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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
#1
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
#2
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 16, 2017: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/28212981/development-of-solid-sedds-vi-effect-of-precoating-of-neusilin%C3%A2-us2-with-pvp-on-drug-release-from-adsorbed-self-emulsifying-lipid-based-formulations
#3
Suhas G Gumaste, Beatryz O S Freire, Abu T M Serajuddin
Adsorption of lipid-based formulations, which are usually liquid, onto silicas has been extensively investigated in the past decade to convert them into solid dosage forms. There are conflicting reports on the ability of commercially available porous silicas, like Neusilin® US2, to release lipid formulations completely, especially after long-term storage. In this study, the release of a model drug, probucol, from different formulations of medium chain lipids and a surfactant, Kolliphor EL (Cremophor EL) or polysorbate 80, were studied after adsorbing them onto Neusilin® US2...
February 14, 2017: European Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28188875/hydrophobic-ion-pairing-key-to-highly-payloaded-self-emulsifying-peptide-drug-delivery-systems
#4
Janine Griesser, Gergely Hetényi, Michael Moser, Frédéric Demarne, Vincent Jannin, Andreas Bernkop-Schnürch
AIM: The aim of this study was the formation and characterization of various ion pairs of therapeutic peptides with different surfactants in order to reach a high payload in self-emulsifying drug delivering systems (SEDDS). METHODS: Hydrophobic ion pairs (HIP) were formed between the anionic surfactants sodium docusate, dodecylsulfate and oleate and the peptides leuprorelin (LEU), insulin (INS) and desmopressin (DES). The efficiency of HIP formation was evaluated by quantifying the amount of formed complexes, log P value determination in n-octanol/water via HPLC and zeta potential measurements...
February 7, 2017: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/28137696/storage-stability-of-bivalirudin-hydrophilic-vs-lipophilic-solutions
#5
Ožbej Zupančič, Julia Anita Grießinger, Hung Thanh Lam, Andreas Bernkop-Schnürch
It was the aim of this study to incorporate a model peptide bivalirudin in self-emulsifying drug delivery system (SEDDS) and compare its storage stability with conventional aqueous solutions. Firstly, bivalirudin lipophilicity was increased via hydrophobic ion pairing using anionic or cationic surfactants. The chosen bivalirudin docusate complex (BIV/AOT) was incorporated into SEDDS composed of 40% (w/w) Cremophor EL, 20% (w/w) Capmul PG-8 and 40% (w/w) propylene glycol with a drug payload of 0.20% (w/w). SEDDS were stable over a wide pH range for at least 7 days at 37 (0)C and showed an immediate bivalirudin release profile...
January 27, 2017: Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28024890/assessment-of-cell-viability-and-permeation-enhancement-in-presence-of-lipid-based-self-emulsifying-drug-delivery-systems-using-caco-2-cell-model-polysorbate-80-as-the-surfactant
#6
Pengli Bu, Yue Ji, Silpa Narayanan, Damon Dalrymple, Xingguo Cheng, Abu T M Serajuddin
PURPOSE: Lipid-based self-emulsifying drug delivery systems (SEDDS) are commonly used for solubilizing and enhancing oral bioavailability of poorly water-soluble drugs. However, their effects on viability of intestine epithelial cells and influence on membrane permeation are poorly understood. The present study was undertaken for safety assessment of lipid-based formulations containing medium-chain fatty acid esters as lipids and polysorbate 80 as the surfactant using the Caco-2 in vitro model...
March 1, 2017: European Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/27992953/age-related-disparities-in-trauma-center-access-for-severe-head-injuries-following-the-release-of-the-updated-field-triage-guidelines
#7
Thomas J Flottemesch, Susan Raetzman, Kevin C Heslin, Katie Fingar, Rosanna Coffey, Marguerite Barrett, Ernest Moy
OBJECTIVE: In 2006, the American College of Surgeons' Committee on Trauma and the Center for Disease Control released field triage guidelines with special consideration for older adults. Additional considerations for direct transport to a Level I or II trauma center (TC) were added in 2011, reflecting perceived undertriage to TCs for older adults. We examined whether age-based disparities in TC care for severe head injury decreased following introduction of the 2011 revisions. METHODS: A pre-post design analyzing the 2009 and 2012 Healthcare Cost and Utilization Project State Emergency Department Databases (SEDD) and State Inpatient Databases (SID) with multivariable logistic regressions considered changes in (1) the trauma designation of the emergency department where treatment was initiated and (2) transfer to a TC following initial treatment at a non-TC...
