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https://www.readbyqxmd.com/read/29133172/measuring-the-emulsification-dynamics-and-stability-of-self-emulsifying-drug-delivery-systems
#1
Teófilo Vasconcelos, Sara Marques, Bruno Sarmento
Self-emulsifying drug delivery systems (SEDDS) are one of the most promising technologies in the drug delivery field, particularly for addressing solubility and bioavailability issues of drugs. The development of these drug carriers excessively relies in visual observations and indirect determinations. The present manuscript intended to describe a method able to measure the emulsification of SEDDS, both micro and nano-emulsions, able to measure the droplet size and to evaluate the physical stability of these formulations...
November 10, 2017: European Journal of Pharmaceutics and Biopharmaceutics
https://www.readbyqxmd.com/read/29105238/comparing-state-wide-and-single-center-data-to-predict-high-frequency-emergency-department-utilization-among-patients-with-asthma-exacerbation
#2
Margaret E Samuels-Kalow, Mohammad K Faridi, Janice A Espinola, Jean E Klig, Carlos A Camargo
BACKGROUND: Previous studies examining high-frequency ED utilization have primarily used single-center data, potentially leading to ascertainment bias if patients visit multiple centers. The goals of this study were (1) to create a predictive model to prospectively identify patients at risk of high-frequency ED utilization for asthma, and (2) to examine how that model differed using state-wide versus single-center data. METHODS: To track ED visits within a state, we analyzed 2011-2013 data from the New York State Healthcare Cost and Utilization Project (HCUP) State Emergency Department Databases (SEDD)...
November 4, 2017: Academic Emergency Medicine: Official Journal of the Society for Academic Emergency Medicine
https://www.readbyqxmd.com/read/29099779/self-emulsifying-granules-and-pellets-composition-and-formation-mechanisms-for-instant-or-controlled-release
#3
REVIEW
Ioannis Nikolakakis, Ioannis Partheniadis
Many articles have been published in the last two decades demonstrating improvement in the dissolution and absorption of low solubility drugs when formulated into self-emulsifying drug delivery systems (SEDDS). Several such pharmaceutical products have appeared in the market for medium dose (Neoral(®) for Cyclsoprin A, Kaletra(®) for Lopinavir and Ritonavir), or low dose medications (Rocaltrol(®) for Calcitriol and Avodart(®) for Dutasteride). However, these are in the form of viscous liquids or semisolid presentations, characterized by the disadvantages of high production cost, stability problems and the requirement of large quantities of surfactants...
November 3, 2017: Pharmaceutics
https://www.readbyqxmd.com/read/29080507/mucus-permeating-self-emulsifying-drug-delivery-systems-sedds-about-the-impact-of-mucolytic-enzymes
#4
Nuri Ari Efiana, Thi Nhu Quynh Phan, Arko Jatmiko Wicaksono, Andreas Bernkop-Schnürch
This study aimed to improve the mucus permeating properties of self-emulsifying drug delivery systems (SEDDS) by anchoring lipidized bromelain, papain and trypsin using palmitoyl chloride. SEDDS containing enzyme-palmitate conjugates were characterized regarding droplet size and zeta potential. Their mucus permeating properties were evaluated by Transwell diffusion and rotating tube method using fluorescein diacetate (FDA) as marker. Degree of substitution of modified enzymes was 35.3%, 47.8% and 38.5% for bromelain-palmitate, papain-palmitate and trypsin-palmitate, respectively...
October 23, 2017: Colloids and Surfaces. B, Biointerfaces
https://www.readbyqxmd.com/read/29079537/enzyme-decorated-drug-carriers-targeted-swords-to-cleave-and-overcome-the-mucus-barrier
#5
Claudia Menzel, Andreas Bernkop-Schnürch
The use of mucus permeating drug carrier systems being able to overcome the mucus barrier can lead to a remarkable enhancement in bioavailability. One promising approach is the design of mucolytic enzyme decorated carrier systems (MECS). These systems include micro- and nanoparticles as well as self-emulsifying drug delivery systems (SEDDS) decorated with mucin cleaving enzymes such as papain (PAP) or bromelain (BRO). MECS are able to cross the mucus barrier in a comparatively efficient manner by cleaving mucus substructures in front of them on their way to the epithelium...
October 24, 2017: Advanced Drug Delivery Reviews
https://www.readbyqxmd.com/read/29043863/preparation-and-evaluation-of-vinpocetine-self-emulsifying-ph-gradient-release-pellets
#6
Mengqi Liu, Shiming Zhang, Shuxia Cui, Fen Chen, Lianqun Jia, Shu Wang, Xiumei Gai, Pingfei Li, Feifei Yang, Weisan Pan, Xinggang Yang
The main objective of this study was to develop a pH gradient release pellet with self-emulsifying drug delivery system (SEDDS), which could not only improve the oral bioavailability of Vinpocetine (VIN), a poor soluble drug, but reduce the fluctuation of plasma concentration. First, the liquid VIN SEDDS formulation was prepared. Then the self-emulsifying pH gradient release pellets were prepared by extrusion spheronization technique, and formulation consisted by the liquid SEDDS, absorbent (colloidal silicon dioxide), penetration enhancer (sodium chloride), microcrystalline cellulose, ethyl alcohol, and three coating materials (HPMC, Eudragit L30D55, Eudragit FS30D) were eventually selected...
