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Pharmaceutics

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https://www.readbyqxmd.com/read/30513962/analysis-of-vipadenant-and-its-in-vitro-and-in-vivo-metabolites-via-liquid-chromatography-quadrupole-time-of-flight-mass-spectrometry
#1
Seok-Ho Shin, Min-Ho Park, Jin-Ju Byeon, Byeong Ill Lee, Yuri Park, Nahye Kim, Jangmi Choi, Young G Shin
A simple and sensitive liquid chromatography⁻quadrupole-time-of-flight⁻mass spectrometric (LC-QTOF-MS) assay has been developed for the evaluation of drug metabolism and pharmacokinetics (PK) properties of vipadenant in rat, a selective A2a receptor antagonist as one of the novel immune checkpoint inhibitors. A simple protein precipitation method using acetonitrile was used for the sample preparation and the pre-treated samples were separated by a reverse-phase C18 column. The calibration curve was evaluated in the range of 3...
December 3, 2018: Pharmaceutics
https://www.readbyqxmd.com/read/30513888/modeling-of-disintegration-and-dissolution-behavior-of-mefenamic-acid-formulation-using-numeric-solution-of-noyes-whitney-equation-with-cellular-automata-on-microtomographic-and-algorithmically-generated-surfaces
#2
Reiji Yokoyama, Go Kimura, Christian M Schlepütz, Jörg Huwyler, Maxim Puchkov
Manufacturing parameters may have a strong impact on the dissolution and disintegration of solid dosage forms. In line with process analytical technology (PAT) and quality by design approaches, computer-based technologies can be used to design, control, and improve the quality of pharmaceutical compacts and their performance. In view of shortcomings of computationally intensive finite-element or discrete-element methods, we propose a modeling and simulation approach based on numerical solutions of the Noyes-Whitney equation in combination with a cellular automata-supported disintegration model...
December 3, 2018: Pharmaceutics
https://www.readbyqxmd.com/read/30513861/buccal-bullfrog-rana-catesbeiana-shaw-oil-emulsion-a-mucoadhesive-system-intended-for-treatment-of-oral-candidiasis
#3
Susiane S Moreira-Oliveira, Lucas Amaral-Machado, Wógenes Nunes de Oliveira, Éverton N Alencar, Kelly Cristine Zatta, Luanda B F C de Souza, Aldo da Cunha Medeiros, Guilherme Maranhão Chaves, Eryvaldo S T Egito
Oral candidiasis (OC) is an infectious disease caused by microorganisms of the genus Candida , leading to lesions in the buccal cavity. Its treatment consists of the administration of topical or systemic antifungal agents, which may compromise the patient compliance due to its side effects, highlighting the need for alternative treatments. In this scenario, bullfrog oil, an animal oil composed of a pool of saturated and unsaturated fatty acids, is introduced as a potential antifungal raw material. Thus, the aim of this work was to produce a mucoadhesive emulsified system able to deliver the bullfrog oil in the buccal cavity to treat the OC...
December 3, 2018: Pharmaceutics
https://www.readbyqxmd.com/read/30513860/importance-of-binding-affinity-for-the-activity-of-a-metallodendritic-chemical-nuclease
#4
Yi-Hsuan Tang, Sodio C N Hsu, Po-Yu Chen, Si-Ting Liou, Hui-Ting Chen, Carol Hsin-Yi Wu, Chai-Lin Kao
A family of bis (2-pyridyl)amino-modified poly(amidoamine) dendrimer Cu complexes was prepared, and their chemical nuclease activities and binding affinity ( Kb ) levels for DNA plasmid were investigated. The K b values of the G2 to G6 apodendrimers for DNA plasmid were found to be 7.4, 23, 48, 70, and 280 µM-1 , respectively, using ethidium bromide (EtBr) displacement experiments. The chemical nuclease activities of the corresponding complexes were determined by gel electrophoresis, and a clear positive dendritic effect was observed...
