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https://www.readbyqxmd.com/read/27914041/paliperidone-loaded-nanolipomer-system-for-sustained-delivery-and-enhanced-intestinal-permeation-superiority-to-polymeric-and-solid-lipid-nanoparticles
#1
Hala Mahmoud Helal, Sana Mohamed Mortada, Marwa Ahmed Sallam
Paliperidone (PPD) is the most recent second-generation atypical antipsychotic approved for the treatment of schizophrenia. An immediate release dose causes extrapyramidal side effects. In this work, a novel nanolipomer carrier system for PPD with enhanced intestinal permeability and sustained release properties has been developed and optimized. PPD was successfully encapsulated into a lipomer consisting of a specific combination of biocompatible materials including poly-ε-caprolactone as a polymeric core, Lipoid S75, and Gelucire® 50/13 as a lipid shell and polyvinyl alcohol as a stabilizing agent...
December 2, 2016: AAPS PharmSciTech
https://www.readbyqxmd.com/read/27913974/incorporation-of-estradiol-benzoate-to-cidr-protocol-improves-the-reproductive-responses-in-crossbred-dairy-heifers
#2
Muhammad Usman Mehmood, Ahmad Qamar, Abdul Sattar, Liaquat Ahmad, Nasim Ahmad
The present study was designed to determine the effect of estradiol benzoate (EB) on reproductive response following a controlled internal drug release (CIDR) protocol in crossbred (Sahiwal × Friesian) dairy heifers. In the first trial, a total of 100 crossbred dairy heifers were treated with CIDR protocol for 7 days and injected with the PGF2α on day 6. After 24 h of CIDR removal, one group (EB = 50) was injected with estradiol benzoate whereas the other (control = 50) remained untreated. Estrus intensity and response were recorded visually and ovulation rate was recorded by ultrasonography...
December 2, 2016: Tropical Animal Health and Production
https://www.readbyqxmd.com/read/27913319/assessing-the-benefits-of-targeted-drug-delivery-by-nanocarriers-a-partico-pharmacokinetic-framework
#3
Ronald A Siegel, Ameya R Kirtane, Jayanth Panyam
OBJECTIVE: An in vivo kinetic framework is introduced to analyze and predict the quantitative advantage of using nanocarriers to deliver drugs, especially anticancer agents, compared to administering the same drugs in their free form. METHODS: This framework recognizes three levels of kinetics. First is the particokinetics associated with deposition of nanocarriers into tissues associated with drug effect and toxicity, their residence inside those tissues, and elimination of the nanocarriers from the body...
November 29, 2016: IEEE Transactions on Bio-medical Engineering
https://www.readbyqxmd.com/read/27913240/activity-of-vancomycin-release-from-bioinspired-coatings-of-hydroxyapatite-or-tio2-nanotubes
#4
Daniela Ionita, Daniela Bajenaru-Georgescu, Georgeta Totea, Anca Mazare, Patrik Schmuki, Ioana Demetrescu
Herein we investigate the efficiency of various biomimetic coatings for localized drug delivery, using vancomycin as key therapeutic drug, which is a widely used antibiotic for the treatment of strong infections caused by positive Gram bacteria. We evaluate classical hydroxyapatite and biomimetic hydroxyapatite-collagen coatings obtained by electrochemical deposition as well as TiO2 nanotubes arrays obtained by electrochemical anodization. Surface morphology, compositional and structural data confirm the incorporation of vancomycin into the layers and drug release profiles for vancomycin evaluate their release ability...
November 29, 2016: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/27913210/trpv4-activation-of-endothelial-nitric-oxide-synthase-resists-nonalcoholic-fatty-liver-disease-by-blocking-cyp2e1-mediated-redox-toxicity
#5
Ratanesh K Seth, Suvarthi Das, Diptadip Dattaroy, Varun Chandrashekaran, Firas Alhasson, Gregory Michelotti, Mitzi Nagarkatti, Prakash Nagarkatti, Anna Mae Diehl, Darwin P Bell, Wolfgang Liedtke, Saurabh Chatterjee
NAFLD is a clinically progressive disease with steatosis, inflammation, endothelial dysfunction and fibrosis being the stages where clinical intervention becomes necessary. Lack of early biomarkers and absence of a FDA approved drug obstructs efforts for effective treatment. NAFLD progression is strongly linked to a balance between liver injury, tissue regeneration and the functioning of endogenous defense mechanisms. The failure of the defense pathways to resist the tissue damage arising from redox stress, one of the "multiple hits" in disease progression, give rise to heightened inflammation and occasional fibrosis...
