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https://www.readbyqxmd.com/read/29754485/supersaturable-self-emulsifying-drug-delivery-system-of-krill-oil-with-improved-oral-absorption-and-hypotriglyceridemic-function
#1
Yoshiki Seto, Chikara Morizane, Kodai Ueno, Hideyuki Sato, Satomi Onoue
This study aimed to develop a supersaturable self-emulsifying drug delivery system (S-SEDDS) of krill oil (KO), a rich source of docosahexaenoic acid and eicosapentaenoic acid (EPA), to improve its hypotriglyceridemic function. S-SEDDS of KO (KO/S-SEDDS) was prepared by the addition of lysolecithin, glycerin, and hydroxypropyl methylcellulose (HPMC). SEDDS of KO (KO/SEDDS) and KO with HPMC (KO/HPMC) were also prepared for comparison purposes. The physicochemical and pharmacokinetic properties of KO samples were characterized, and the hypotriglyceridemic function of KO/S-SEDDS was evaluated...
May 14, 2018: Journal of Agricultural and Food Chemistry
https://www.readbyqxmd.com/read/29717664/lipids-and-surfactants-the-inside-story-of-lipid-based-drug-delivery-systems
#2
Vikas Pandey, Seema Kohli
In the bioavailability enhancement of poorly aqueous soluble drugs, self-emulsifying/microemulsifying drug delivery systems (SEDDS/SMEDDS) are isotropic mixtures of oils, surfactants, solvents, and cosolvents/surfactants that have gained immense popularity because of their self-emulsification ability. This characteristic relies on some critical parameters such as surfactant concentration, oil-to-surfactant ratio, polarity of the emulsion, droplet size and charge, which are acquired from an amalgamation of appropriate excipients...
2018: Critical Reviews in Therapeutic Drug Carrier Systems
https://www.readbyqxmd.com/read/29627681/role-of-self-emulsifying-drug-delivery-systems-in-optimizing-the-oral-delivery-of-hydrophilic-macromolecules-and-reducing-interindividual-variability
#3
REVIEW
Khaled AboulFotouh, Ayat A Allam, Mahmoud El-Badry, Ahmed M El-Sayed
Self-emulsifying drug delivery systems (SEDDS) have been widely employed to improve the oral bioavailability of poorly soluble drugs. In the past few years, SEDDS were extensively investigated to overcome various barriers encountered in the oral delivery of hydrophilic macromolecules (e.g., protein/peptide therapeutics and plasmid DNA (pDNA)), as well as in lowering the effect of food on drugs' bioavailability. However, the main mechanism(s) by which SEDDS could achieve such promising effects remains not fully understood...
March 26, 2018: Colloids and Surfaces. B, Biointerfaces
https://www.readbyqxmd.com/read/29574041/in-vivo-evaluation-of-an-oral-self-emulsifying-drug-delivery-system-sedds-for-exenatide
#4
Claudia Menzel, Thomas Holzeisen, Flavia Laffleur, Sergey Zaichik, Muthanna Abdulkarim, Mark Gumbleton, Andreas Bernkop-Schnürch
BACKGROUND: The aim of the study was to develop an oral self-emulsifying drug delivery system (SEDDS) for exenatide and to evaluate its in vivo efficacy. METHODS: Exenatide was lipidised via hydrophobic ion pairing with sodium docusate (DOC) and incorporated in SEDDS consisting of 35% Cremophor EL, 25% Labrafil 1944, 30% Capmul-PG 8 and 10% propylene glycol. Exenatide/DOC was characterized in terms of lipophilicity evaluating the octanol/water phase distribution (logP)...
