: Amino Acids
https://www.readbyqxmd.com/read/29778824/-gel-in-core-carbosomes-as-novel-ophthalmic-vehicles-with-enhanced-corneal-permeation-and-residence
#2
Mona A Moustafa, Wessam M El-Refaie, Yosra S R Elnaggar, Ossama Y Abdallah
Carbopol is a good bio-adhesive polymer that increases the residence time in the eye. However, the effect of blinking and lacrimation still reduce the amount of polymer and the incorporated drug available for bioadhesion. Gel-core liposomes are advanced systems offering benefits making it a good tool for improved ocular drug delivery and residence time. Incorporation of carbopol in gel-core liposomes and their potential in ocular delivery have not so far been investigated. Fluconazole (FLZ) was selected as a challenging important ocular antifungal suffering from poor corneal permeation and short residence time...
May 17, 2018: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/29778706/validated-stability-indicating-spectrophotometric-methods-for-the-determination-of-silodosin-in-the-presence-of-its-degradation-products
#3
Shereen A Boltia, Mohammed Abdelkawy, Taghreed A Mohammed, Nahla N Mostafa
Five simple, rapid, accurate, and precise spectrophotometric methods are developed for the determination of Silodosin (SLD) in the presence of its acid induced and oxidative induced degradation products. Method A is based on dual wavelength (DW) method; two wavelengths are selected at which the absorbance of the oxidative induced degradation product is the same, so wavelengths 352 and 377 nm are used to determine SLD in the presence of its oxidative induced degradation product. Method B depends on induced dual wavelength theory (IDW), which is based on selecting two wavelengths on the zero-order spectrum of SLD where the difference in absorbance between them for the spectrum of acid induced degradation products is not equal to zero so through multiplying by the equality factor, the absorption difference is made to be zero for the acid induced degradation product while it is still significant for SLD...
April 24, 2018: Spectrochimica Acta. Part A, Molecular and Biomolecular Spectroscopy
https://www.readbyqxmd.com/read/29778036/polymeric-nanoparticles-as-a-platform-for-permeability-enhancement-of-class-iii-drug-amikacin
#4
Saman Fatima, Zeenat Iqbal, A K Panda, M Samim, Sushama Talegaonkar, Farhan Jalees Ahmad
Amikacin (A), a water soluble aminoglycoside antibiotic is commercially available for intravenous administration only. Present investigation is aimed at the development of poly-lactic-co-glycolic acid (PLGA) nanoparticles (A-NPs).1 for oral permeability enhancement of amikacin. The pharmaceutical attributes of the A-NPs revealed particle size, 260.3 ± 2.05 nm, zeta potential, -12.9 ± 1.12 mV and drug content, 40.10 ± 1.87 μg/mg with spherical shape and smooth surface. In vitro antibacterial studies showed that the A-NPs were active against P...
May 16, 2018: Colloids and Surfaces. B, Biointerfaces
https://www.readbyqxmd.com/read/29777934/specific-stability-indicating-spectrofluorimetric-method-for-determination-of-ledipasvir-in-the-presence-of-its-confirmed-degradation-products-application-in-human-plasma
#5
Ramadan Ali, Adel A Marzouk, Reda A Abdelhameid, Mahmoud A Omar
A rapid and specific spectrofluorimetric method with higher sensitivity was developed for determination of ledipasvir (LDS) in tablets and human plasma. The proposed method relies on hydrogen bonding formations between the hydroxyl groups of polyoxyethylene 50 stearate and LDS, causing significant enhancement of its native fluorescence. The fluorescence intensity was measured at 430 nm after excitation at 340 nm. The fluorescence-concentration plot was rectilinear over the range 1-400 ng mL-1 with detection and quantification limits of 0...