November 29, 2016: Free Radical Biology & Medicine
https://www.readbyqxmd.com/read/27913204/the-selective-bcl-2-inhibitor-venetoclax-a-bh3-mimetic-does-not-dysregulate-intracellular-ca-2-signaling
#6
Tamara Vervloessem, Hristina Ivanova, Tomas Luyten, Jan B Parys, Geert Bultynck
Anti-apoptotic B cell-lymphoma-2 (Bcl-2) proteins are emerging as therapeutic targets in a variety of cancers for precision medicines, like the BH3-mimetic drug venetoclax (ABT-199), which antagonizes the hydrophobic cleft of Bcl-2. However, the impact of venetoclax on intracellular Ca(2+) homeostasis and dynamics in cell systems has not been characterized in detail. Here, we show that venetoclax did not affect Ca(2+)-transport systems from the endoplasmic reticulum (ER) in permeabilized cell systems. Venetoclax (1μM) did neither trigger Ca(2+) release by itself nor affect agonist-induced Ca(2+) release in a variety of intact cell models...
November 29, 2016: Biochimica et Biophysica Acta
https://www.readbyqxmd.com/read/27913127/co-assembly-of-doxorubicin-and-curcumin-targeted-micelles-for-synergistic-delivery-and-improving-anti-tumor-efficacy
#7
Wenzhuan Ma, Qiang Guo, Ying Li, Xiaohui Wang, Jinling Wang, Pengfei Tu
Chemotherapeutic drugs have a series of limitations in anti-tumor treatment, mainly including multidrug resistance (MDR) and serious adverse reactions. Co-delivery system with two or more synergistic therapeutic drugs is an effective strategy to settle these limitations. In this study, active tumor-targeted co-delivery micelles (DOX+Cur)-PMs, with two synergistic drugs of a therapeutic drug of doxorubicin (DOX) and a chemosensitizer of curcumin (Cur) co-encapsulated into hyaluronic acid-vitamin E succinate (HA-VES) graft copolymer, were prepared and delivered simultaneously into tumor cells for improving therapeutic effects of DOX...
November 29, 2016: European Journal of Pharmaceutics and Biopharmaceutics
https://www.readbyqxmd.com/read/27913104/d-ala2-gip-glu-pal-is-neuroprotective-in-a-chronic-parkinson-s-disease-mouse-model-and-increases-bndf-expression-while-reducing-neuroinflammation-and-lipid-peroxidation
#8
Yanwei Li, WeiZhen Liu, Lin Li, Christian Hölscher
Type 2 diabetes mellitus (T2DM) is a risk factor for Parkinson's disease (PD). Therefore, treatment to improve insulin resistance in T2DM may be useful for PD patients. Glucose dependent insulinotropic polypeptide (GIP) is a member of the incretin hormone family that can promote insulin release and improve insulin resistance. Several GIP analogues have been developed as potential treatments for T2DM. We had shown previously that D-Ala2-GIP-glu-PAL, a novel long-acting GIP analogue, can play a neuroprotective role in the PD mouse model induced by acute MPTP injection...
November 29, 2016: European Journal of Pharmacology
https://www.readbyqxmd.com/read/27912116/application-of-melatonin-loaded-poly-n-isopropylacrylamide-hydrogel-particles-to-reduce-the-toxicity-of-airborne-pollutes-to-raw264-7-cells
#9
Wenjing Zhang, Pengfei Jiang, Jin Chen, Chaonan Zhu, Zhengwei Mao, Changyou Gao
The adverse effect of airborne PM2.5 pollutes on human beings and the environment, most likely due to heavy metal leaching, has received extensive attention recently. It is urgently required to develop a simple and effective method to suppress the toxicity of PM2.5 pollutes. In this study, the heavy metal content of PM2.5 pollutes around Zhejiang university were firstly identified. Their cytotoxicity was confirmed, by inducing significantly enhanced intracellular reactive oxygen species level. Poly(N-isopropylacrylamide) (PNIPAM) submicron hydrogel particles with tunable crosslinking densities and thermo-responsive swelling/shrinking properties were then prepared by adjusting the crosslinking density...
November 22, 2016: Journal of Colloid and Interface Science
https://www.readbyqxmd.com/read/27911756/activation-of-group-ii-metabotropic-glutamate-receptors-promotes-ltp-induction-at-schaffer-collateral-ca1-pyramidal-cell-synapses-by-priming-nmda-receptors
#10
Nadia Rosenberg, Urs Gerber, Jeanne Ster
: It is well established that selective activation of group I metabotropic glutamate (mGlu) receptors induces LTD of synaptic transmission at Schaffer collateral-CA1 synapses. In contrast, application of 1S,3R-ACPD, a mixed agonist at group I and group II mGlu receptors, induces LTP. Using whole-cell recordings from CA1 pyramidal cells and field recordings in the hippocampal CA1 region, we investigated the specific contribution of group II mGlu receptors to synaptic plasticity at Schaffer collateral-CA1 synapses in acute slices of adult mice...
