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Sanipon Chanburee, Waree Tiyaboonchai
This study aimed to compare the intestinal permeation of curcumin-loaded polymer coated nanostructured lipid carriers (NLCs) and uncoated NLCs using the Caco-2 cell model. The uncoated NLCs were prepared using a warm microemulsion technique, while polymer-coated NLCs were prepared with the same method but were followed by coating particle surface with polyethylene glycol (PEG) 400 or polyvinyl alcohol (PVA). After lyophilization, all formulations possessed a mean size of <400 nm with a zeta potential of ∼-30 mV and a high entrapment efficacy up to 90%...
March 21, 2017: Journal of Biomedical Materials Research. Part B, Applied Biomaterials
Sandra Šegan, Nina Božinović, Igor Opsenica, Filip Andrić
Lipophilicity is one of the essential properties influencing drug absorption, excretion and metabolism. It is used for screening of viable drug candidates. Chromatographic behavior of thiepino[3,2-c:6,7-c']dipyridine and 16 benzothiepino[3,2-c]pyridine derivatives as potential antifungal drugs was studied using thin-layer chromatography under typical reversed-phase conditions and two microemulsion chromatographic systems. Seventeen chromatographic and nine in silico lipophilicity measures were estimated. They were compared by classical multivariate approaches: principal component analysis, hierarchical cluster analysis, and ranked and grouped by the non-parametric method-Sum of ranking differences...
March 21, 2017: Journal of Separation Science
Dongmei Li, Qinghua He, Yonghong He, Meiguo Xin, Yilong Zhang, Zhiyuan Shen
A new type of sensing protocol, based on a high precision metrology of quantum weak measurement, was first proposed for molecularly imprinted polymers (MIP) sensor. The feasibility, sensitivity and selectivity of weak measurement based MIP (WMMIP) sensor were experimentally demonstrated with bovine serum albumin (BSA). Weak measurement system exhibits high sensitivity to the optical phase shift corresponding to the refractive index change, which is induced by the specific capture of target protein molecules with its recognition sites...
March 10, 2017: Biosensors & Bioelectronics
Cedric Vancaeyzeele, Florian Olivier, Gwendoline Petroffe, Sebastien Peralta, Frederic Vidal
We capitalized herein the inherent tortuosity of bicontinuous microemulsion to conceive nanostructured drug delivery devices. First, we show that it is possible to synthesize bicontinuous materials with continuous hydrophilic domains of PNIPAM network entangled with continuous hydrophobic polymer domains, dual phase continuity being imposed by the bicontinuous microemulsions used as soft template. A particular attention is paid to the microemulsion formulations using a surfmer to preserve the one-to-one replication of the bicontinuous nanostructure after polymerization...
March 17, 2017: ACS Applied Materials & Interfaces
Vanessa de Fátima Lima Paiva Medeiros, Ítalo Medeiros Azevedo, Marília Daniela Ferreira Carvalho, Cláudia Nunes Oliveira, Eryvaldo Sócrates Tabosa do Egito, Aldo Cunha Medeiros
To evaluate the effect of tadalafil in renal ischemia/reperfusion (I/R) injury in rats Methods: Group I/R saline rats (n=6) were subjected to 45 minutes of left renal ischemia and treated with saline; the I/R tadalafil rats (n=6) received oral 10mg/kg tadalafil microemulsion one hour before ischemia. In both groups, 8 hours after ischemia, laboratory analysis were performed Results: Better tissue perfusion was lower in ischemic left/kidney than in right/kidney in saline group, suggesting reduced kidney clearance...
February 2017: Acta Cirúrgica Brasileira
Minh Nguyet Pham, Toi Van Vo, Van-Thanh Tran, Phuong Ha-Lien Tran, Thao Truong-Dinh Tran
Microemulsion has the potentials to enhance dissolution as well as facilitate absorption and permeation of poorly water-soluble drugs through biological membranes. However, its application to govern a controlled release buccal delivery for local treatment has not been discovered. The aim of this study is to develop microemulsion-based mucoadhesive wafers for buccal delivery based on an incorporation of the microemulsion with mucoadhesive agents and mannitol. Ratio of oil to surfactant to water in the microemulsion significantly impacted quality of the wafers...
March 15, 2017: AAPS PharmSciTech
Nina Hecht, Nils Terveer, Curd Schollmayer, Ulrike Holzgrabe, Lorenz Meinel
Triazolopyrimidine derivatives from the VAS library have been found to be efficient and selective NADPH oxidase (NOX) inhibitors in vitro. In spite of numerous publications on this compound class detailing efficacy for the treatment of cardiovascular diseases, in vivo translation is challenged by their very low water solubility which is preventing further use of these compounds and blocking clinical translation. Therefore, we addressed the challenge of water solubility for three triazolopyrimidine derivatives, VAS2870, VAS3947, and VAS4024, and developed formulations for oral or parenteral application with translational potential into preclinical and clinical studies...