March 21, 2018: Journal of Controlled Release: Official Journal of the Controlled Release Society
https://www.readbyqxmd.com/read/29525534/the-evaluation-of-three-comorbidity-indices-in-predicting-postoperative-complications-and-readmissions-in-pediatric-urology
#5
Ruiyang Jiang, Steven Wolf, Muhammad H Alkazemi, Gina-Maria Pomann, J Todd Purves, John S Wiener, Jonathan C Routh
INTRODUCTION: The surgical comorbidity assessment is important for patient risk stratification, counseling, and research. In adults, risk assessment indices, such as the Charlson Co-morbidity Score (CCS) or Van Walraven Index (VWI), are well established. In pediatrics, however, risk assessment indices are scarce. Recently, a pediatric-specific risk assessment index, the Rhee index, was developed to discriminate mortality for pediatric general surgery patients. Currently, there is no validated risk assessment tool in pediatric urology...
February 26, 2018: Journal of Pediatric Urology
https://www.readbyqxmd.com/read/29488425/amikacin-containing-self-emulsifying-delivery-systems-via-pulmonary-administration-for-treatment-of-bacterial-infections-of-cystic-fibrosis-patients
#6
Gergely Hetényi, Janine Griesser, Simon Fontana, Anja Martinez Gutierrez, Helmut Ellemunter, Katharina Niedermayr, Péter Szabó, Andreas Bernkop-Schnürch
AIM: The aim of the study was to develop self-emulsifying delivery systems (SEDDS) exhibiting improved permeation rate for pulmonary delivery of amikacin for treatment of cystic fibrosis (CF) patients. MATERIALS & METHODS: Solubility of amikacin in lipids was improved by hydrophobic ion pairing with sodium myristyl sulfate. The complex was loaded into SEDDS. Drug-release studies were performed and the permeation properties of SEDDS through human CF mucus were examined...
April 1, 2018: Nanomedicine
https://www.readbyqxmd.com/read/29484996/enhancing-solubility-and-bioavailability-of-rosuvastatin-into-self-emulsifying-drug-delivery-system
#7
Hatice Yesim Karasulu, E Gundogdu, U O Turk, T Turgay, S Apaydın, I Yildırım Simsir, C Yılmaz, E Karasulu
The aim of this study was to develop new Rosuvastatin calcium (RCa) self emulsifying drug delivery system (SEDDS) and to evaluate the bioavailability and pharmacodynamic effect of RCa-SEDDS in Yorkshire pigs. Firstly, SEDDS was developed and prepared then RCa was incorporated into SEDDS which was evaluated regarding their characterization, stability properties, drug release profiles, permeation and cytotoxicity studies. Finally, in vivo performance of RCa-SEDDS (F1-RCa-SEDDS) was examined by pharmacokinetic and pharmacodynamics studies...
February 25, 2018: Current Drug Delivery
https://www.readbyqxmd.com/read/29458206/mucoadhesive-self-emulsifying-delivery-systems-for-ocular-administration-of-econazole
#8
Ibrahim A Elbahwy, Noemi Lupo, Hany M Ibrahim, Hatem R Ismael, Alaa A Kasem, Cagri Caliskan, Barbara Matuszczak, Andreas Bernkop-Schnürch
AIM: Development of mucoadhesive self-emulsifying drug delivery systems (SEDDS) providing a prolonged ocular residence time for poorly soluble active pharmaceutical ingredient. METHODS: l-Cysteine was covalently linked to 6-mercaptonicotinamide. The obtained ligand, Cysteine-6-mercaptonicotinamide (Cys-6-MNA) was attached to Eudragit® L100-55 via a carbodiimide mediated amide bond formation. The resulting entirely S-protected thiolated Eudragit® L100-55 was characterized regarding the degree of modification as well as stability toward oxidation in the presence of strong oxidizing agent (H2 O2 )...