December 19, 2016: Academic Emergency Medicine: Official Journal of the Society for Academic Emergency Medicine
https://www.readbyqxmd.com/read/27910752/submicron-emulsions-and-their-applications-in-oral-delivery
#8
REVIEW
Veenu Mundada, Mitali Patel, Krutika Sawant
A "submicron emulsion" is an isotropic mixture of drug, lipids, and surfactants, usually with hydrophilic cosolvents and with droplet diameters ranging from 10 to 500 nm. Submicron emulsions are of increasing interest in medicine due to their kinetic stability, high solubilizing capacity, and tiny globule size. Because of these properties, they have been applied in various fields, such as personal care, cosmetics, health care, pharmaceuticals, and agrochemicals. Submicron emulsions are by far the most advanced nanoparticulate systems for the systemic delivery of biologically active agents for controlled drug delivery and targeting...
2016: Critical Reviews in Therapeutic Drug Carrier Systems
https://www.readbyqxmd.com/read/27907978/comparison-of-the-single-dose-pharmacokinetics-pharmacodynamics-and-safety-of-two-novel-oral-formulations-of-dimethandrolone-undecanoate-dmau-a-potential-oral-male-contraceptive
#9
R Ayoub, S T Page, R S Swerdloff, P Y Liu, J K Amory, A Leung, L Hull, D Blithe, A Christy, J H Chao, W J Bremner, C Wang
Dimethandrolone (DMA, 7α,11β-dimethyl-19-nortestosterone) has both androgenic and progestational activities, ideal properties for a male hormonal contraceptive. In vivo, dimethandrolone undecanoate (DMAU) is hydrolyzed to DMA. We showed previously that single oral doses of DMAU powder in capsule taken with food are well tolerated and effective at suppressing both LH and testosterone (T), but absorption was low. We compared the pharmacokinetics and pharmacodynamics of two new formulations of DMAU, in castor oil and in self-emulsifying drug delivery systems (SEDDS), with the previously tested powder formulation...
December 1, 2016: Andrology
https://www.readbyqxmd.com/read/27890596/monoacyl-phosphatidylcholine-inhibits-the-formation-of-lipid-multilamellar-structures-during-in-vitro-lipolysis-of-self-emulsifying-drug-delivery-systems
#10
Thuy Tran, Scheyla D V S Siqueira, Heinz Amenitsch, Thomas Rades, Anette Müllertz
The colloidal structures formed during lipolysis of self-emulsifying drug delivery systems (SEDDS) might affect the solubilisation and possibly the absorption of drugs. The aim of the current study is to elucidate the structures formed during the in vitro lipolysis of four SEDDS containing medium-chain glycerides and caprylocaproyl polyoxyl-8 glycerides (Labrasol), with or without monoacyl phosphatidylcholine (MAPC). In situ synchrotron small-angle X-ray scattering (SAXS) was combined with ex situ cryogenic transmission electron microscopy (cryo-TEM) and dynamic light scattering (DLS) to elucidate the generated structures...
November 24, 2016: European Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/27876599/self-emulsifying-drug-delivery-systems-sedds-proof-of-concept-how-to-make-them-mucoadhesive
#11
Gintare Leonaviciute, Nada Trivic Adamovic, Hung Thanh Lam, Julia Rohrer, Alexandra Partenhauser, Andreas Bernkop-Schnürch
AIM: The objective of this study was to provide a proof-of-concept that self-emulsifying drug delivery systems can be made mucoadhesive by the incorporation of hydrophobic mucoadhesive polymers. METHODS: In order to obtain such a hydrophobic mucoadhesive polymer, Eudragit® S100 was thiolated by covalent attachment of cysteamine. After determination of the thiol group content, in vitro mucoadhesion studies (rotating cylinder and rheological measurements) were performed...
