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https://www.readbyqxmd.com/read/28493003/bio-shielding-in-situ-forming-gels-bsifg-loaded-with-lipospheres-for-depot-injection-of-quetiapine-fumarate-in-vitro-and-in-vivo-evaluation
#1
Mustafa M Abo Elela, Nermeen A ElKasabgy, Emad B Basalious
Quetiapine fumarate (QF), an anti-schizophrenic drug, suffers from rapid elimination and poor bioavailability due to extensive first-pass effect. Intramuscularly (IM) injected lipospheres were designed to enhance the drug's bioavailability and extend its release. A central composite design was applied to optimize the liposphere preparation by a melt dispersion technique using Compritol® 888 ATO or glyceryl tristearate as lipid component and polyvinyl alcohol as surfactant. Lipospheres were evaluated for their particle size, entrapment efficiency, and in vitro release...
May 10, 2017: AAPS PharmSciTech
https://www.readbyqxmd.com/read/28156176/respirable-controlled-release-polymeric-colloid-rcrpc-of-bosentan-for-the-management-of-pulmonary-hypertension-in-vitro-aerosolization-histological-examination-and-in-vivo-pulmonary-absorption
#2
COMPARATIVE STUDY
Lydia A Hanna, Emad B Basalious, Omaima N ELGazayerly
Bosentan is an endothelin receptor antagonist (ERA) prescribed for patients with pulmonary arterial hypertension (PAH). The oral delivery of bosentan possesses several drawbacks such as low bioavailability (about 50%), short duration of action, frequent administration, hepatotoxicity and systemic hypotension. The pulmonary administration would circumvent the pre-systemic metabolism thus improving the bioavailability and avoids the systemic adverse effects of oral bosentan. However, the short duration of action and the frequent administration are the major drawbacks of inhalation therapy...
November 2016: Drug Delivery
https://www.readbyqxmd.com/read/28156162/contribution-of-both-olfactory-and-systemic-pathways-for-brain-targeting-of-nimodipine-loaded-lipo-pluronics-micelles-in-vitro-characterization-and-in-vivo-biodistribution-study-after-intranasal-and-intravenous-delivery
#3
COMPARATIVE STUDY
Hassan M Rashed, Rehab N Shamma, Emad B Basalious
Nimodipine (NM) is the only FDA-approved drug for treating subarachnoid hemorrhage induced vasospasm. NM has poor oral bioavailability (5-13%) due to its low aqueous solubility, and extensive first pass metabolism. The objective of this study is to develop radiolabeled NM-loaded LPM and to test its ability prolong its circulation time, reduce its frequency of administration and eventually target it to the brain tissue. NM was radiolabeled with (99m)Tc by direct labeling method using sodium dithionite. Different reaction conditions that affect the radiolabeling yield were studied...
November 2016: Drug Delivery
https://www.readbyqxmd.com/read/27322631/quantification-of-sofosbuvir-and-ledipasvir-in-human-plasma-by-uplc-ms-ms-method-application-to-fasting-and-fed-bioequivalence-studies
#4
Mamdouh R Rezk, Ehab R Bendas, Emad B Basalious, Iman A Karim
A rapid and sensitive LC-MS/MS method was developed, optimized and validated for quantification of sofosbuvir (SF) and ledipasvir (LD) in human plasma using eplerenone as an internal standard (IS). Analytes and IS were extracted from plasma by simple liquid-liquid extraction technique using methyl tertiary butyl ether. The prepared samples were chromatographed on Acquity UPLC BEH C18 column. Separation was done using a mobile phase formed of 0.1% formic acid and acetonitrile (50:50, v/v) in an isocratic mode at a flow rate of 0...
August 15, 2016: Journal of Chromatography. B, Analytical Technologies in the Biomedical and Life Sciences
https://www.readbyqxmd.com/read/27232152/development-and-validation-of-sensitive-and-rapid-uplc-ms-ms-method-for-quantitative-determination-of-daclatasvir-in-human-plasma-application-to-a-bioequivalence-study
#5
Mamdouh R Rezk, Ehab R Bendas, Emad B Basalious, Iman A Karim
A rapid and sensitive UPLC-MS/MS method was developed and validated for determination of daclatasvir (DAC) in human plasma using sofosbuvir (SOF) as an internal standard (IS). The Xevo TQD LC-MS/MS was operated under the multiple-reaction monitoring mode using electrospray ionization. Precipitation with acetonitrile was used in sample preparation. The prepared samples were chromatographed on Acquity UPLC HSS C18 (50×2.1mm, 1.8μm) column by pumping 10mM ammonium formate (pH 3.5) and acetonitrile in an isocratic mode at a flow rate of 0...