December 3, 2018: Pharmaceutics
https://www.readbyqxmd.com/read/30513858/novel-findings-about-double-loaded-curcumin-in-hp%C3%AE-cyclodextrin-in-liposomes-effects-on-the-lipid-bilayer-and-drug-release
#5
Ana-María Fernández-Romero, Francesca Maestrelli, Paola Angela Mura, Antonio María Rabasco, María Luisa González-Rodríguez
In this study, the encapsulation of curcumin (Cur) in "drug-in-cyclodextrin-in-liposomes (DCL)" by following the double-loading technique (DL) was proposed, giving rise to DCL⁻DL. The aim was to analyze the effect of cyclodextrin (CD) on the physicochemical, stability, and drug-release properties of liposomes. After selecting didodecyldimethylammonium bromide (DDAB) as the cationic lipid, DCL⁻DL was formulated by adding 2-hydroxypropyl-α/β/γ-CD (HPβCD)⁻Cur complexes into the aqueous phase...
December 3, 2018: Pharmaceutics
https://www.readbyqxmd.com/read/30513856/improving-encapsulation-of-hydrophilic-chloroquine-diphosphate-into-biodegradable-nanoparticles-a-promising-approach-against-herpes-virus-simplex-1-infection
#6
Tábata Loíse Cunha Lima, Renata de Carvalho Feitosa, Emanuell Dos Santos-Silva, Alaine Maria Dos Santos-Silva, Emerson Michell da Silva Siqueira, Paula Renata Lima Machado, Alianda Maira Cornélio, Eryvaldo Sócrates Tabosa do Egito, Matheus de Freitas Fernandes-Pedrosa, Kleber Juvenal Silva Farias, Arnóbio Antônio da Silva-Júnior
Chloroquine diphosphate (CQ) is a hydrophilic drug with low entrapment efficiency in hydrophobic nanoparticles (NP). Herpes simplex virus type 1 (HSV-1) is an enveloped double-stranded DNA virus worldwide known as a common human pathogen. This study aims to develop chloroquine-loaded poly(lactic acid) (PLA) nanoparticles (CQ-NP) to improve the chloroquine anti- HSV-1 efficacy. CQ-NP were successfully prepared using a modified emulsification-solvent evaporation method. Physicochemical properties of the NP were monitored using dynamic light scattering, atomic force microscopy, drug loading efficiency, and drug release studies...
December 3, 2018: Pharmaceutics
https://www.readbyqxmd.com/read/30513791/formulation-and-characterization-of-native-and-crosslinked-hyaluronic-acid-microspheres-for-dermal-delivery-of-sodium-ascorbyl-phosphate-a-comparative-study
#7
Arianna Fallacara, Filippo Marchetti, Michele Pozzoli, Ugo Raffaello Citernesi, Stefano Manfredini, And Silvia Vertuani
The present work evaluates for the first time the use of urea-crosslinked hyaluronic acid (HA-CL), a novel derivative of native hyaluronic acid (HA), to produce microspheres (MS) by emulsification-solvent evaporation, for dermal delivery of sodium ascorbyl phosphate (SAP). As the term of comparison, HA MS were prepared. A pre-formulation study-investigation of the effects of polymers solutions properties (pH, viscosity) and working conditions-led to the - production of optimized HA-CL MS and HA-CL-SAP MS with: almost unimodal size distributions; mean diameter of 13...
December 1, 2018: Pharmaceutics
https://www.readbyqxmd.com/read/30513750/pharmacokinetic-profile-of-kaurenoic-acid-after-oral-administration-of-araliae-continentalis-radix-extract-powder-to-humans
#8
Eun-Jeong Choi, Go-Wun Choi, Seung-Jeong Yang, Yong-Bok Lee, Hea-Young Cho
The objective of this study was to characterize pharmacokinetics (PKs) of kaurenoic acid (KAU) after administration of the clinical usual dose of Araliae Continentalis Radix extract powder to Korean subjects for the first time and evaluate the mechanism of its absorption in vitro . A simple, sensitive, and selective analytical method was developed for the detection of KAU in human plasma. Concentrations of KAU were quantified by ultra-performance liquid chromatography tandem mass spectrometry after simple liquid⁻liquid extraction...
