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https://www.readbyqxmd.com/read/28589736/development-and-in-vitro-characterization-of-self-emulsifying-drug-delivery-system-sedds-for-oral-opioid-peptide-delivery
#1
Ožbej Zupančič, Julia Rohrer, Hung Thanh Lam, Julia Anita Grießinger, Andreas Bernkop-Schnürch
AIM: In this study SEDDS for oral delivery of opioid peptide dalargin were developed and characterized in vitro. METHODS: Dalargin lipophilicity was increased by O-esterification of tyrosine OH group, hydrophobic ion pairing or a combination thereof. Distribution coefficients (log D) of lipidized dalargin derivatives were determined. Then, dalargin was incorporated in chosen SEDDS, namely SEDDS-1, composed of 50% Capmul 907, 40% Cremophor EL and 10% propylene glycol and comparatively more lipophilic SEDDS-2 composed of 30% Captex 8000, 30% Capmul MCM, 30% Cremophor EL and 10% propylene glycol...
June 7, 2017: Drug Development and Industrial Pharmacy
https://www.readbyqxmd.com/read/28569515/self-emulsifying-drug-delivery-system-sedds-of-ibuprofen-formulation-in-vitro-and-in-vivo-evaluation
#2
Subhash Chandra Bose Penjuri, Saritha Damineni, Nagaraju Ravouru, Srikanth Reddy Poreddy
The goal of the present study was to develop a self-emulsifying drug delivery system for the oral poorly water-soluble drug ibuprofen and to evaluate its oral bioavailability. Phase diagrams were constructed to determine the phase behaviour of the microemulsions and to compare the efficiency of various surfactant-oil mixtures. The SEDDS formulations of ibuprofen were prepared from a mixture of Labrafil M2125, Cremophor RH40, and Plurol oleique. The prepared emulsions were characterized for in vitro and in vivo behaviour...
2017: Ceská a Slovenská Farmacie
https://www.readbyqxmd.com/read/28553114/ravuconazole-self-emulsifying-delivery-system-in-vitro-activity-against-trypanosoma-cruzi-amastigotes-and-in-vivo-toxicity
#3
Pollyanna Álvaro Spósito, Ana Lia Mazzeti, Caroline de Oliveira Faria, Julio A Urbina, Gwenaelle Pound-Lana, Maria Terezinha Bahia, Vanessa Furtado Mosqueira
Self-emulsifying drug delivery systems (SEDDSs) are lipid-based anhydrous formulations composed of an isotropic mixture of oil, surfactant, and cosurfactants usually presented in gelatin capsules. Ravuconazole (Biopharmaceutics Classification System [BCS] Class II) is a poorly water-soluble drug, and a SEDDS type IIIA was designed to deliver it in a predissolved state, improving dissolution in gastrointestinal fluids. After emulsification, the droplets had mean hydrodynamic diameters <250 nm, zeta potential values in the range of -45 mV to -57 mV, and showed no signs of ravuconazole precipitation...
2017: International Journal of Nanomedicine
https://www.readbyqxmd.com/read/28528850/overview-of-solidification-techniques-for-self-emulsifying-drug-delivery-systems-from-industrial-perspective
#4
J Mandić, A Zvonar Pobirk, F Vrečer, M Gašperlin
Self-emulsifying drug delivery systems (SEDDS) are lipid formulations that improve solubility and oral bioavailability of the incorporated drug with poor biopharmaceutical properties. As liquids they are traditionally filled into soft or hard capsules. Transformation of SEDDS into solid dosage form has been extensively investigated in the recent years because solid dosage forms improve stability, handling and patient compliance. By using different solidification techniques selfemulsifying powders, granules, pellets and tablets can be produced...
May 18, 2017: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/28516413/self-emulsification-of-lipidic-drug-delivery-system-in-pure-water-and-in-concentrated-glycerol-solution
#5
Carole Planchette, Annalisa Mercuri, Lorenzo Arcangeli, Manfred Kriechbaum, Peter Laggner
Self-emulsifying drug delivery systems (SEDDS), often intended for oral delivery, are normally explored in biorelevant aqueous media. The high complexity of these multi-component systems leaves the understanding of self-emulsification poor, hindering formulation rationalization. In this work, we aimed to fill this gap by studying the effects of glycerol on the self-emulsification of a ternary component formulation made of 20% w/w Tween 80, 15% w/w Span 80, and 65% w/w Captex 300 Low C6. The behavior of SEDDS in pure water and a binary mixture of water and glycerol (58...