April 25, 2018: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/29455137/can-the-watershed-non-point-phosphorus-pollution-be-interpreted-by-critical-soil-properties-a-new-insight-of-different-soil-p-states
#9
Chen Lin, Ronghua Ma, Junfeng Xiong
The physicochemical properties of surface soil play a key role in the fate of watershed non-point source pollution. Special emphasis is needed to identify soil properties that are sensitive to both particulate P (PP) pollution and dissolved P (DP) pollution, which is essential for watershed environmental management. The Chaohu Lake basin, a typical eutrophic lake in China, was selected as the study site. The spatial features of the Non-point Source (NPS) PP loads and DP loads were calculated simultaneously based on the integration of sediment delivery distributed model (SEDD) and pollution loads (PLOAD) model...
July 1, 2018: Science of the Total Environment
https://www.readbyqxmd.com/read/29414123/development-of-a-new-class-of-sulforaphane-enabled-self-emulsifying-drug-delivery-systems-sfn-sedds-by-high-throughput-screening-a-case-study-with-curcumin
#10
Mohammad M Kamal, Sami Nazzal
Self-emulsifying drug delivery systems (SEDDS) have been used as a formulation strategy to overcome the challenges in formulating poorly water soluble drugs. The objective of the present study was to report on the solubilizing capacity of sulforaphane (SFN) and its utilization to formulate SEDDS of poorly water soluble drugs. A set of 24 drugs was tested for their solubility in SFN of which Cyclosporine A, Celecoxib, Paclitaxel, Docetaxel, and Curcumin were selected for subsequent SEDDS formulation development utilizing SFN as common solubilizer...
March 25, 2018: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/29355620/impact-of-different-hydrophobic-ion-pairs-of-octreotide-on-its-oral-bioavailability-in-pigs
#11
Sonja Bonengel, Max Jelkmann, Muthanna Abdulkarim, Mark Gumbleton, Vera Reinstadler, Herbert Oberacher, Felix Prüfert, Andreas Bernkop-Schnürch
The objective of this study was to investigate the impact of different hydrophobic ion pairs (HIP) on the oral bioavailability of the model drug octreotide in pigs. Octreotide was ion paired with the anionic surfactants deoxycholate, decanoate and docusate differing in lipophilicity. These hydrophobic ion pairs were incorporated in self-emulsifying drug delivery systems (SEDDS) based on BrijO10, octyldodecanol, propylene glycol and ethanol in a concentration of 5mg/ml. SEDDS were characterized regarding size distribution, zeta potential, stability towards lipase, log DSEDDS/release medium and mucus diffusion behavior...
March 10, 2018: Journal of Controlled Release: Official Journal of the Controlled Release Society
https://www.readbyqxmd.com/read/29339247/self-emulsifying-peptide-drug-delivery-systems-how-to-make-them-highly-mucus-permeating
#12
Janine Griesser, Gergely Hetényi, Hatice Kadas, Frédéric Demarne, Vincent Jannin, Andreas Bernkop-Schnürch
AIM: It was the aim of this study to evaluate the mucus permeating properties of self-emulsifying drug delivery systems (SEDDS) exhibiting different size and zeta potential. METHODS: Various SEDDS were prepared and characterized regarding droplet size, zeta potential and stability. Desmopressin was incorporated as model peptide drug and log P (SEDDS/water) was determined. Thereafter, mucus permeation studies with freshly isolated porcine mucus via Transwell method were performed...
March 1, 2018: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/29336263/in-vitro-methods-for-in-vitro-in-vivo-correlation-ivivc-for-poorly-water-soluble-drugs-lipid-based-formulation-perspective
#13
Mohsin Kazi, Rayan Rayan Al Amri, Fars K Alanazi, Muhammad Delwar Hussain
A great number of new drug candidates identified from the discovery pipeline are poorly water soluble, which is a drawback to bring such candidates into the pharmaceutical market. Formulating these compounds as self-emulsifying/microemulsifying/ nanoemulsifying drug delivery systems (SEDDS/SMEDDS/SNEDDS) within lipid based formulations is of growing interests. Some of the recent studies have resulted in commercial products that provided improved bioavailability and dissolution due to the better dispersion properties of SEDDS/SMEDDS/SNEDDS...