March 8, 2017: European Journal of Pharmaceutics and Biopharmaceutics
Yunrong Zhang, Li He, Shanlan Yue, Qingting Huang, Yuhong Zhang, Junyi Yang
The purpose of this study was to characterize and evaluate tectorigenin-loaded self-microemulsifying drug delivery system (TG-SMEDDS), a previously studied preparation, and further confirm the improvement of TG in solubility and bioavailability. The appearance of TG-SMEDDS was clear and transparent, with good mobility. The microemulsion formed by TG-SMEDDS was globular, edge smooth, clear-cut, and distribution homogeneous under transmission electron microscope. The stability studies revealed that TG-SMEDDS remained stable at room temperature for at least 3 months...
November 2017: Drug Delivery
Jéssica Bassi da Silva, Sabrina Barbosa de Souza Ferreira, Osvaldo de Freitas, Marcos Luciano Bruschi
Mucoadhesion is a useful strategy for drug delivery systems, such as tablets, patches, gels, liposomes, micro/nanoparticles, nanosuspensions, microemulsions and colloidal dispersions. Moreover, it has contributed to many benefits like increased residence time at application sites, drug protection, increased drug permeation and improved drug availability. In this context, investigation into the mucoadhesive properties of pharmaceutical dosage forms is fundamental, in order to characterize, understand and simulate the in vivo interaction between the formulation and the biological substrate, contributing to the development of new mucoadhesive systems with effectiveness, safety and quality...
March 1, 2017: Drug Development and Industrial Pharmacy
Handan He, Phi Tran, Helen Gu, Vivienne Tedesco, Jin Zhang, Wen Lin, Ewa Gatlik, Kai Klein, Tycho Heimbach
The absorption, metabolism and excretion of midostaurin, a potent class III tyrosine protein kinase inhibitor for acute myelogenous leukemia, were evaluated in healthy subjects. A microemulsion formulation was chosen to optimize absorption. After a 50 mg [14C]midostaurin dose, oral absorption was high (> 90%) and relatively rapid. In plasma, the major circulating components were midostaurin (22%), CGP52421 (32.7%), and CGP62221 (27.7%). Long plasma half-lives were observed for midostaurin (20.3 h), CGP52421 (495 h), and CGP62221 (33...
March 7, 2017: Drug Metabolism and Disposition: the Biological Fate of Chemicals
Jiansong Lin, Linyan Yang, Ting Wang, Renxian Zhou
Four different synthetic routes (co-precipitation, oxidation-precipitation, citric acid sol-gel and reversed microemulsion) are adopted to prepare barium modified Pd/CeO2-ZrO2 catalysts and their catalytic activity towards CO, HC and NOx conversions is studied. The surface and bulk properties of these catalysts are characterized via XRD, N2 adsorption, XPS, UV-Raman, H2-TPR, and in situ DRIFTS. The catalyst prepared via the co-precipitation method exhibits the optimum three-way catalytic behavior, which is mainly due to its superior redox ability, whereas the oxidation-precipitation synthesis renders the catalyst with the best homogeneity and thermal resistance...
March 6, 2017: Physical Chemistry Chemical Physics: PCCP
Mohamed Adel Bakr, Ayman Maher Nagib, Osama Ashry Gheith, Ahmed Farouk Hamdy, Ayman Fathi Refaie, Ahmed Farouk Donia, Ahmed Hassan Neamatalla, Khaled Farouk Eldahshan, Ahmed Abdelfattah Denewar, Mohamed Hamed Abbas, Amany Ismail Mostafa, Mohamed Ahmed Ghoneim
OBJECTIVES: We review different immunosuppressant protocols used for living-donor kidney transplant recipients at our center. MATERIALS AND METHODS: Many prospective randomized studies from our center have been reported between March 1976 and 2016, with more than 2700 renal transplant procedures conducted. The first study was a prospective randomized trial of azathioprine versus cyclosporine. The second study compared triple therapy (prednisolone + azathioprine + cyclosporine) versus conventional therapy (prednisolone + azathioprine)...
February 2017: Experimental and Clinical Transplantation
Mara Rosa Gil Hernandes, Lucélia Campelo Albuquerque Moraes, Elton Brito Ribeiro, Danny Laura Gomes Fagundes, Adenilda Cristina Honorio-França, Eduardo Luzía França
BACKGROUND: Giardiasis is one of the main parasites that infect the gastrointestinal tract of humans, affecting hundreds of millions of people worldwide, particularly in developing countries. Antiparasitics administered to treat giardiasis are inefficient in 20% of the cases, usually because of parasite resistance and side effects. In this scenario, microemulsions are a promising pharmaceutical alternative as carriers of molecules with therapeutic action that stimulate the immune system...