May 17, 2017: AAPS PharmSciTech
https://www.readbyqxmd.com/read/28506870/development-of-solid-sedds-vii-effect-of-pore-size-of-silica-on-drug-release-from-adsorbed-self-emulsifying-lipid-based-formulations
#6
Suhas G Gumaste, Abu T M Serajuddin
PURPOSE: Lipid-based self-emulsifying drug delivery systems (SEDDS) are usually liquids, and they can be converted into solid dosage forms by adsorbing onto silicates. However, most commercially available silicates are mesoporous with small pore sizes of 1 to 50nm that lead to incomplete emulsification of SEDDS inside the pores and thus incomplete drug release. The objective of this study was to investigate the impact of silica pore size on the extent of drug release from SEDDS solidified by adsorbing onto macroporous silicas with different pore sizes...
May 12, 2017: European Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28492325/theoretical-study-of-the-solvation-effect-on-the-reductive-reaction-of-vinylene-carbonate-in-the-electrolyte-solution-of-lithium-ion-batteries
#7
Kento Kasahara, Hiroshi Nakano, Hirofumi Sato
Carbon monoxide generation reaction of vinylene carbonate (VC) in the electrolyte solution of lithium ion batteries (ethylene carbonate (EC) and 1.0 M LiClO4/EC) is studied using the RISM-SCF-SEDD method, a hybrid methodology of statistical mechanics for molecular liquids and quantum chemistry. The analytical treatment of the solvent and lithium salt enables us to treat the complicated composition of the solution such as the concentration of the salt which is difficult for the methods based on the molecular dynamics (MD) simulation...
May 11, 2017: Journal of Physical Chemistry. B
https://www.readbyqxmd.com/read/28457894/lipophilic-peptide-character-what-oral-barriers-fear-the-most
#8
REVIEW
Ožbej Zupančič, Andreas Bernkop-Schnürch
Peptide therapeutics is currently one of the fastest growing markets worldwide and consequently convenient ways of administration for these drugs are highly on demand. In particular, oral dosage forms would be preferred. A relative large molecular weight and high hydrophilicity, however, result in comparatively very low oral bioavailability being in most cases below 1%. Lipid based formulations (LBF), in particular self-emulsifying drug delivery systems (SEDDS) and solid lipid nanoparticles (SLN) as well as liposomes are among the most promising tools for oral peptide delivery...
April 28, 2017: Journal of Controlled Release: Official Journal of the Controlled Release Society
https://www.readbyqxmd.com/read/28445766/inhibitory-effect-of-emulsifiers-in-sedds-on-protease-activity-just-an-illusion
#9
Noemi Lupo, Una Fidahic, Gergely Hetényi, Janine Griesser, Andreas Bernkop-Schnürch
AIM: Evaluation of inhibitory effect of emulsifiers on pancreatic trypsin and α-chymotrypsin. METHODS: The inhibitory effect of Cremophor EL, Cremophor RH 40, Brij O10, Tween 20, polyethylene glycol 8000, polyethylene glycol 400, Carbitol, Pemulen TR-1, Pemulen TR-2, Carbopol Ultrez 20 and Carbopol Ultrez 21 on pancreatic trypsin and α-chymotrypsin was tested. BAEE (Nα-Benzoyl-l-arginine ethyl ester), BTEE (N-Benzoyl-l-tyrosine ethyl ester), casein and insulin were used as substrates for trypsin and α-chymotrypsin...
April 23, 2017: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/28438550/lipophilic-salts-of-poorly-soluble-compounds-to-enable-high-dose-lipidic-sedds-formulations-in-drug-discovery
#10
Michael Morgen, Ajay Saxena, Xue-Qing Chen, Warren Miller, Richard Nkansah, Aaron Goodwin, Jon Cape, Roy Haskell, Ching Su, Olafur Gudmundsson, Michael Hageman, Anoop Kumar, Gajendra Singh Chowan, Abhijith Rao, Vinay K Holenarsipur
Self-emulsifying drug delivery systems (SEDDS) have been used to solubilize poorly water-soluble drugs to improve exposure in high-dose pharmacokinetic (PK) and toxicokinetic (TK) studies. However, the absorbable dose is often limited by drug solubility in the lipidic SEDDS vehicle. This study focuses on increasing solubility and drug loading of ionizable drugs in SEDDS vehicles using lipophilic counterions to prepare lipophilic salts of drugs. SEDDS formulations of two lipophilic salts-atazanavir-2-naphthalene sulfonic acid (ATV-2-NSA) and atazanavir-dioctyl sulfosuccinic acid (ATV-Doc)-were characterized and their performance compared to atazanavir (ATV) free base formulated as an aqueous crystalline suspension, an organic solution, and a SEDDS suspension, using in vitro, in vivo, and in silico methods...