September 5, 2016: Journal of Pharmaceutical and Biomedical Analysis
https://www.readbyqxmd.com/read/27132526/neuromodulation-for-restoring-memory
#6
REVIEW
Sarah K B Bick, Emad N Eskandar
Disorders of learning and memory have a large social and economic impact in today's society. Unfortunately, existing medical treatments have shown limited clinical efficacy or potential for modification of the disease course. Deep brain stimulation is a successful treatment for movement disorders and has shown promise in a variety of other diseases including psychiatric disorders. The authors review the potential of neuromodulation for the treatment of disorders of learning and memory. They briefly discuss learning circuitry and its involvement in Alzheimer disease and traumatic brain injury...
May 2016: Neurosurgical Focus
https://www.readbyqxmd.com/read/27063851/novel-instantly-soluble-transmucosal-matrix-istm-using-dual-mechanism-solubilizer-for-sublingual-and-nasal-delivery-of-dapoxetine-hydrochloride-in-vitro-in-vivo-evaluation
#7
COMPARATIVE STUDY
Shahinaze A Fouad, Rehab N Shamma, Emad B Basalious, Mohamed A El-Nabarawi, Saadia A Tayel
Dapoxetine (D) suffers from poor oral bioavailability (42%) due to extensive first pass metabolism. The usefulness of transmucosal (sublingual and intranasal) drug delivery to improve bioavailability of D, a weak basic drug, has been hampered by its poor solubility in the neutral pH of the body fluids. In this study, instantly-soluble transmucosal matrices (ISTMs) of D, containing dual mechanism solubilizer (Pluronic F-127/citric acid mixture), were prepared by lyophilization technique to enhance matrix disintegration, dissolution and transmucosal permeation...
May 30, 2016: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/26821881/novel-and-sensitive-uplc-ms-ms-method-for-quantification-of-sofosbuvir-in-human-plasma-application-to-a-bioequivalence-study
#8
Mamdouh R Rezk, Emad B Basalious, Mohammed E Amin
A novel and sensitive LC-MS/MS method was developed and validated for determination of sofosbuvir (SF) using eplerenone as an internal standard. The Xevo TQD LC-MS/MS was operated under the multiple-reaction monitoring mode using electrospray ionization. Extraction with tert-butyl methyl ether was used in sample preparation. The prepared samples were chromatographed on Acquity UPLC BEH C18 (50 × 2.1 mm, 1.7 μm) column by pumping 0.1% formic acid and acetonitrile in an isocratic mode at a flow rate of 0...
September 2016: Biomedical Chromatography: BMC
https://www.readbyqxmd.com/read/26241752/novel-self-assembled-nano-tubular-mixed-micelles-of-pluronics-p123-pluronic-f127-and-phosphatidylcholine-for-oral-delivery-of-nimodipine-in-vitro-characterization-ex-vivo-transport-and-in-vivo-pharmacokinetic-studies
#9
Emad B Basalious, Rehab N Shamma
Subarachnoid hemorrhage (SAH) is a major cause of death in patients suffering from stroke. Nimodipine (NM) is the only FDA-approved drug for treating SAH-induced vasospasm. However, NM suffers from poor oral bioavailability (5-13%) due to its low aqueous solubility, extensive first pass metabolism and short elimination half-life (1-2h). The objective of this study was to develop NM-loaded Pluronic/phosphatidylcholine/polysorbate 80 mixed micelles (PPPMM) that can solubilize NM in aqueous media even after dilution, prolong its circulation time, improve its bioavailability and eventually help in targeting it to the brain tissue...
September 30, 2015: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/26086847/bioenhanced-sublingual-tablet-of-drug-with-limited-permeability-using-novel-surfactant-binder-and-microencapsulated-polysorbate-in-vitro-in-vivo-evaluation
#10
Doaa Ahmed El-Setouhy, Emad B Basalious, Nevine Shawky Abdelmalak
Formulation of sublingual tablets of drugs with limited permeability poses a great challenge due to their poor absorption. In this study, bioenhanced sublingual tablets (BESTs) of zolmitriptan were prepared using novel surfactant binder (Pluronic® p123/Syloid® mixture) to enhance tablet disintegration and dissolution. Microencapsulated polysorbate 80 (Sepitrap™ 80) were included in the composition of BESTs to enhance the drug transport through the sublingual mucosa. Tablets were evaluated for in vitro/in vivo disintegration, in vitro dissolution and ex vivo permeation...