December 1, 2018: Pharmaceutics
https://www.readbyqxmd.com/read/30513738/moisture-resistant-co-spray-dried-netilmicin-with-l-leucine-as-dry-powder-inhalation-for-the-treatment-of-respiratory-infections
#9
Yingtong Cui, Xuejuan Zhang, Wen Wang, Zhengwei Huang, Ziyu Zhao, Guanlin Wang, Shihao Cai, Hui Jing, Ying Huang, Xin Pan, Chuanbin Wu
Netilmicin (NTM) is one of the first-line drugs for lower respiratory tract infections (LRTI) therapy, but its nephrotoxicity and ototoxicity caused by intravenous injection restrict its clinical application. Dry powder inhalation (DPI) is a popular local drug delivery system that is introduced as a solution. Due to the nature of NTM hygroscopicity that hinders its direct use through DPI, in this study, L-leucine (LL) was added into NTM dry powder to reduce its moisture absorption rate and improve its aerosolization performance...
December 1, 2018: Pharmaceutics
https://www.readbyqxmd.com/read/30513734/l-cysteine-and-l-serine-modified-dendrimer-with-multiple-reduced-thiols-as-a-kidney-targeting-reactive-oxygen-species-scavenger-to-prevent-renal-ischemia-reperfusion-injury
#10
Satoru Matsuura, Hidemasa Katsumi, Hiroe Suzuki, Natsuko Hirai, Rie Takashima, Masaki Morishita, Toshiyasu Sakane, Akira Yamamoto
l-cysteine (Cys)- and l-serine (Ser)-modified, third-generation polyamidoamine (PAMAM) dendrimer with multiple reduced thiols (Ser-PAMAM-Cys) was synthesized as a kidney-targeting reactive oxygen species (ROS) scavenger to help prevent renal ischemia/reperfusion injury. Ser-PAMAM-Cys effectively scavenged 2,2-diphenyl-1-picrylhydrazyl (DPPH) radical and ROS (hydrogen peroxide and hydroxyl radical) in phosphate-buffered saline (PBS). In addition, ~64% of 111 In-labeled Ser-PAMAM-Cys accumulated in mouse kidney 3 h after intravenous administration...
December 1, 2018: Pharmaceutics
https://www.readbyqxmd.com/read/30513731/dealing-with-skin-and-blood-brain-barriers-the-unconventional-challenges-of-mesoporous-silica-nanoparticles
#11
REVIEW
Alessandra Nigro, Michele Pellegrino, Marianna Greco, Alessandra Comandè, Diego Sisci, Luigi Pasqua, Antonella Leggio, Catia Morelli
Advances in nanotechnology for drug delivery are fostering significant progress in medicine and diagnostics. The multidisciplinary nature of the nanotechnology field encouraged the development of innovative strategies and materials to treat a wide range of diseases in a highly specific way, which allows reducing the drug dosage and, consequently, improving the patient's compliance. Due to their good biocompatibility, easy synthesis, and high versatility, inorganic frameworks represent a valid tool to achieve this aim...
December 1, 2018: Pharmaceutics
https://www.readbyqxmd.com/read/30513707/investigation-of-combined-cyclodextrin-and-hydrogel-formulation-for-ocular-delivery-of-dexamethasone-acetate-by-means-of-experimental-designs
#12
Roseline Mazet, Luc Choisnard, Delphine Levilly, Denis Wouessidjewe, Annabelle Gèze
Dexamethasone acetate (DXMa) has proven its efficiency to treat corneal inflammation, without a great propensity to increase intraocular pressure. Unfortunately, its poor aqueous solubility, associated with a rapid precorneal elimination, results in a low drug bioavailability and a low penetration after topical ocular administration. The main objective of this study was to improve the apparent aqueous solubility of DXMa using cyclodextrins. First, hydroxypropyl-β-CD (HPβCD) and hydroxypropyl-γ-CD (HPγCD) were used to enhance DXMa concentration in aqueous solution...
