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Pharmaceutics

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https://www.readbyqxmd.com/read/29232856/resveratrol-loaded-lipid-nanocarriers-correlation-between-in-vitro-occlusion-factor-and-in-vivo-skin-hydrating-effect
#1
Lucia Montenegro, Carmela Parenti, Rita Turnaturi, Lorella Pasquinucci
Lipid nanocarriers show occlusive properties that may be related to their ability to improve skin hydration. The aim of this work was to evaluate the relationship between in vitro occlusion factor and in vivo skin hydration for three types of lipid nanocarriers: nanoemulsions (NEs), solid lipid nanoparticles (SLNs) and nanostructured lipid carriers (NLCs). These lipid nanocarriers were loaded with trans-resveratrol (RSV) and incorporated in gel vehicles. In vitro occlusion factor was in the order SLNs > NLCs > NEs...
December 10, 2017: Pharmaceutics
https://www.readbyqxmd.com/read/29215597/application-of-pharmacokinetics-modelling-to-predict-human-exposure-of-a-cationic-liposomal-subunit-antigen-vaccine-system
#2
Raj K S Badhan, Swapnil Khadke, Yvonne Perrie
The pharmacokinetics of a liposomal subunit antigen vaccine system composed of the cationic lipid dimethyldioctadecylammonium bromide (DDA) and the immunostimulatory agent trehalose 6,6-dibehenate (TDB) (8:1 molar ratio) combined with the Ag85B-ESAT-6 (H1) antigen were modelled using mouse in-vivo data. Compartment modelling and physiologically based pharmacokinetics (PBPK) were used to predict the administration site (muscle) and target site (lymph) temporal concentration profiles and factors governing these...
December 7, 2017: Pharmaceutics
https://www.readbyqxmd.com/read/29211047/a-chitosan-based-liposome-formulation-enhances-the-in-vitro-wound-healing-efficacy-of-substance-p-neuropeptide
#3
Tamara Mengoni, Manuela Adrian, Susana Pereira, Beatriz Santos-Carballal, Mathias Kaiser, Francisco M Goycoolea
Currently, there is considerable interest in developing innovative biodegradable nanoformulations for controlled administration of therapeutic proteins and peptides. Substance P (SP) is a neuropeptide of 11 amino acids that belongs to the tachykinins family and it plays an important role in wound healing. However, SP is easily degradable in vivo and has a very short half-life, so the use of chitosan-based nanocarriers could enhance its pharmaceutical properties. In light of the above, the aim of this work was to produce and characterize chitosan-coated liposomes loaded with SP (SP-CH-LP) as novel biomaterials with potential application in mucosal wound healing...
December 6, 2017: Pharmaceutics
https://www.readbyqxmd.com/read/29206148/a-comparative-study-of-coupled-preferential-crystallizers-for-the-efficient-resolution-of-conglomerate-forming-enantiomers
#4
Aniruddha Majumder, Zoltan K Nagy
The separation of enantiomers is of great importance due to their possible differences in therapeutic properties. Preferential crystallization in various configurations of coupled batch crystallizers is used as an attractive means to separate the conglomerate-forming enantiomers from racemic mixtures. However, the productivity of such batch processes can be limited by the nucleation of the counter enantiomer and consumption of the supersaturation. In this work, a recently proposed process configuration, which uses coupled mixed suspension mixed product removal (MSMPR) with liquid phase exchange, is investigated by simulation studies...
December 5, 2017: Pharmaceutics
https://www.readbyqxmd.com/read/29194387/preparation-and-characterization-of-cabamazepine-cocrystal-in-polymer-solution
#5
Hao Zhang, Ying Zhu, Ning Qiao, Yang Chen, Linghuan Gao
In this study, we attempted to prepare carbamazepine (CBZ) cocrystal through the solution method in ethanol-water solvent mixture (volume ratio 1:1) and polyvinyl pyrrolidone (PVP) solution. Nicotinamide (NIC) and saccharin (SAC) were selected as cocrystal coformers. Cocrystal screening products were characterized by Fourier Transform Infrared Spectroscopy (FTIR), Differential Scanning Calorimetry (DSC), and Powder X-ray Diffraction (PXRD) techniques. Characterization results show that in ethanol-water solvent mixture, pure CBZ-NIC cocrystal can be prepared, while CBZ-SAC cocrystal cannot be obtained...