April 21, 2017: European Journal of Pharmaceutics and Biopharmaceutics
https://www.readbyqxmd.com/read/28434635/readmissions-unplanned-emergency-room-visits-and-surgical-retreatment-rates-after-anti-reflux-procedures
#11
Hsin-Hsiao S Wang, Rohit Tejwani, Steven Wolf, John S Wiener, Jonathan C Routh
INTRODUCTION/BACKGROUND: The choice between endoscopic injection (EI) and ureteroneocystotomy (UNC) for surgical correction of vesicoureteral reflux (VUR) is controversial. OBJECTIVE: To compare postoperative outcomes of EI vs UNC. STUDY DESIGN: This study reviewed linked inpatient (SID), ambulatory surgery (SASD), and emergency department (SEDD) data from five states in the United States (2007-10) to identify pediatric patients with primary VUR undergoing EI or UNC as an initial surgical intervention...
April 7, 2017: Journal of Pediatric Urology
https://www.readbyqxmd.com/read/28425577/postoperative-hemorrhage-and-hospital-revisit-after-transoral-robotic-surgery
#12
Joseph Zenga, Jasmina Suko, Dorina Kallogjeri, Patrik Pipkorn, Brian Nussenbaum, Ryan S Jackson
OBJECTIVES/HYPOTHESIS: To investigate the incidence and complications related to postoperative hemorrhage (POH) after transoral robotic surgery (TORS). STUDY DESIGN: Retrospective review of the State Inpatient Database (SID), the State Ambulatory Surgery Database (SASD), and the State Emergency Department Database (SEDD) from the Healthcare Cost and Utilization Project. METHODS: Patients were identified from the SID, SASD, and SEDD for the states of Florida, New York, and California from 2005 to 2013 who had an International Classification of Diseases, Ninth Edition code for a surgical procedure on the upper aerodigestive tract associated with a code for robotic-assisted surgery...
April 20, 2017: Laryngoscope
https://www.readbyqxmd.com/read/28398288/spatiotemporal-historical-datasets-at-micro-level-for-geocoded-individuals-in-five-swedish-parishes-1813-1914
#13
Finn Hedefalk, Patrick Svensson, Lars Harrie
This paper presents datasets that enable historical longitudinal studies of micro-level geographic factors in a rural setting. These types of datasets are new, as historical demography studies have generally failed to properly include the micro-level geographic factors. Our datasets describe the geography over five Swedish rural parishes, and by linking them to a longitudinal demographic database, we obtain a geocoded population (at the property unit level) for this area for the period 1813-1914. The population is a subset of the Scanian Economic Demographic Database (SEDD)...
April 11, 2017: Scientific Data
https://www.readbyqxmd.com/read/28365295/in-vitro-and-in-vivo-performance-of-monoacyl-phospholipid-based-self-emulsifying-drug-delivery-systems
#14
Thuy Tran, Scheyla D V S Siqueira, Heinz Amenitsch, Anette Müllertz, Thomas Rades
This study investigates the effect of monoacyl phospholipid incorporation on the in vitro and in vivo performance of self-emulsifying drug delivery systems (SEDDS). Monoacyl phosphatidylcholine (Lipoid S LPC 80 (LPC)) was incorporated into four different fenofibrate (FF)-loaded long-chain SEDDS to investigate the impact of LPC on the emulsion droplet size, extent of digestion, colloidal structure evolution and drug precipitation during in vitro lipolysis simulating human conditions and drug bioavailability in a rat model...
March 30, 2017: Journal of Controlled Release: Official Journal of the Controlled Release Society
https://www.readbyqxmd.com/read/28349550/photo-absorption-of-p-coumaric-acid-in-aqueous-solution-rism-scf-sedd-theory-approach
#15
Kenji Hirano, Hiroshi Nakano, Yoshihide Nakao, Hirofumi Sato, Shigeyoshi Sakaki
Photo absorption properties of p-coumaric acid, the chromophore of photoactive yellow protein, in aqueous solution were investigated by means of reference interaction site model self-consistent field with spatial electron density distribution (RISM-SCF-SEDD) method. RISM-SCF-SEDD is a combination methodology of electronic structure theory and statistical mechanics for molecular liquids. Here, time-dependent density functional theory was coupled with RISM equation to study the electronic structure of p-coumaric acid in aqueous system...