December 1, 2018: Pharmaceutics
https://www.readbyqxmd.com/read/30501051/pharmacodynamic-effect-of-luteolin-micelles-on-alleviating-cerebral-ischemia-reperfusion-injury
#13
Liwei Tan, Chen Liang, Yeye Wang, Yu Jiang, Shengqiao Zeng, Rui Tan
Oxidative stress and inflammation are important mechanisms of cerebral ischemia reperfusion (IR) injury. Luteolin (Lu), one of the major active components in the classical Tibetan prescription, which has been used in the treatment of cardiovascular diseases since 700 BC, has potential for IR injury therapy. Its hydrophobicity has impeded its further applications. In this study, we first prepared Lu micelles (M-Lu) by self-assembling with an amphiphilic copolymer via the thin film hydration method to improve the dispersion of Lu in water...
November 29, 2018: Pharmaceutics
https://www.readbyqxmd.com/read/30487449/flurbiprofen-loaded-solid-snedds-preconcentrate-for-the-enhanced-solubility-in-vitro-dissolution-and-bioavailability-in-rats
#14
Rae Man Kim, Dong-Jin Jang, Yu Chul Kim, Jin-Ha Yoon, Kyoung Ah Min, Han-Joo Maeng, Kwan Hyung Cho
The aim of this work was to prepare and optimize a solid self-nanoemulsifying drug delivery system pre-concentrate (SSP) containing water-insoluble flurbiprofen (FL) using a novel pseudo-ternary phase diagram. The pseudo-ternary phase diagram, composed of FL as the drug and dispersion core, Kollisolv MCT 70 as the oil phase, and TPGS (tocopherol polyethylene glycol 1000 succinate) as the surfactant, was constructed for the determination of the SSP region. SSP was investigated in terms of particle size, physical state by differential scanning calorimetry (DSC) and powder X-ray diffraction (PXRD), in vitro dissolution and oral pharmacokinetics in rats...
November 28, 2018: Pharmaceutics
https://www.readbyqxmd.com/read/30469356/mrna-expression-and-activity-of-nucleoside-transporters-in-human-hepatoma-heparg-cells
#15
Abdullah Mayati, Amélie Moreau, Elodie Jouan, Marie Febvre-James, Claire Denizot, Yannick Parmentier, Olivier Fardel
The HepaRG cell line is a highly differentiated human hepatoma cell line, displaying the expression of various drug transporters. However, functional expression of nucleoside transporters remains poorly characterized in HepaRG cells, although these transporters play a key role in hepatic uptake of antiviral and anticancer drugs. The present study was, therefore, designed to characterize the expression, activity and regulation of equilibrative (ENT) and concentrative (CNT) nucleoside transporter isoforms in differentiated HepaRG cells...
November 21, 2018: Pharmaceutics
https://www.readbyqxmd.com/read/30463361/-n-2-hydroxy-propyl-3-trimethylammonium-o-mysristoyl-chitosan-enhances-the-solubility-and-intestinal-permeability-of-anticancer-curcumin
#16
Daniella S Silva, Danilo M Dos Santos, Andreia Almeida, Leonardo Marchiori, Sérgio P Campana-Filho, Sidney J L Ribeiro, Bruno Sarmento
An amphiphilic derivative of chitosan containing quaternary ammonium and myristoyl groups, herein named as ammonium myristoyl chitosan (DMCat), was synthesized by reacting glycidyltrimethylammonium chloride (GTMAC) and myristoyl chitosan (DMCh). The success of the modification was confirmed using Fourier-transform infrared spectroscopy (FTIR) and ¹H nuclear magnetic resonance (NMR) spectroscopy. The average degrees of alkylation and quaternization ( D Q ¯ ) were determined by using ¹H NMR and conductometric titration...