August 2015: European Journal of Pharmaceutics and Biopharmaceutics
https://www.readbyqxmd.com/read/26037157/development-of-a-sensitive-uplc-esi-ms-ms-method-for-quantification-of-sofosbuvir-and-its-metabolite-gs-331007-in-human-plasma-application-to-a-bioequivalence-study
#11
Mamdouh R Rezk, Emad B Basalious, Iman A Karim
A rapid and simple LC-MS/MS method was developed and validated for the simultaneous estimation of sofosbuvir (SF) and its metabolite GS-331007 (GS) using famotidine as an internal standard (IS). The Xevo TQD LC-MS/MS was operated under the multiple-reaction monitoring mode using electrospray ionization. Extraction with ethyl acetate was used in sample preparation. The prepared samples were chromatographed on Acquity UPLC HSS C₁₈ (50 mm × 2.1 mm, 1.8 μm) column by pumping 0.1% formic acid and acetonitrile (50:50, v/v) in an isocratic mode at a flow rate of 0...
October 10, 2015: Journal of Pharmaceutical and Biomedical Analysis
https://www.readbyqxmd.com/read/26002566/novel-self-nanoemulsifying-self-nanosuspension-snesns-for-enhancing-oral-bioavailability-of-diacerein-simultaneous-portal-blood-absorption-and-lymphatic-delivery
#12
Hanan M El-Laithy, Emad B Basalious, Boushra M El-Hoseiny, Maha M Adel
The application of self-nanoemulsified drug delivery system (SNEDDS) to improve bioavailability of diacerein (D) has been hampered by its large dose and limited solubility. This work aimed to prepare diacerein loaded self nanoemulsifying self nanosuspension (D-SNESNS) containing high drug load. D-SNESNS was prepared by homogenizing D into Maisine™-based SNEDDS that gave the highest drug solubility. D-SNESNS was evaluated for particle size, zeta potential and in vitro dissolution. Significant increase of D solubility was observed from D-SNESNS (∼ 309 μg/mL) than traditional SNEDDS (∼162μg/mL) due to the spontaneous simultaneous formation of nanoemulsion and nanosuspension (top-down approach)...
July 25, 2015: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/25567033/rapidly-disintegrating-vagina-retentive-cream-suppositories-of-progesterone-development-patient-satisfaction-and-in-vitro-in-vivo-studies
#13
RANDOMIZED CONTROLLED TRIAL
Ehab Rasmy Bendas, Emad B Basalious
Our objective was to develop novel vagina retentive cream suppositories (VRCS) of progesterone having rapid disintegration and good vaginal retention. VRCS of progesterone were prepared using oil in water (o/w) emulsion of mineral oil or theobroma oil in hard fat and compared with conventional vaginal suppositories (CVS) prepared by hard fat. VRCS formulations were tested for content uniformity, disintegration, melting range, in vitro release and stability studies. The most stable formulation (VRCS I) was subjected to scaling-up manufacturing and patients' satisfaction test...
2016: Pharmaceutical Development and Technology
https://www.readbyqxmd.com/read/23792042/microemulsion-and-poloxamer-microemulsion-based-gel-for-sustained-transdermal-delivery-of-diclofenac-epolamine-using-in-skin-drug-depot-in-vitro-in-vivo-evaluation
#14
Shahinaze A Fouad, Emad B Basalious, Mohamed A El-Nabarawi, Saadia A Tayel
Microemulsion (ME) and poloxamer microemulsion-based gel (PMBG) were developed and optimized to enhance transport of diclofenac epolamine (DE) into the skin forming in-skin drug depot for sustained transdermal delivery of drug. D-optimal mixture experimental design was applied to optimize ME that contains maximum amount of oil, minimum globule size and optimum drug solubility. Three formulation variables; the oil phase X1 (Capryol(®)), Smix X2 (a mixture of Labrasol(®)/Transcutol(®), 1:2 w/w) and water X3 were included in the design...
September 10, 2013: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/22339303/rapidly-absorbed-orodispersible-tablet-containing-molecularly-dispersed-felodipine-for-management-of-hypertensive-crisis-development-optimization-and-in-vitro-in-vivo-studies
#15
RANDOMIZED CONTROLLED TRIAL
Emad B Basalious, Wessam El-Sebaie, Omaima El-Gazayerly
A liquisolid orodispersible tablet of felodipine, a BCS Class II drug, was developed to improve drug dissolution and absorption through the buccal mucosa for management of hypertensive crisis. A 24 full-factorial design was applied to optimize felodipine liquisolid systems (FLSs) having acceptable flow properties and possessing enhanced drug dissolution rates. Four formulation variables; The liquid type, X1 (PG or PEG), drug concentration, X2 (10% and 20%), type of coat, X3 (Aerosil® and Aeroperl®) and excipients ratio, X4 (10 and 20) were included in the design...
