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Azza A Mahmoud, Nermeen A Elkasabgy, Abdel Fatah A Abdelkhalek
Roflumilast is a selective inhibitor of phosphodiesterase-4 isoenzyme in lung cells. Having psychiatric adverse reactions when administered orally affects negatively the patients' adherence to the drug. This work aimed to prepare emulsified spray dried alginate microparticles for the pulmonary delivery of roflumilast. Sodium alginate was used as microparticle-forming material, isopropyl myristate as an oil, Tween®80 as surfactant and calcium beta-glycerophosphate as cross-linking agent to enhance the mechanical properties of the particles...
June 18, 2018: European Journal of Pharmaceutical Sciences
Matthew McMillin, Stephanie Grant, Gabriel Frampton, Anca D Petrescu, Jessica Kain, Elaina Williams, Rebecca Haines, Lauren Canady, Sharon DeMorrow
Background & Aims: Hepatic encephalopathy is a serious neurologic complication of acute and chronic liver diseases. We previously showed that aberrant bile acid signaling contributes to the development of hepatic encephalopathy via farnesoid X receptor (FXR)-mediated mechanisms in neurons. In the brain, a novel alternative bile acid synthesis pathway, catalyzed by cytochrome p450 46A1 (Cyp46A1), is the primary mechanism by which the brain regulates cholesterol homeostasis. The aim of this study was to determine if FXR activation in the brain altered cholesterol homeostasis during hepatic encephalopathy...
2018: Cellular and Molecular Gastroenterology and Hepatology
Ana Maria Dos Santos Moreira, Vanessa Bittencourt, Fábio Costa, Maria Elena de Lima, Miriam Lopes, Warley S Borges, Gustavo Martins, Jeferson da Silva, Ângelo M Leite Denadai, Keyller Bastos Borges
In the present work, hydrophobic nanoprecipitates (HNPs) of inclusion complexes formed between -cyclodextrin (CD) and the avermectins (AVMs) named eprinomectin (EPRI) and ivermectin (IVER) were synthesized and characterized, and their larvicidal activity against Aedes aegypti and human safety against fibroblasts were evaluated. Initially, thermogravimetric analysis/differential thermal analysis data revealed that inclusion increased the thermal stability of AVMs in the presence of CD. Nuclear magnetic resonance experiments and density functional theory calculations pointed out the inclusion of the benzofuran ring of the two AVMs in the βCD cavity...
June 21, 2018: Journal of Agricultural and Food Chemistry
Carolina Aloisio, Micaela Ponce-Ponte, Gladys E Granero, Marcela R Longhi
The aim of this work was to predict the permeability of two model drugs, sulfamerazine (SMR) and indomethacin (INM), and to determine the effect on their apparent permeabilities by complexation with cyclodextrins and/or meglumine or incorporation in microemulsions. Permeation experiments were performed using two-chamber diffusion cells with a new composition of bio-mimetic membrane composed of 80% of Lipoid® S100 and 20% of cholesterol in n-octanol 10% w/w solution, at 37 ± 0.5°C and 14,000 rpm. The predictive capacity of the permeability of passive diffusion absorbed compounds was evaluated using 20 drug standards and showed an exponential correlation between the apparent permeability coefficients (Papp ) and the fraction absorbed percentages in humans (Fa%), with an R2 value of 0...
June 19, 2018: AAPS PharmSciTech
Alaini Priebe, Megan Hunke, Raquel Tonello, Yogesh Sonawane, Temugin Berta, Amarnath Natarajan, Nattamai Bhuvanesh, Mahesh Pattabiraman, Surabhi Chandra
Purpose: Search for alternate pain medications has gained more importance in the past few years due to adverse effects associated with currently prescribed drugs including nervous system dysfunction with opioids, gastrointestinal discomfort with nonsteroidal anti-inflammatory drugs, and cardiovascular anomalies with cyclooxygenase-2 (COX-2) inhibitors. Phytomedicine has been explored for the treatment of pain, as these have been used for generations in regional communities and tend to lack major side effects in general...