November 9, 2016: Journal of Neuroscience: the Official Journal of the Society for Neuroscience
https://www.readbyqxmd.com/read/27911136/a-functional-nanocarrier-that-copenetrates-extracellular-matrix-and-multiple-layers-of-tumor-cells-for-sequential-and-deep-tumor-autophagy-inhibitor-and-chemotherapeutic-delivery
#11
Yang Wang, Yue Qiu, Sheng Yin, Li Zhang, Kairong Shi, Huile Gao, Zhirong Zhang, Qin He
To further enhance the intensity of deep tumor drug delivery and integrate a combined therapy, we herein report on a core-shell nanocarrier that could simultaneously overcome the double barriers of the extracellular matrix (ECM) and multiple layers of tumor cells (MLTC). A pH-triggered reversible swelling-shrinking core and an MMP2 (matrix metallopeptidase 2) degradable shell were developed to encapsulate chemotherapeutics and macroautophagy/autophagy inhibitors, respectively. MMP2 degraded the shell, which was followed by the autophagy inhibitors release...
December 2, 2016: Autophagy
https://www.readbyqxmd.com/read/27910742/review-article-fabricated-microparticles-an-innovative-method-to-minimize-the-side-effects-of-nsaids-in-arthritis
#12
Shaivad Shabee Hulhasan Abadi, Afrasim Moin, Gangadharappa Hosahalli Veerabhadrappa
Microparticles are polymeric bodies ranging 1-1000 µm that constitute a variety of forms such as microcapsules, microspheres, microcages, microshells, microrods, biosensors microparticles, radiolabeled microparticles, and so forth. This review focuses on general microparticles, mainly microcapsules and microspheres. Nonsteriodal anti-inflammatory drugs (NSAIDs) are one of the mostcommonly prescribed medications in the world. Most of the NSAIDs available have severe side effects. With increased awareness of NSAID-induced gastrointestinal (GI) side effects, safety has become a priority in treatment of arthritis and other inflammatory diseases with NSAIDs...
2016: Critical Reviews in Therapeutic Drug Carrier Systems
https://www.readbyqxmd.com/read/27910739/overview-on-therapeutic-applications-of-microparticulate-drug-delivery-systems
#13
Swarna Bale, Amit Khurana, A Shiva Shankar Reddy, Mandip Singh, Chandraiah Godugu
Research in novel drug delivery systems is being explored competitively in order to attain maximum therapeutic effect while minimizing the adverse effects. Despite several advancements in pharmaceutical formulations, one of the major challenges still persisting is sustained drug release. Microencapsulation enacts as an intelligent approach with a strong therapeutic impact and is in demand globally in medical technology due to its specific and attractive properties, including biocompatibility, stability, target specificity, uniform encapsulation, better compliance, and controlled and sustained release patterns that are responsible for diminishing the toxicity and dosage frequency...
2016: Critical Reviews in Therapeutic Drug Carrier Systems
https://www.readbyqxmd.com/read/27909943/simulating-different-dosing-scenarios-for-a-child-appropriate-valproate-er-formulation-in-a-new-pediatric-two-stage-dissolution-model
#14
Frank Karkossa, Antonia Krueger, Jana Urbaniak, Sandra Klein
Predictive in vitro test methods addressing the parameters relevant to drug release in the pediatric gastrointestinal tract could be an appropriate means for reducing the number of in vivo studies in children. However, dissolution models addressing the particular features of pediatric gastrointestinal physiology and typical pediatric dosing scenarios have not yet been described. The objective of the present study was to combine the knowledge on common vehicle types and properties and current information on pediatric gastrointestinal physiology to design a dissolution model that enables a biorelevant simulation of the gastrointestinal conditions in young children...
December 1, 2016: AAPS PharmSciTech
https://www.readbyqxmd.com/read/27908759/cathepsin-nanofiber-substrates-as-potential-agent-for-targeted-drug-delivery
#15
Yael Ben-Nun, Galit Fichman, Lihi Adler-Abramovich, Boris Turk, Ehud Gazit, Galia Blum
The development of reactive drug carriers that could actively respond to biological signals is a challenging task. Different peptides can self-assemble into biocompatible nanostructures of various functionalities, including drugs carriers. Minimal building blocks, such as diphenylalanine, readily form ordered nanostructures. Here we present development of self-assembled tetra-peptides that include the diphenylalanine motif, serving as substrates of the cathepsin proteases. This is of great clinical importance as cathepsins, whose activity and expression are highly elevated in cancer and other pathologies, have been shown to serve as efficient enzymes for therapeutic release...