November 19, 2016: European Journal of Pharmaceutics and Biopharmaceutics
https://www.readbyqxmd.com/read/27774912/development-of-self-emulsifying-formulations-of-poorly-soluble-naproxen-for-enhanced-drug-delivery
#12
Subhash Chandra Bose Penjuri, Saritha Damineni, Nagaraju Ravouru, Srikanth Reddy Poreddy Reddy Poreddy
BACKGROUND: The objective of this investigation was to develop a self emulsifying drug delivery system (SEDDS) of naproxen, a poorly water soluble drug, which could improve its solubility and oral bioavailability. Methoda: The recent patents on SEDDS of abiraterone acetate (WO2014/009434 A1) and tamoxifen (WO2013/0080083) helped in selecting the naproxen and excipients. Phase diagrams were constructed and the formulations were taken from the micro emulsion region. Formulations were subjected to thermodynamic stability, dispersibility and precipitation tests for optimization...
October 19, 2016: Recent Patents on Drug Delivery & Formulation
https://www.readbyqxmd.com/read/27693677/development-in-vitro-and-in-vivo-evaluation-of-a-self-emulsifying-drug-delivery-system-sedds-for-oral-enoxaparin-administration
#13
Ožbej Zupančič, Julia Anita Grieβinger, Julia Rohrer, Irene Pereira de Sousa, Lukas Danninger, Alexandra Partenhauser, Nadine Elli Sündermann, Flavia Laffleur, Andreas Bernkop-Schnürch
AIM: The aim of this study was to develop SEDDS for oral enoxaparin administration and evaluate it in vitro and in vivo. METHODS: The emulsifying properties of SEDDS composed of long chain lipids (LC-SEDDS), medium chain lipids (MC-SEDDS), short chain lipids (SC-SEDDS) and no lipids (NL-SEDDS) were evaluated. Thereafter, enoxaparin was incorporated via hydrophobic ion pairing in the chosen SEDDS, which were evaluated regarding their mucus permeating properties, stability towards pancreatic lipase, drug release profile and cytotoxicity...
December 2016: European Journal of Pharmaceutics and Biopharmaceutics
https://www.readbyqxmd.com/read/27685505/controversies-with-self-emulsifying-drug-delivery-system-from-pharmacokinetic-point-of-view
#14
Bappaditya Chatterjee, Samah Hamed Almurisi, Ather Ahmed Mahdi Dukhan, Uttam Kumar Mandal, Pinaki Sengupta
Self-emulsifying drug delivery system (SEDDS) is an isotropic mixture of lipid, surfactant and co-surfactant, which forms a fine emulsion when comes in contact of an aqueous medium with mild agitation. SEDDS is considered as a potential platform for oral delivery of hydrophobic drug in order to overcome their poor and irregular bioavailability challenges. In spite of fewer advantages like improved solubility of drug, bypassing lymphatic transport etc., SEDDS faces different controversial issues such as the use of appropriate terminology (self-microemulsifying drug delivery system; SMEDDS or self-nanoemulsifying drug delivery system; SNEDDS), presence of high amount of surfactant, correlation of in vitro model to in vivo studies, lack of human volunteer study and effect of conversion of SEDDS to final administrable dosage form on pharmacokinetic behavior of the drug...
November 2016: Drug Delivery
https://www.readbyqxmd.com/read/27615708/in-vivo-evaluation-of-lipid-based-formulations-for-oral-delivery-of-apomorphine-and-its-diester-prodrugs
#15
Nrupa Borkar, René Holm, Mingshi Yang, Anette Müllertz, Huiling Mu
In the present study, the differences in oral absorption of apomorphine and its diester prodrugs and the effect of lipid-based formulations on the absorption of apomorphine or its prodrugs were investigated. Apomorphine, dilauroyl apomorphine (DLA) and dipalmitoyl apomorphine (DPA) were orally administered (0.24mmol/kg) to rats as: DLA-o/w emulsion, DPA-o/w emulsion, apomorphine-o/w emulsion, apomorphine aqueous suspension, DLA-Maisine, DLA-soybean oil, DLA-self-emulsifying drug delivery systems (SEDDS), and DLA-w/o emulsion...
November 20, 2016: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/27608983/time-dependent-density-functional-theory-td-dft-coupled-with-reference-interaction-site-model-self-consistent-field-explicitly-including-spatial-electron-density-distribution-rism-scf-sedd
#16
D Yokogawa
Theoretical approach to design bright bio-imaging molecules is one of the most progressing ones. However, because of the system size and computational accuracy, the number of theoretical studies is limited to our knowledge. To overcome the difficulties, we developed a new method based on reference interaction site model self-consistent field explicitly including spatial electron density distribution and time-dependent density functional theory. We applied it to the calculation of indole and 5-cyanoindole at ground and excited states in gas and solution phases...