2018: Journal of Pain Research
Rudra Pangeni, Jeong Uk Choi, Vijay Kumar Panthi, Youngro Byun, Jin Woo Park
Objective: The current study sought to design an oral delivery system of pemetrexed (PMX), a multitargeted antifolate antimetabolite, by enhancing its intestinal membrane permeability. Materials and methods: PMX was ionically complexed with a permeation enhancer such as N α -deoxycholyl-l-lysyl-methylester (DCK) and prepared as an amorphous solid dispersion by mixing with dispersants such as 2-hydroxypropyl-beta-cyclodextrin (HP-beta-CD) and poloxamer 188 (P188), forming an HP-beta-CD/PMX/DCK/P188; the complex was incorporated into multiple water-in-oil-in-water nanoemulsions in a supersaturated state (HP-beta-CD/PMX/DCK/P188-NE)...
2018: International Journal of Nanomedicine
Jing Li, Chao Qiu, Haoran Fan, Yuxiang Bai, Zhengyu Jin, Jinpeng Wang
A novel cyclodextrin-functionalized hybrid silicon nano-adsorbent material (6-EA-β-CD-Si) was synthesized via the nucleophilic substitution method. The structure was detected by Fourier transform infrared (FT-IR), X-ray, thermogravimetric analysis, and Brunauer-Emmett-Teller (BET) analysis. Results reveal that the BET surface area of 6-EA-β-CD-Si is 240 m²/g and the average pore size is 4.16 nm. The adsorption properties of 6-EA-β-CD-Si onto methylene blue (MB) were studied and fitted with adsorption kinetic models...
June 19, 2018: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
Fei Fang, Xiao-Jun Huang, Yi Zong Guo, Xiao Hong, Hui Min Wu, Rong Liu, Da Jing Chen
Cyclodextrins (CDs) are a family of cyclic oligosaccharides and its unique hydrophilic outer surface and lipophilic central cavity facilitate the formation of inclusion complexes with various biomolecules, such as cholesterol and phospholipids, via multi-interactions. Low-density lipoprotein (LDL) is the main carrier of cholesterol in bloodstream and is associated with the progression of atherosclerosis. The surface of LDL is composed of a shell of phospholipids monolayer containing most of the free unesterified cholesterol, as well as the single copy of apolipoprotein B-100...
June 20, 2018: Langmuir: the ACS Journal of Surfaces and Colloids
Kavitha Ramadass, Mallavarapu Megharaj, Kadiyala Venkateswarlu, Ravi Naidu
Heavier fraction hydrocarbons (C15 -C36 ) formed in soil after biotic and abiotic weatherings of engine oil are the continuing constraints in the bioremediation strategy, and their bioavailability remains a poorly quantified regulatory factor. In a microcosm study, we used two strains of Pseudomonas, P. putida TPHK-1 and P. aeruginosa TPHK-4, in strategies of bioremediation, viz., natural attenuation, biostimulation and bioaugmentation, for removal of weathered total petroleum hydrocarbons (TPHs) in soil contaminated long-term with high concentrations of engine oil (39,000-41,000 mg TPHs kg-1 soil)...
September 15, 2018: Science of the Total Environment
Moritz Vollrath, Julia Engert, Gerhard Winter
The aim of this work is a better understanding of solid lipid extrusion (SLE) for protein depot production using a lab-scale twin-screw (tsc) extruder. In this context, little is known about the relationship of process parameters such as extrusion temperature, screw speed, or formulation on implant characteristics. It is difficult to attribute release characteristics to only one parameter, since the release will always be influenced by a combination of parameters. In this study, we describe the use of an online pressure measurement tool which allows to characterize pressure profiles during an extrusion run...
June 15, 2018: European Journal of Pharmaceutics and Biopharmaceutics
Yusra Rahman, Shumaila Afrin, Mohammad Tabish
Studying the interaction of therapeutic molecules with serum albumin is important to understand their biopharmaceutics, pharmacokinetics and toxicity as well as their relation with the structure and function of protein. The biomolecular interaction of an anti-spasmodic drug, pirenzepine with bovine serum albumin (BSA) was investigated using multi-spectroscopic, calorimetric and docking studies. Fluorescence quenching of BSA on interaction with pirenzepine revealed the static mode of quenching. Pirenzepine exhibited a moderate binding to serum albumin with the binding constant value in the order of 104  M-1 ...