May 16, 2018: Spectrochimica Acta. Part A, Molecular and Biomolecular Spectroscopy
https://www.readbyqxmd.com/read/29777855/polymer-lipid-hybrid-nanoparticles-as-enhanced-indomethacin-delivery-systems
#6
Annalisa Dalmoro, Sabrina Bochicchio, Shamil F Nasibullin, Paolo Bertoncin, Gaetano Lamberti, Anna Angela Barba, Rouslan I Moustafine
Non-steroidal anti-inflammatory drugs (NSAIDs), i.e. indomethacin used for rheumatoid arthritis and non-rheumatoid inflammatory diseases, are known for their injurious actions on the gastrointestinal (GI) tract. Mucosal damage can be avoided by using nanoscale systems composed by a combination of liposomes and biodegradable natural polymer, i.e. chitosan, for enhancing drug activity. Aim of this study was to prepare chitosan-lipid hybrid delivery systems for indomethacin dosage through a novel continuous method based on microfluidic principles...
May 16, 2018: European Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/29777794/regulatory-t-cell-targeted-hybrid-nanoparticles-combined-with-immuno-checkpoint-blockage-for-cancer-immunotherapy
#7
Wenquan Ou, Raj Kumar Thapa, Liyuan Jiang, Soe Zar Chi, Milan Gautam, Jae-Hoon Chang, Jee-Heon Jeong, Sae Kwang Ku, Han-Gon Choi, Chul Soon Yong, Jong Oh Kim
Immunosuppression in tumor microenvironments induced by regulatory T (Treg) cells is regarded a critical mechanism of tumor immune escape and poses a major impediment to cancer immunotherapy. In this study, we developed tLyp1 peptide-conjugated hybrid nanoparticles for targeting Treg cells in the tumor microenvironment. The tLyp1 peptide-modified hybrid nanoparticles presented good stability and effective targeting to Treg cells, and they enhanced the effect of imatinib in downregulating Treg cell suppression through inhibition of STAT3 and STAT5 phosphorylation...
May 16, 2018: Journal of Controlled Release: Official Journal of the Controlled Release Society
https://www.readbyqxmd.com/read/29777765/in-vitro-and-in-vivo-evaluation-of-an-oral-sustained-release-hepatoprotective-caffeine-loaded-w-o-pickering-emulsion-formula-containing-wheat-germ-oil-and-stabilized-by-magnesium-oxide-nanoparticles
#8
Heba Elmotasem, Hala K Farag, Abeer A A Salama
The objective of this study was to innovate an effective oral sustained release hepatoprotective formula for - the water soluble drug - caffeine. Caffeine is rapidly absorbed and eliminated which dictates frequent administration to achieve adequate therapeutic effect. A w/o Pickering emulsion incorporating caffeine in the internal phase was primed. It contained wheat germ oil and was stabilized by synthesized magnesium oxide nanoparticles (MgO NPs). Components selection was based on their antioxidant, hepatoprotective and anticarcinogenic effects...
May 16, 2018: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/29777296/polymersomes-as-nanoreactors-for-preparative-biocatalytic-applications-current-challenges-and-future-perspectives
#9
REVIEW
Ludwig Klermund, Kathrin Castiglione
Polymersomes are hollow, spherical vesicles that are surrounded by a polymer membrane. The applied polymer must be amphiphilic to promote self-assembly in aqueous solution. At the same time, the polymer composition is highly versatile, which leads to diverse properties in terms of chemical and mechanical stability, membrane permeability and the ability to functionalize the membrane. By encapsulating chemical or biological substances within the polymersomes, drug delivery systems, cell mimetics or catalytic nanoreactors can be assembled...
May 17, 2018: Bioprocess and Biosystems Engineering
https://www.readbyqxmd.com/read/29775968/in-silico-structure-prediction-and-inhibition-mechanism-studies-of-athda14-as-revealed-by-homology-modeling-docking-molecular-dynamics-simulation