March 2013: Pharmaceutical Development and Technology
https://www.readbyqxmd.com/read/21770719/development-of-novel-sustained-release-matrix-pellets-of-betahistine-dihydrochloride-effect-of-lipophilic-surfactants-and-co-surfactants
#16
Rehab Nabil Shamma, Emad B Basalious, Raguia Shoukri
Sustained release matrix pellets of the freely water soluble drug, betahistine dihydrochloride (BH), were prepared using freeze pelletization technique. Different waxes and lipids (cetyl alcohol, beeswax, glyceryl tripalmitate (GTP) and glyceryl tristearate) were evaluated for the preparation of matrix pellets. A D-optimal design was employed for the optimization and to explore the effect of drug loading (X(1)), concentration of lipophilic surfactant (X(2)), concentration of co-surfactant (X(3)) and wax type (X(4)) on the release extent of the drug from matrix pellets...
September 2012: Pharmaceutical Development and Technology
https://www.readbyqxmd.com/read/21701960/application-of-pharmaceutical-qbd-for-enhancement-of-the-solubility-and-dissolution-of-a-class-ii-bcs-drug-using-polymeric-surfactants-and-crystallization-inhibitors-development-of-controlled-release-tablets
#17
Emad B Basalious, Wessam El-Sebaie, Omaima El-Gazayerly
The aim of this study was to apply quality by design (QbD) for pharmaceutical development of felodipine solid mixture (FSM) containing hydrophilic carriers and/or polymeric surfactants, for easier development of controlled-release tablets of felodipine. The material attributes, the process parameters (CPP), and the critical quality attributes of the FSMs were identified. Box-Behnken experimental design was applied to develop space design and determine the control space of FSMs that have maximum solubility, maximum dissolution, and ability to inhibit felodipine crystallization from supersaturated solution...
September 2011: AAPS PharmSciTech
https://www.readbyqxmd.com/read/21145958/development-and-optimization-of-a-multiple-unit-controlled-release-formulation-of-a-freely-water-soluble-drug-for-once-daily-administration
#18
Rehab N Shamma, Emad B Basalious, Raguia A Shoukri
A controlled release resinate beads of betahistine diHCl (BHCl), a short half-life freely water soluble drug, was developed to allow once-daily administration to improve patient compliance and eliminate the risk of intolerance of the drug. BHCl-resin complex was subsequently coated with Eudragit RS100. A 2(4) full factorial design was employed for optimization and to explore the effect of Eudragit RS100 concentration in the coating solution (X(1)), the coating percentage (X(2)), the speed of rotation (X(3)) and the concentration of plasticizer (PEG 400) (X(4)) on the release rate of the drug from the microcapsules...
February 28, 2011: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/20532709/optimization-and-in-vivo-pharmacokinetic-study-of-a-novel-controlled-release-venlafaxine-hydrochloride-three-layer-tablet
#19
RANDOMIZED CONTROLLED TRIAL
Ahmed A Aboelwafa, Emad B Basalious
Several matrix tablet formulations (hydrophilic-based, wax-based, and three-layer tablets) were designed for controlling the release of the highly water soluble drug, venlafaxine hydrochloride (VenHCl) for once-daily administration. The three-layer tablets consist of non-swellable, compritol-based middle layers containing the drug to which hydrophilic top and bottom barrier layers were applied. A 2(3) full-factorial design was employed for optimization and to explore the effect of different variables on the release rate of the drug from the three-layer tablets...
September 2010: AAPS PharmSciTech
https://www.readbyqxmd.com/read/20214965/snedds-containing-bioenhancers-for-improvement-of-dissolution-and-oral-absorption-of-lacidipine-i-development-and-optimization
#20
Emad B Basalious, Nevine Shawky, Shaimaa M Badr-Eldin
The aim of this study was to develop and optimize SNEDDS formulations containing surfactants reported to be bioenhancers for improvement of dissolution and oral absorption of lacidipine (LCDP). Preliminary screening was carried out to select proper components combination. D-optimal mixture experimental design was applied to optimize a SNEDDS that contains a minimum amount of surfactant, a maximum amount of lipid, and possesses enhanced emulsification and dissolution rates. Three formulation variables; the oil phase X(1) (a mixture of Labrafil/Capmul), the surfactant X(2) (a mixture of Cremophor/Tween 80) and the co-surfactant X(3), were included in the design...
May 31, 2010: International Journal of Pharmaceutics
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