January 15, 2018: Current Drug Delivery
https://www.readbyqxmd.com/read/29317226/oral-delivery-of-highly-lipophilic-poorly-water-soluble-drugs-self-emulsifying-drug-delivery-systems-to-improve-oral-absorption-and-enable-high-dose-toxicology-studies-of-a-cholesteryl-ester-transfer-protein-inhibitor-in-preclinical-species
#14
Xue-Qing Chen, Theresa Ziemba, Christine Huang, Ming Chang, Carrie Xu, Jennifer X Qiao, Tammy C Wang, Heather J Finlay, Mark E Salvati, Leonard P Adam, Olafur Gudmundsson, Michael J Hageman
BMS-A an inhibitor of cholesteryl ester transfer protein and is a highly lipophilic compound (clogP 10.5) with poor aqueous solubility (<0.0001 mg/mL at pH 6.5). The compound exhibits low oral exposure when dosed as cosolvent solution formulations. The purpose of this study was to evaluate lipid-based formulations for enabling high-dose toxicology studies and enhancing toxicology margins of BMS-A in preclinical studies in nonrodent species. The solubility of BMS-A was screened in lipid and cosolvent/surfactant excipients, and prototype formulations were developed...
January 6, 2018: Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/29287908/do-drug-release-studies-from-sedds-make-any-sense
#15
Andreas Bernkop-Schnürch, Aamir Jalil
Self-emulsifying drug delivery systems (SEDDS) are considered as a potential platform for mucosal drug delivery. The in vitro-in vivo correlation, however, is in particular for this type of delivery systems considerably poor resulting quite often in a simple trial and error approach in order to optimize formulations. One reason for this situation is certainly the lack of appropriate methods to determine the drug release from SEDDS in vitro, as the process is particularly troublesome. For quantification of the drug in the release medium the oily droplets need to be separated...
February 10, 2018: Journal of Controlled Release: Official Journal of the Controlled Release Society
https://www.readbyqxmd.com/read/29273857/development-of-a-dietary-formulation-of-the-sheta2-chemoprevention-drug-for-mice
#16
Doris M Benbrook, Naveena B Janakiram, Vishal Chandra, Gopal Pathuri, Venkateshwar Madka, Nicole C Stratton, Chioniso P Masamha, Cassadie N Farnsworth, Lucila Garcia-Contreras, Manolya Kukut Hatipoglu, Stan Lighfoot, Chinthalapally V Rao
Development of cancer chemoprevention compounds requires enhanced consideration for toxicity and route of administration because the target population is healthy. The small molecule drug, SHetA2 (NSC 726189), exhibited in vivo chemoprevention activity and lack of toxicity when administered by oral gavage. Our objective was to determine if a dietary formulation of SHetA2 could achieve effective tissue drug levels without toxicity. C57bl/6 J mice were monitored on modified American Institute of Nutrition (AIN)76A diet mixed with SHetA2 in a 3:1 ratio with Kolliphor HS15, a self-emulsifying drug delivery system (SEDDS) to deliver 37...
December 22, 2017: Investigational New Drugs
https://www.readbyqxmd.com/read/29133172/measuring-the-emulsification-dynamics-and-stability-of-self-emulsifying-drug-delivery-systems
#17
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...
February 2018: European Journal of Pharmaceutics and Biopharmaceutics
https://www.readbyqxmd.com/read/29105238/comparing-statewide-and-single-center-data-to-predict-high-frequency-emergency-department-utilization-among-patients-with-asthma-exacerbation
#18
Margaret E Samuels-Kalow, Mohammad K Faridi, Janice A Espinola, Jean E Klig, Carlos A Camargo
BACKGROUND: Previous studies examining high-frequency emergency department (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 statewide versus single-center data. METHODS: To track ED visits within a state, we analyzed 2011 to 2013 data from the New York State Healthcare Cost and Utilization Project State Emergency Department Databases...
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
#19
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
#20
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
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