November 28, 2016: Journal of Controlled Release: Official Journal of the Controlled Release Society
https://www.readbyqxmd.com/read/27908758/thermally-triggered-release-of-the-bacteriophage-endolysin-chapk-and-the-bacteriocin-lysostaphin-for-the-control-of-methicillin-resistant-staphylococcus-aureus-mrsa
#16
Hollie Hathaway, Jude Ajuebor, Liam Stephens, Aidan Coffey, Ursula Potter, J Mark Sutton, A Toby A Jenkins
Staphylococcus aureus infections of the skin and soft tissue pose a major concern to public health, largely owing to the steadily increasing prevalence of drug resistant isolates. As an alternative mode of treatment both bacteriophage endolysins and bacteriocins have been shown to possess antimicrobial efficacy against multiple species of bacteria including otherwise drug resistant strains. Despite this, the administration and exposure of such antimicrobials should be restricted until required in order to discourage the continued evolution of bacterial resistance, whilst maintaining the activity and stability of such proteinaceous structures...
November 28, 2016: Journal of Controlled Release: Official Journal of the Controlled Release Society
https://www.readbyqxmd.com/read/27908720/preparation-and-characterization-of-polymeric-nanoparticles-surface-modified-with-chitosan-for-target-treatment-of-colorectal-cancer
#17
Mohamed M Badran, Mohsen M Mady, Magdy M Ghannam, Faiyaz Shakeel
5-Fluorouracil (5-FU) loaded chitosan (C) coated polylactic-co-glycolic acid (PLGA) nanoparticles [NPs] (C-5-FU PLGA NPs) and polycaprolactone [PCL] (C-5-FU PCL NPs) were employed as the carriers for cancer treatment. The prepared NPs showed the spherical shape of NPs with the particle size in the range of 188.1-302.2nm with polydispersity index (PDI) of<0.30. C-coated NPs converted zeta potential from negative to positive value with small modification in particle size distribution. The entrapment efficiency of 5-FU was recorded in the range of 32-51%...
November 28, 2016: International Journal of Biological Macromolecules
https://www.readbyqxmd.com/read/27908412/preparation-physicochemical-characterization-and-antioxidant-activity-of-diphenyl-diselenide-loaded-poly-lactic-acid-nanoparticles
#18
Osmar Dos Reis Antunes Junior, Emilli Antônio, Rubiana Mara Mainardes, Najeh Maissar Khalil
In this study, we developed, characterized and evaluated the antioxidant activity of poly (lactic acid) nanoparticles containing diphenyl diselenide (PhSe)2. Nanoparticles were characterized in terms of mean particle size, polydispersity index, zeta potential, encapsulation efficiency, in vitro release profile, physical stability, polymer-drug interactions and thermal properties. Also, the antioxidant activity of nanoparticles on hypochlorous acid (HOCl) was assessed. Nanoparticles presented a mean size of 210nm, had low polydispersity, zeta potential of -24mV, and an encapsulation efficiency over 90%...
January 2017: Journal of Trace Elements in Medicine and Biology
https://www.readbyqxmd.com/read/27908270/the-importance-of-wireless-capsule-endoscopy-for-research-into-the-intestinal-absorption-window-of-5-aminosalicylic-acid-in-experimental-pigs
#19
Jaroslav Kvetina, Ilja Tacheci, Milan Nobilis, Marcela Kopacova, Martin Kunes, Jan Bures
BACKGROUND: Absorption windows in particular segments of the small intestine can contribute to the development of orally administered drug formulations and can limit the bioavailability of released compounds. OBJECTIVE: The aim of this study was to evaluate use of wireless capsule enteroscopy regarding the disintegration kinetic process of tablets in the small intestine and its comparison with the levels of the model drug (5-aminosalicylic acid; 5-ASA), and its majority metabolite (N-acetyl-5-aminosalicylic acid; N-acetyl-5-ASA) in blood plasma...
December 1, 2016: Current Pharmaceutical Design
https://www.readbyqxmd.com/read/27908267/development-of-poly-lactide-co-glicolide-nanoparticles-incorporating-morphine-hydrochloride-to-prolong-its-circulation-in-blood
#20
Victoria Gómez-Murcia, Mercedes García Montalbán, Juan Carmelo Gómez-Fernández, Pilar Almela
Formulations incorporating nanoparticles (NPs) are widely used to prolong drug release. In this regard, poly(lactide-co-glicolide) (PLGA) is often used in their preparation due to its high degree of biocompatibility and biodegradability. In the present study, morphine HCl is incorporated in PLGA-NPs and different preparation alternatives are evaluated for their effects on the properties, stability and capacity of encapsulation. NPs were prepared by a double emulsion solvent diffusion-ammonium loading (DESD-AL) or double emulsion solvent diffusion-traditional (DESD-T) technique...
December 1, 2016: Current Pharmaceutical Design
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