November 20, 2018: Pharmaceutics
https://www.readbyqxmd.com/read/30463341/anionic-long-circulating-quantum-dots-for-long-term-intravital-vascular-imaging
#17
Haolu Wang, Haotian Yang, Zhi Ping Xu, Xin Liu, Michael S Roberts, Xiaowen Liang
A major impediment to the long-term in vivo vascular imaging is a lack of suitable probes and contrast agents. Our developed mercaptosuccinic acid (MSA) capped cadmium telluride/cadmium sulfide (CdTe/CdS) ultrasmall quantum dots (QDs) have high fluorescent quantum yield, long fluorescence lifetime and long half-life in blood, allowing high resolution long-term intravital vascular imaging. In this study, we showed that these QDs can be used to visualize the in vivo the vasculature in normal and cancerous livers in mice using multiphoton microscopy (MPM) coupled with fluorescence lifetime imaging (FLIM), with cellular resolution (~1 µm) up to 36 h after intravenous injection...
November 20, 2018: Pharmaceutics
https://www.readbyqxmd.com/read/30463329/development-of-paroxetine-hydrochloride-single-layer-controlled-release-tablets-based-on-3%C3%A2-factorial-design
#18
Yao Yang, Zhengwei Huang, Xuan Zhang, Jinyuan Li, Ying Huang, Wanxin Chen, Xin Pan, Chuanbin Wu
Major depressive disorder (MDD) is one of the main contributors to disability and suicide mortality globally. Paroxetine hydrochloride (PHH) is the most potent antidepressant used for MDD treatment. Due to its reduced side effects PAXIL® CR is a widely-used controlled-release formulation of PHH. However, the complicated double-layer production of PAXIL® CR faces the risk of layer separation. In this study, PHH enteric coating single layer controlled-release tablets (PHH-EC-SLTs) were designed as a simplified substitution of PAXIL® CR through a rational formulation screening...
November 20, 2018: Pharmaceutics
https://www.readbyqxmd.com/read/30463290/diatoms-green-nanotechnology-for-biosilica-based-drug-delivery-systems
#19
REVIEW
Monica Terracciano, Luca De Stefano, Ilaria Rea
Diatom microalgae are the most outstanding natural source of porous silica. The diatom cell is enclosed in a three-dimensional (3-D) ordered nanopatterned silica cell wall, called frustule. The unique properties of the diatom frustule, including high specific surface area, thermal stability, biocompatibility, and tailorable surface chemistry, make diatoms really promising for biomedical applications. Moreover, they are easy to cultivate in an artificial environment and there is a large availability of diatom frustules as fossil material (diatomite) in several areas of the world...
November 20, 2018: Pharmaceutics
https://www.readbyqxmd.com/read/30453699/comparative-study-on-excretive-characterization-of-main-components-in-herb-pair-notoginseng-safflower-and-single-herbs-by-lc%C3%A2-ms-ms
#20
Ying-Yuan Lu, Jin-Yang Song, Yan Li, Yu-Qing Meng, Ming-Bo Zhao, Yong Jiang, Peng-Fei Tu, Xiao-Yu Guo
The herbal medicine combination of notoginseng-safflower has been commonly used clinically for the prevention and treatment of cardiovascular diseases. A reliable liquid chromatography-tandem mass spectrometry (LC⁻MS/MS) method was developed for simultaneous determination of six bioactive components (hydroxysafflor yellow A, notoginsenoide R1, ginsenoside Rb1, Re, Rd, and Rg1) in rat urine and feces after oral administration of notoginseng total saponins (NS), safflower total flavonoids (SF), and the combination of NS and SF (CNS)...
November 18, 2018: Pharmaceutics
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