#10
Ming-Lang Zhao, Wang Wang, Hu Nie, Sha-Sha Cao, Lin-Fang Du
Histone deacetylases (HDACs) play a significant role in the epigenetic mechanism by catalyzing deacetylation of lysine on histone in both animals and plants. HDACs involved in growth, development and response to stresses in plants. Arabidopsis thaliana histone deacetylase 14 (AtHDA14) is found to localize in the mitochondria and chloroplasts, and it involved in photosynthesis and melatonin biosynthesis. However, its mechanism of action was still unknowns so far. Therefore, in this study, we constructed AtHDA14 protein model using homology modeling method, validated using PROCHECK and presented using Ramachandran plots...
May 6, 2018: Computational Biology and Chemistry
https://www.readbyqxmd.com/read/29775669/nanogels-as-potential-drug-nanocarriers-for-cns-drug-delivery
#11
REVIEW
Arti Vashist, Ajeet Kaushik, Atul Vashist, Jyoti Bala, Roozbeh Nikkhah-Moshaie, Vidya Sagar, Madhavan Nair
Hydrogel-based drug delivery systems (DDSs) have versatile applications such, as tissue engineering, scaffolds, drug delivery, and regenerative medicines. The drawback of higher size and poor stability in such DDSs are being addressed by developing nano-sized hydrogel particles, known as nanogels, to achieve the desired biocompatibility and encapsulation efficiency for better efficacy than conventional bulk hydrogels. In this review, we describe advances in the development of nanogels and their promotion as nanocarriers to deliver therapeutic agents to the central nervous system (CNS)...
May 15, 2018: Drug Discovery Today
https://www.readbyqxmd.com/read/29775625/reduction-sensitive-polymeric-nanomedicines-an-emerging-multifunctional-platform-for-targeted-cancer-therapy
#12
Huanli Sun, Yifan Zhang, Zhiyuan Zhong
The development of smart delivery systems that are robust in circulation and quickly release drugs following selective internalization into target cancer cells is a key to precision cancer therapy. Interestingly, reduction-sensitive polymeric nanomedicines showing high plasma stability and triggered cytoplasmic drug release behavior have recently emerged as one of the most exciting platforms for targeted delivery of various anticancer drugs including small chemical drugs, proteins, and nucleic acids. In vivo studies in varying tumor models reveal that these reduction-sensitive multifunctional nanomedicines outperform the currently used clinical formulations and reduction-insensitive counterparts, bringing about not only significantly enhanced tumor selectivity, accumulation and inhibition efficacy but also markedly reduced systemic toxicity and improved therapeutic index...
May 15, 2018: Advanced Drug Delivery Reviews
https://www.readbyqxmd.com/read/29775296/incorporation-of-a-theranostic-two-tone-luminescent-silver-complex-into-biocompatible-agar-hydrogel-composite-for-the-eradication-of-eskape-pathogens-in-a-skin-and-soft-tissue-infection-model
#13
Miguel N Pinto, Jorge Martinez-Gonzalez, Indranil Chakraborty, Pradip K Mascharak
Microbial invasion and colonization of the skin and underlying soft tissues are among the most common types of infections, becoming increasingly prevalent in hospital settings. Systemic antibiotic chemotherapies are now extremely limited due to emergence of drug-resistant Gram-positive and multidrug-resistant Gram-negative bacterial strains. Topical administration of antimicrobials provides an effective route for the treatment of skin and soft tissue infections (SSTIs). Therefore, the development of new and effective materials for the delivery of these agents is of paramount importance...
May 18, 2018: Inorganic Chemistry
https://www.readbyqxmd.com/read/29774926/an-anionic-shell-shields-a-cationic-core-allowing-for-uptake-and-release-of-polyelectrolytes-within-core-shell-responsive-microgels