November 2017: Drug Delivery
https://www.readbyqxmd.com/read/28957774/effect-of-inorganic-mesoporous-carriers-on-1-palmitoyl-2-linoleoyl-3-acetyl-rac-glycerol-loaded-solid-self-emulsifying-drug-delivery-system-physicochemical-characterization-and-bioavailability-in-rats
#7
Dong Shik Kim, Eun Su Yang, Chul Soon Yong, Yu Seok Youn, Kyung Taek Oh, Dong Xun Li, Jong Oh Kim, Sung Giu Jin, Han-Gon Choi
The purpose of this study was to assess the impact of inorganic mesoporous carriers on the physicochemical properties and oral bioavailability of 1-palmitoyl-2-linoleoyl-3-acetyl-rac-glycerol (PLAG)-loaded solid self-emulsifying drug delivery system (solid SEDDS). Numerous PLAG-loaded solid SEDDS formulations were prepared by spray drying technique with sodium laurylsulfate (SLS), butylated hydroxyanisole (BHA) and inorganic mesoporous materials as a surfactant, antioxidant and solid carrier, respectively. The mesoporous materials, such as calcium silicate, silicon dioxide and magnesium aluminosilicate were used as the solid carriers...
September 19, 2017: Colloids and Surfaces. B, Biointerfaces
https://www.readbyqxmd.com/read/28954512/ionic-liquid-forms-of-weakly-acidic-drugs-in-oral-lipid-formulations-preparation-characterization-in-vitro-digestion-and-in-vivo-absorption-studies
#8
Yasemin Sahbaz, Tri-Hung Nguyen, Leigh Ford, Claire L McEvoy, Hywel D Williams, Peter J Scammells, Christopher J H Porter
This study aimed to transform weakly acidic poorly water-soluble drugs (PWSD) into ionic liquids (ILs) to promote solubility in, and the utility of, lipid-based formulations. Ionic liquids (ILs) were formed directly from tolfenamic acid (Tolf), meclofenamic acid, diclofenac, and ibuprofen by pairing with lipophilic counterions. The drug-ILs were obtained as liquids or low melting solids and were significantly more soluble (either completely miscible or highly soluble) in lipid based, self-emulsifying drug delivery systems (SEDDS) when compared to the equivalent free acid...
November 6, 2017: Molecular Pharmaceutics
https://www.readbyqxmd.com/read/28782582/development-and-in-vitro-characterization-of-a-papain-loaded-mucolytic-self-emulsifying-drug-delivery-system-sedds
#9
Christina Leichner, Claudia Menzel, Flavia Laffleur, Andreas Bernkop-Schnürch
The aim of the study was to create a self-emulsifying drug delivery system (SEDDS) with mucolytic properties based on incorporated papain for improved mucus permeation. In order to increase the lipophilicity of the enzyme and to dissolve it in SEDDS, hydrophobic ion pairing with sodium deoxycholate in a molar ratio of 20:1 (surfactant: enzyme) was performed. The yield of precipitated papain was 86.8±2.7% and the ion pair was loaded into the formulations to 1% (m/m). Suitable formulations were chosen according to their properties to dissolve the ion pair and characterized regarding droplet size and polydispersity index...
August 3, 2017: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/28684278/zeta-potential-changing-self-emulsifying-drug-delivery-systems-containing-phosphorylated-polysaccharides
#10
Janine Griesser, Stephanie Burtscher, Saskia Köllner, Isabelle Nardin, Felix Prüfert, Andreas Bernkop-Schnürch
AIM: The aim of the study was to develop novel zeta potential changing self-emulsifying drug delivery systems (SEDDS) containing phosphorylated polysaccharides. METHODS: Starch and hydroxypropyl starch (HPS) were phosphorylated by utilizing phosphorus pentoxide. The modified starches, starch phosphate (SP) and hydroxypropyl starch phosphate (HPSP), were loaded into SEDDS and investigated regarding particle size, zeta potential, stability and cell viability. The release of immobilized phosphate by intestinal alkaline phosphatase (IAP) was analyzed via malachite green assay...
October 2017: European Journal of Pharmaceutics and Biopharmaceutics
https://www.readbyqxmd.com/read/28589736/development-and-in-vitro-characterization-of-self-emulsifying-drug-delivery-system-sedds-for-oral-opioid-peptide-delivery
#11
Ožbej Zupančič, Julia Rohrer, Hung Thanh Lam, Julia Anita Grießinger, Andreas Bernkop-Schnürch
AIM: In this study, self-emulsifying drug delivery system (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...
October 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
#12
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
#13
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
#14
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...
November 30, 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
#15
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...
November 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
#16
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
#17
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
#18
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
#19
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
#20
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
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