September 7, 2016: Journal of Chemical Physics
https://www.readbyqxmd.com/read/27329673/development-and-in-vitro-evaluation-of-zeta-potential-changing-self-emulsifying-drug-delivery-systems-for-enhanced-mucus-permeation
#17
Wongsakorn Suchaoin, Irene Pereira de Sousa, Kesinee Netsomboon, Hung Thanh Lam, Flavia Laffleur, Andreas Bernkop-Schnürch
The aim of this study was the development of zeta potential changing self-emulsifying drug delivery systems (SEDDS). Various cationic surfactants were incorporated into a formulation consisting of 30% Cremophor EL, 30% Capmul MCM, 30% Captex 355 and 10% propylene glycol (w/w). A substrate of intestinal alkaline phosphatase (IAP), 1,2-dipalmitoyl-sn-glycero-3-phosphatidic acid sodium (PA), was thereafter incorporated into SEDDS. Size, zeta potential and polydispersity index were determined. Phosphate release studies were performed using three different models, namely, isolated IAP, Caco-2 cell monolayer and rat intestinal mucosa and the amount of released phosphate was quantified by malachite green assay...
August 20, 2016: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/27279337/current-trends-in-self-emulsifying-drug-delivery-systems-seddss-to-enhance-the-bioavailability-of-poorly-water-soluble-drugs
#18
REVIEW
Rohit Karwal, Tarun Garg, Goutam Rath, Tanmay S Markandeywar
The main object of the self-emulsifying drug-delivery system (SEDDS) is oral bioavailability (BA) enhancement of a poorly water-soluble drug. Low aqueous solubility and low oral BA are major concerns for formulation scientists. As many drugs are lipophilic in nature, their lower solubility and dissolution are major drawbacks for their successful formulation into oral dosage forms. More than 60% of drugs have a lipophilic nature and exhibit poor aqueous solubility. Various strategies are reported in the literature to improve the solubility and enhance BA of lipophilic drugs, including the formation of a cyclodextrin complex, solid dispersions, and micronization...
2016: Critical Reviews in Therapeutic Drug Carrier Systems
https://www.readbyqxmd.com/read/27241877/formulation-optimization-of-docetaxel-loaded-self-emulsifying-drug-delivery-system-to-enhance-bioavailability-and-anti-tumor-activity
#19
Guru R Valicherla, Kandarp M Dave, Anees A Syed, Mohammed Riyazuddin, Anand P Gupta, Akhilesh Singh, Wahajuddin, Kalyan Mitra, Dipak Datta, Jiaur R Gayen
Poor bioavailability of Docetaxel (DCT) arising due to its low aqueous solubility and permeability limits its clinical utility. The aim of the present study was to develop DCT loaded self-emulsified drug delivery systems (D-SEDDS) and evaluate its potential ability to improve the oral bioavailability and therapeutic efficacy of DCT. D-SEDDS were characterized for their in vitro antitumor activity, in situ single pass intestinal perfusion (SPIP), bioavailability, chylomicron flow blocking study and bio-distribution profile...
2016: Scientific Reports
https://www.readbyqxmd.com/read/27230902/development-and-optimization-of-self-emulsifying-drug-delivery-systems-sedds-for-enhanced-dissolution-and-permeability-of-rosuvastatin
#20
H Y Karasulu, E Gündoğdu, T Turgay, U Ö Türk, S Apaydın, I Yildırım Şimşir, C Yilmaz, E Karasulu
Rosuvastatin calcium is commonly used statin for treatment of dyslipidemia. It has low bioavailability. The aim of this study was to develop new rosuvastatin calcium self-emulsifying drug delivery systems (SEDDS) as an alternative formulation and to evaluate the permeability of rosuvastatin calcium SEDDS by using Caco-2 cells. Rosuvastatin calcium SEDDSs were developed by using pseudo ternary phase diagram and characterized by using heating cooling cycle, robustness to dilution, stability and in vitro drug release and permeability...
2016: Current Drug Delivery
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