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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
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...
February 28, 2018: Nanomedicine
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
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 )...
February 16, 2018: International Journal of Pharmaceutics
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...
February 15, 2018: Science of the Total Environment
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...
January 31, 2018: International Journal of Pharmaceutics
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...
January 17, 2018: Journal of Controlled Release: Official Journal of the Controlled Release Society
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...
January 12, 2018: International Journal of Pharmaceutics
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
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 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 pre-GLP studies in non-rodent 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
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...
December 26, 2017: Journal of Controlled Release: Official Journal of the Controlled Release Society
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
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
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
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
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
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
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
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...
December 1, 2017: Colloids and Surfaces. B, Biointerfaces
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
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