March 27, 2017: Journal of Computational Chemistry
https://www.readbyqxmd.com/read/28347848/comparison-of-the-protective-effect-of-self-emulsifying-peptide-drug-delivery-systems-towards-intestinal-proteases-and-glutathione
#16
Gergely Hetényi, Janine Griesser, Michael Moser, Frédéric Demarne, Vincent Jannin, Andreas Bernkop-Schnürch
AIM: The aim of this study was to evaluate the protective effect of self-emulsifying drug delivery systems (SEDDS) for therapeutic peptides towards intestinal proteases and reduced glutathione (GSH). METHODS: Sodium docusate was applied as anionic surfactant for hydrophobic ion pairing with leuprorelin (LEU), insulin (INS) and desmopressin (DES). The complexes were loaded into SEDDS that were characterized regarding droplet size distribution and zeta potential. The release profile of the peptides was examined by dialysis membrane method...
March 24, 2017: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/28323109/self-emulsifying-drug-delivery-systems-design-of-a-novel-vaginal-delivery-system-for-curcumin
#17
S Köllner, I Nardin, R Markt, J Griesser, F Prüfert, A Bernkop-Schnürch
AIM: The aim of this study was to develop a vaginal self-emulsifying delivery system for curcumin being capable of spreading, of permeating the mucus gel layer and of protecting the drug being incorporated in oily nanodroplets towards mucus interactions and immobilization. METHODS: The emulsifying properties of curcumin loaded SEDDS containing 30% Cremophor RH40, 20% Capmul PG-8, 30% Captex 300, 10% DMSO and 10% tetraglycol (SEDD formulation A) as well as 25% PEG 200, 35% Cremophor RH40, 20% Captex 355, 10% Caprylic acid and 10% Tween 80 (SEDD formulation B) after diluting 1+2 with artificial vaginal fluid were characterized regarding droplet size and zeta potential...
June 2017: European Journal of Pharmaceutics and Biopharmaceutics
https://www.readbyqxmd.com/read/28283859/combination-of-sedds-and-preactivated-thiomer-technology-incorporation-of-a-preactivated-thiolated-amphiphilic-polymer-into-self-emulsifying-delivery-systems
#18
Gergely Hetényi, Janine Griesser, Isabelle Nardin, Andreas Bernkop-Schnürch
PURPOSE: The aim of the study was to create novel mucoadhesive drug delivery systems by incorporating amphiphilic hydrophobically modified, thiolated and preactivated polymers (preactivated thiomers) into self-emulsifying drug delivery systems (SEDDS). METHODS: L-Cysteine methyl ester was covalently attached to the polymeric backbone of Pemulen TR-2 and preactivated using 2-mercaptonicotinic acid (2-MNA). These thiomers were incorporated in a concentration of 0...
June 2017: Pharmaceutical Research
https://www.readbyqxmd.com/read/28224392/investigation-of-need-of-natural-bioenhancer-for-a-metabolism-susceptible-drug-raloxifene-in-a-designed-self-emulsifying-drug-delivery-system
#19
Poonam Singh Thakur, Narinder Singh, Abhay T Sangamwar, Arvind Kumar Bansal
Bioenhancers can increase the bioavailability of metabolism susceptible drugs. The present study was designed to understand the impact of bioenhancer on permeability and bioavailability of a biopharmaceutical drug disposition classification system (BDDCS) class II drug raloxifene (RLX). RLX undergoes extensive first pass metabolism by UGT enzymes in gastrointestinal tract (GIT) and has an oral bioavailability of about 2%. Self-emulsifying drug delivery system (SEDDS) of RLX was developed using a designed approach and this formulation was loaded with reported bioenhancers: quercetin and piperine...
February 21, 2017: AAPS PharmSciTech
https://www.readbyqxmd.com/read/28216465/increased-intestinal-permeation-and-modulation-of-presystemic-metabolism-of-resveratrol-formulated-into-self-emulsifying-drug-delivery-systems
#20
G Mamadou, C Charrueau, J Dairou, N Limas Nzouzi, B Eto, G Ponchel
Despite various beneficial biological properties, resveratrol lacks therapeutic applications because of poor bioavailability due to variable absorption and extensive metabolism. The present study aims at evaluating the capability of self-emulsifying drug delivery systems (SEDDS) to enhance resveratrol permeation across rat intestine and to modulate its presystemic metabolism. For that purpose, semi-solid (SS) and liquid (L) SEDDS were prepared and dispersed in an aqueous buffer to produce nanoemulsions (NE)...
February 17, 2017: International Journal of Pharmaceutics
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