June 13, 2018: Archives of Biochemistry and Biophysics
Xiaohui Niu, Zunli Mo, Xing Yang, Mingyuan Sun, Pan Zhao, Zhenliang Li, Meixuan Ouyang, Zhenyu Liu, Huhu Gao, Ruibin Guo, Nijuan Liu
β-Cyclodextrin (β-CD) possess a hydrophobic inner cavity and a hydrophilic exterior surface. They exhibit excellent inclusion properties with the guest molecules that match cavity size, and β-CD-based materials drew widespread attention in electrochemical sensors. The hydroxy groups at the edge of the cavity can form hydrogen bonds and undergo electrostatic and dipole-dipole interactions with other molecules. This review (with 109 refs.) reveals β-CD-based detection mechanisms from the viewpoint of the size/shape-fit concept, and summarizes the current state of multiple electrochemical sensors based on the use of β-CD and functionalized β-CD such as carboxymethyl-β-CD, mono-(6-ethanediamine-6-deoxy)-β-CD, hydroxypropyl-β-CD, thio-β-cyclodextrin, and others...
June 16, 2018: Mikrochimica Acta
Hideto Matsui, Atsushi Tamura, Mamoru Osawa, Asato Tonegawa, Yoshinori Arisaka, Mitsuaki Matsumura, Hiroyuki Miura, Nobuhiko Yui
Because macrophages are involved in the pathology of many diseases, targeting delivery of therapeutic molecules to macrophages is important issue. Polyrotaxanes (PRXs) composed of multiple cyclodextrins threaded with a linear polymer were utilized as a therapeutic agent for metabolic disease and for regulating cellular metabolism. For targeting delivery of PRXs to macrophages, carboxyethyl ether group-modified PRXs (CEE-PRXs) are designed for promoting interaction to macrophage scavenger receptor class A (SR-A)...
June 13, 2018: Macromolecular Bioscience
Andrea C S M Gomes, Samuel R Dos Santos, Maycon C Ribeiro, Pedro V L Cravo, José Daniel G Vieira, Keili M C DE Souza, Andre C Amaral
In the present work, different Brazilian biomes aiming to identify and select cyclodextrin glycosyltransferase-producer bacteria are explored. This enzyme is responsible for converting starch to cyclodextrin, which are interesting molecules to carry other substances of economic interest applied by textile, pharmaceutical, food, and other industries. Based on the enzymatic index, 12 bacteria were selected and evaluated, considering their capacity to produce the enzyme in culture media containing different starch sources...
April 2018: Anais da Academia Brasileira de Ciências
Akihito Hashidzume, Akihiro Kuse, Tomoya Oshikiri, Seiji Adachi, Mitsutaka Okumura, Hiroyasu Yamaguchi, Akira Harada
In the molecular world, molecular ratchets can realize the unidirectional movement in molecular machines. However, construction of artificial molecular ratchets has been still a great challenge. In this study, we investigate the formation of pseudo-rotaxane of a newly designed two-station axis molecule with α-cyclodextrin (α-CD) and the deuteration of acidic protons in the axis in D2 O by 1 H NMR at varying temperatures. Using the NMR data, we roughly estimate apparent rate constants for association, dissociation, and translation of α-CD during the pseudo-rotaxane formation based on a simplified kinetic model...
June 12, 2018: Scientific Reports
Anton A Ivanov, Clément Falaise, Pavel A Abramov, Michael A Shestopalov, Kaplan Kirakci, Kamil Lang, Mhamad A Moussawi, Maxim N Sokolov, Nikolay G Naumov, Sébastien Floquet, David Landy, Mohamed Haouas, Konstantin A Brylev, Yuri V Mironov, Yann Molard, Stéphane Cordier, Emmanuel Cadot
Water-soluble salts of anionic [Re6Q8(CN)6]4- (Q = S, Se, Te) chalcogenide octahedral rhenium clusters react with γ-cyclodextrin (γ-CD) producing a new type of inclusion compounds. Crystal structures determined through single-crystal X-ray diffraction analysis revealed supramolecular host-guest assemblies resulting from close encapsulations of the octahedral cluster within two γ-CDs. Interestingly, nature of the inner Q ligands influences strongly the host-guest conformation. The cluster [Re₆S₈(CN)6]4- interacts preferentially with the primary faces of the γ-CD while the bulkier clusters [Re6Se8(CN)6]4- and [Re6Te8(CN)6]4- exhibit specific interactions with the secondary faces of the cyclic host...