#14
Arjan P H Gelissen, Andrea Scotti, Sarah K Turnhoff, Corinna Janssen, Aurel Radulescu, Andrij Pich, Andrey A Rudov, Igor I Potemkin, Walter Richtering
To realize carriers for drug delivery, cationic containers are required for anionic guests. Nevertheless, the toxicity of cationic carriers limits their practical use. In this study, we investigate a model system of polyampholyte N-isopropylacrylamide (NIPAM)-based microgels with a cationic core and an anionic shell to study whether the presence of a negative shell allows the cationic core to be shielded while still enabling the uptake and release of the anionic guest polyelectrolytes. These microgels are loaded with polystyrene sulfonate of different molecular weights to investigate the influence of their chain length on the uptake and release process...
May 18, 2018: Soft Matter
https://www.readbyqxmd.com/read/29774759/melatonin-stimulated-biosynthesis-of-anti-microbial-znonps-by-enhancing-bio-reductive-prospective-in-callus-cultures-of-catharanthus-roseus-var-alba
#15
Hafiza Rida Riaz, Syed Salman Hashmi, Tariq Khan, Christophe Hano, Nathalie Giglioli-Guivarc'h, Bilal Haider Abbasi
Melatonin as plant growth regulator induces differential effects on metabolites that are responsible for reduction, capping and stabilization of zinc oxide nanoparticles. Phytochemical analysis of callus cultures was performed and results were compared with callus cultures supplemented with other plant growth regulators (α-napthalene acetic acid, 2,4-dichlorophenoxy acetic acid and thidiazuron). Highest total phenolic and flavonoid content [42.23 mg of gallic acid equivalent (GAE) g-1 DW and 36.4 mg of (quercetin equivalent) g-1 DW, respectively] were recorded at melatonin (1...
May 18, 2018: Artificial Cells, Nanomedicine, and Biotechnology
https://www.readbyqxmd.com/read/29774521/patient-reported-outcomes-of-multiple-myeloma-patients-treated-with-panobinostat-after-%C3%A2-2-lines-of-therapy-based-on-the-international-phase-3-randomized-double-blind-placebo-controlled-panorama-1-trial
#16
Paul G Richardson, Robert L Schlossman, Anuja N Roy, Ashok Panneerselvam, Suddhasatta Acharyya, Monika Sopala, Sagar Lonial
The phase 3 PANORAMA-1 trial led to regulatory approvals of panobinostat (PAN) in combination with bortezomib (BTZ) and dexamethasone (DEX) for the treatment of multiple myeloma after ≥2 prior regimens, including BTZ and an immunomodulatory drug. Patient-reported outcomes (PROs) were assessed in PANORAMA-1, with data available for 73 patients in the PAN + BTZ + DEX arm and 74 patients in the placebo (PBO) + BTZ + DEX arm. Per the European Organisation for Research and Treatment of Cancer Quality of Life Questionnaire-Core 30 (EORTC QLQ-C30), global health status/quality of life (QoL) scores initially declined with PAN + BTZ + DEX during the first 24 weeks before approaching baseline scores and remaining steady during the next 24 weeks, with no difference between arms at Week 48...
May 17, 2018: British Journal of Haematology
https://www.readbyqxmd.com/read/29774078/targeting-intracellular-mmps-efficiently-inhibits-tumor-metastasis-and-angiogenesis
#17
Yaqi Lv, Xiangmei Zhao, Lidan Zhu, Sijia Li, Qingqing Xiao, Wei He, Lifang Yin
Treatment for metastatic cancer is a great challenge throughout the world. Commonly, directed inhibition of extracellular matrix metalloproteinases (MMPs) secreted by cancer cells can reduce metastasis. Here, a novel nanoplatform (HPMC NPs) assembled from hyaluronic acid (HA)-paclitaxel (PTX) prodrug and marimastat (MATT)/β-casein (CN) complexes was established to cure a 4T1 metastatic cancer model via targeting CD44 and intracellular, rather than extracellular, MMPs. Methods: HPMC NPs were prepared by assembling the complexes and prodrug under ultrasonic treatment, which the interaction between them was evaluated by förster resonance energy transfer, circular dichroism and fluorescence spectra...