February 28, 2017: Parasitology International
Wen-Ke Xu, Hui Jiang, Kui Yang, Ya-Qin Wang, Qian Zhang, Jian Zuo
α-Mangostin (MG) is a versatile bioactive compound isolated from mangosteen and possesses significant pharmacokinetic shortages. To augment the potential clinical efficacy, MG-loaded self-microemulsion (MG-SME) was designed and prepared in this study, and its potential as a drug loading system was evaluated based on the pharmacokinetic performance and tissue distribution feature. The formula of MG-SME was optimized by an orthogonal test under the guidance of ternary phase diagram, and the prepared MG-SME was characterized by encapsulation efficiency, size distribution, and morphology...
March 2017: Kaohsiung Journal of Medical Sciences
Xu Li, Youssef W Naguib, Solange Valdes, Stephanie Hufnagel, Zhengrong Cui
The development of phosphonate-metal materials is tightly related to the advancement in their synthesis methods. Herein, using zoledronic acid (Zol), a bisphosphonate (bioacitve phosphonate with a 'P-C-P' structure), and calcium as model molecules, we applied the reverse microemulsion (RM) to synthesize a series of Zol-Ca complexes. We comprehensively i) studied the relationship between RM conditions, including the component ratio of RM, co-surfactants, reaction time, reactant concentrations, reaction temperature, and the presence of a phospholipid, 1, 2-dioleoyl-sn-glycero-3-phosphate acid (DOPA), and the physical properties of the complexes synthesized (i...
March 2, 2017: ACS Applied Materials & Interfaces
Daqiao Hu, Shan Jin, Yi Shi, Xiaofeng Wang, Robert W Graff, Wenqi Liu, Manzhou Zhu, Haifeng Gao
A robust approach is developed to prepare hyperstar polymer-Au25(SR)18 nanocomposites for catalysis. The synthesis started with atom transfer radical copolymerization of an inimer with a cyclic disulfide-containing methacrylate monomer in a microemulsion to produce hyperbranched copolymers with high molar mass, low polydispersity, and a vital fraction of dangling disulfide groups. The core-shell structured hyperstar polymers were then prepared using hyperbranched copolymers as macroinitiators to polymerize oligo(ethylene glycol) methyl ether methacrylate (Mn = 500) and grow the radiating arms...
March 1, 2017: Nanoscale
P Mishra, A P B Balaji, P K Dhal, R S Suresh Kumar, S Magdassi, K Margulis, B K Tyagi, A Mukherjee, N Chandrasekaran
The occurrence of pesticidal pollution in the environment and the resistance in the mosquito species makes an urge for the safer and an effective pesticide. Permethrin, a poorly water-soluble pyrethroid pesticide, was formulated into a hydrodispersible nanopowder through rapid solvent evaporation of pesticide-loaded oil in water microemulsion. Stability studies confirmed that the nanopermethrin dispersion was stable in paddy field water for 5 days with the mean particle sizes of 175.3 ± 0.75 nm and zeta potential of -30...
March 1, 2017: Bulletin of Entomological Research
Wei Liu, Yong-Mei Wang, Yu-Hao Li, Shi-Jiao Cai, Xue-Bo Yin, Xi-Wen He, Yu-Kui Zhang
Imaging-guided therapy systems (IGTSs) are revolutionary techniques used in cancer treatment due to their safety and efficiency. IGTSs should have tunable compositions for bioimaging, a suitable size and shape for biotransfer, sufficient channels and/or pores for drug loading, and intrinsic biocompatibility. Here, a biocompatible nanoscale zirconium-porphyrin metal-organic framework (NPMOF)-based IGTS that is prepared using a microemulsion strategy and carefully tuned reaction conditions is reported. A high content of porphyrin (59...
February 28, 2017: Small
K Podgórna, K Szczepanowicz, M Piotrowski, M Gajdošová, F Štěpánek, P Warszyński
Synthesis of theranostic nanoparticles, which combine both therapeutic and diagnostic capabilities in one platform can be considered as a step forward personalized medicine, since it allows tracing the delivery of the drug to targeted organ. Thus, the aim of this work was to prepare gadolinium alginate gel nanoparticles (gadolinum nanogels - GdNG) by the reverse microemulsions and physical crosslinking method as the vehicles able to carry hydrophilic drugs and to be traced by the Magnetic Resonance Imaging (MRI)...
February 21, 2017: Colloids and Surfaces. B, Biointerfaces
Sameer Bhandari, Vikas Rana, Ashok K Tiwary
AIM: The low aqueous solubility of artemether and lumefantrine makes them less bioavailable. It is expected that by formulating self-microemulsifying drug-delivery systems (SMEDDS), their aqueous solubility and absorption will thus be enhanced. Results & methodology: Optimized liquid SMEDDS containing artemether and lumefantrine was adsorbed on Neusilin US2(®) employing spray drying technique to convert it into solid SMEDDS. Almost 90% of both drugs were released within 15 min in their respective official dissolution media...
April 2017: Therapeutic Delivery
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