June 12, 2018: Chemistry: a European Journal
Jia Liu, Xingxin Liu, Ye Yuan, Qilin Li, Bingcheng Chang, Luming Xu, Bo Cai, Chao Qi, Cao Li, Xulin Jiang, Guobin Wang, Zheng Wang, Lin Wang
Since heterogeneity affects many functional aspects of a tumor, a way to overcome it is to arm nanosized drug delivery systems (nanoDDS) with diverse functions required to shatter heterogeneity. However, it remains technically challenging to fabricate a nanocarrier possessing all required functions. Here we propose a modular strategy for generating a supramolecular, multifunctional, stimuli-responsive nanoDDS through docking a parental core nanoDDS with various daughter function-prebuilt modules. Doxorubicin loaded mesoporous silica nanoparticles (MSNs) as the parental nano-core are wrapped by poly(β-cyclodextrin) (PCD) as a gatekeeper through host-guest interactions between cyclodextrin and pyridine groups of pyridine-disulfide bonds that confers pH/redox dual responsiveness, thus constructing stimuli-responsive nanoDDS (DOX@PRMSNs)...
June 12, 2018: ACS Applied Materials & Interfaces
Jan Nekvinda, Bohumír Grüner, Detlef Gabel, Werner Nau, Khaleel Assaf
Polyhedral carboxymethyl-carborane (C₂B₁₀H₁₂) derivatives have been synthesized, which include mono- and di-substituted o-, m-, p- isomers. The supramolecular host-guest complexation of these derivatives with cyclodextrins (CDs, namely, α-CD, β-CD, and γ-CD) has been investigated in water. The globular structure of the carborane binding moiety and its hydrophobic character qualify it as an ideal recognition site to form stable inclusion complexes with macrocyclic host molecules in aqueous solution...
June 12, 2018: Chemistry: a European Journal
Zhenqiang Dong, Yang Kang, Qijuan Yuan, Manli Luo, Zhipeng Gu
Designing stimuli responsive, controllable and biocompatible multifunctional nanoparticles is an important progress in the current quest for drug delivery systems. Herein, we devoted to developing a β-cyclodextrin (β-CD) based drug delivery nanoparticles (NPs) that release Bovine serum albumin (BSA) via glucose-responsive gate. The design involves synthesis of sodium alginate with β-CD modified (Alg-β-CD) and methoxypolyethylene glycol (mPEG-Fc) containing ferrocene (Fc) uncharged end-capping. When α-cyclodextrin (α-CD) was added with these two segments, the stable non-covalent supramolecular structure of Alg-β-CD/mPEG-Fc/α-CD can be self-assembled into NPs in aqueous solution...
2018: Frontiers in Pharmacology
Karim Benhenia, Hamza Rahab, Mustapha-Adnane Smadi, Hamza Benmakhlouf, Ali Lamara, Takfarinas Idres, Mokrane Iguer-Ouada
Vitamin E is a potent molecule, especially when loaded in cyclodextrin, in modulating oxidative stress during the freeze-thawing process. The present study aimed to investigate the effect of different concentrations of cyclodextrin-vitamin E complex (CD-Vit E) on cryopreserved ram sperm. Ejaculates collected from five adult rams were pooled and divided into four aliquots. All aliquots were treated in Tris-extender (Tris-glucose-citric acid) containing 2 mg cholesterol-loaded methyl-β- cyclodextrin/120 × 106 spermatozoa and either 0 (Control), 2, 4 or 6 mg CD-Vit E/120 × 106 spermatozoa, corresponding to 0, 0...
June 6, 2018: Animal Reproduction Science
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