2018: Theranostics
https://www.readbyqxmd.com/read/29773918/rna-modifying-proteins-as-anticancer-drug-targets
#18
REVIEW
P Ann Boriack-Sjodin, Scott Ribich, Robert A Copeland
All major biological macromolecules (DNA, RNA, proteins and lipids) undergo enzyme-catalysed covalent modifications that impact their structure, function and stability. A variety of covalent modifications of RNA have been identified and demonstrated to affect RNA stability and translation to proteins; these mechanisms of translational control have been termed epitranscriptomics. Emerging data suggest that some epitranscriptomic mechanisms are altered in human cancers as well as other human diseases. In this Review, we examine the current understanding of RNA modifications with a focus on mRNA methylation, highlight their possible roles in specific cancer indications and discuss the emerging potential of RNA-modifying proteins as therapeutic targets...
May 18, 2018: Nature Reviews. Drug Discovery
https://www.readbyqxmd.com/read/29773886/pretreatment-with-broad-spectrum-antibiotics-alters-the-pharmacokinetics-of-major-constituents-of-shaoyao-gancao-decoction-in-rats-after-oral-administration
#19
Meng Liu, Jie Yuan, Wen-Juan Hu, Chang-Qiang Ke, Yi-Fan Zhang, Yang Ye, Da-Fang Zhong, Guang-Rong Zhao, Sheng Yao, Jia Liu
The influence of broad-spectrum antibiotics on the pharmacokinetics and biotransformation of major constituents of Shaoyao-Gancao decoction (SGD) in rats was investigated. The pharmacokinetic behaviors of paeoniflorin (PF), albiflorin (AF), liquiritin (LT), isoliquiritin (ILT), liquiritin apioside (LA), isoliquiritin apioside (ILA), and glycyrrhizic acid (GL), seven major constituents of SGD, as well as glycyrrhetinic acid (GA), a major metabolite of GL, were analyzed. A 1-week pretreatment with broad-spectrum antibiotics (ampicillin, metronidazole, neomycin, 1 g L-1 ; and vancomycin, 0...
May 17, 2018: Acta Pharmacologica Sinica
https://www.readbyqxmd.com/read/29773368/mutlifunctional-nanoparticles-prepared-from-arginine-modified-chitosan-and-thiolated-fucoidan-for-oral-delivery-of-hydrophobic-and-hydrophilic-drugs
#20
Chien-Ho Chen, Yung-Song Lin, Shao-Jung Wu, Fwu-Long Mi
Self-assembled nanoparticles (NPs) from arginine-modified chitosan (CS-N-Arg) and thiolated fucoidan (THL-fucoidan) were synthesized to enhance the transport of dextran and curcumin across intestinal epithelial cell layer. CS-N-Arg/THL-fucoidan NPs exhibited a pH-sensitive assembly-disassembly and drug release property. Evaluations of the NPs in enhancing the transport of a hydrophilic macromolecule (FITC-dextran) and a hydrophobic drug (curcumin) were investigated in Caco-2 cell monolayers. The cationic CS-N-Arg in the NPs induced disruption of intestinal epithelial tight junctions as indicated by the decrease of transepithelial electrical resistance (TEER)...
August 1, 2018: Carbohydrate Polymers
keyword
keyword
81597
1
2
Fetch more papers »
Fetching more papers... Fetching...
Read by QxMD. Sign in or create an account to discover new knowledge that matter to you.
Remove bar
Read by QxMD icon Read
×

Search Tips

Use Boolean operators: AND/OR

diabetic AND foot
diabetes OR diabetic

Exclude a word using the 'minus' sign

Virchow -triad

Use Parentheses

water AND (cup OR glass)

Add an asterisk (*) at end of a word to include word stems

Neuro* will search for Neurology, Neuroscientist, Neurological, and so on

Use quotes to search for an exact phrase

"primary prevention of cancer"
(heart or cardiac or cardio*) AND arrest -"American Heart Association"