December 1, 2017: Pharmaceutics
https://www.readbyqxmd.com/read/29156634/an-overview-of-chitosan-nanoparticles-and-its-application-in-non-parenteral-drug-delivery
#6
REVIEW
Munawar A Mohammed, Jaweria T M Syeda, Kishor M Wasan, Ellen K Wasan
The focus of this review is to provide an overview of the chitosan based nanoparticles for various non-parenteral applications and also to put a spotlight on current research including sustained release and mucoadhesive chitosan dosage forms. Chitosan is a biodegradable, biocompatible polymer regarded as safe for human dietary use and approved for wound dressing applications. Chitosan has been used as a carrier in polymeric nanoparticles for drug delivery through various routes of administration. Chitosan has chemical functional groups that can be modified to achieve specific goals, making it a polymer with a tremendous range of potential applications...
November 20, 2017: Pharmaceutics
https://www.readbyqxmd.com/read/29156554/a-high-performance-liquid-chromatography-assay-method-for-the-determination-of-lidocaine-in-human-serum
#7
Hamdah M Al Nebaihi, Matthew Primrose, James S Green, Dion R Brocks
Here we report on the development of a selective and sensitive high-performance liquid chromatographic method for the determination of lidocaine in human serum. The extraction of lidocaine and procainamide (internal standard) from serum (0.25 mL) was achieved using diethyl ether under alkaline conditions. After liquid-liquid extraction, the separation of analytes was accomplished using reverse phase extraction. The mobile phase, a combination of acetonitrile and monobasic potassium phosphate, was pumped isocratically through a C18 analytical column...
November 18, 2017: Pharmaceutics
https://www.readbyqxmd.com/read/29120380/in-vitro-phase-i-metabolism-of-crv431-a-novel-oral-drug-candidate-for-chronic-hepatitis-b
#8
Daniel J Trepanier, Daren R Ure, Robert T Foster
The cytochrome P450-mediated Phase I in vitro metabolism of CRV431 was studied using selective chemical inhibition and recombinant human enzymes. Additionally, the metabolic profile of CRV431 in human, rat, and monkey liver microsomes was investigated. Liver microsomes were incubated for 0-80 min with CRV431, and the metabolite profile was assessed by electrospray ionization liquid chromatography mass spectrometry (ESI-LCMS). CRV431 was extensively metabolized through oxidation to produce various hydroxylated and demethylated species...
November 9, 2017: Pharmaceutics
https://www.readbyqxmd.com/read/29099779/self-emulsifying-granules-and-pellets-composition-and-formation-mechanisms-for-instant-or-controlled-release
#9
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/29064386/the-role-of-pxr-genotype-and-transporter-expression-in-the-placental-transport-of-lopinavir-in-mice
#10
Sarabjit S Gahir, Micheline Piquette-Miller
Lopinavir (LPV), an antiretroviral protease inhibitor frequently prescribed in HIV-positive pregnancies, is a substrate of Abcb1 and Abcc2. As differences in placental expression of these transporters were seen in Pregnane X Receptor (PXR) -/- mice, we examined the impact of placental transporter expression and fetal PXR genotype on the fetal accumulation of LPV. PXR +/- dams bearing PXR +/+, PXR +/-, and PXR -/- fetuses were generated by mating PXR +/- female mice with PXR +/- males. On gestational day 17, dams were administered 10 mg/kg LPV (i...
October 24, 2017: Pharmaceutics
https://www.readbyqxmd.com/read/29065483/rosemary-essential-oil-loaded-lipid-nanoparticles-in-vivo-topical-activity-from-gel-vehicles
#11
Lucia Montenegro, Lorella Pasquinucci, Agata Zappalà, Santina Chiechio, Rita Turnaturi, Carmela Parenti
Although rosemary essential oil (EO) shows many biological activities, its topical benefits have not been clearly demonstrated. In this work, we assessed the effects on skin hydration and elasticity of rosemary EO after topical application via gel vehicles in human volunteers. To improve its topical efficacy, rosemary EO was loaded into lipid nanoparticles (NLCs) consisting of cetyl palmitate as a solid lipid, and non-ionic surfactants. Such NLCs were prepared using different ratios of EO/solid lipid and those containing EO 3% w/w and cetyl pamitate 7% w/w were selected for in vivo studies, showing the best technological properties (small particle size, low polydispersity index and good stability)...
October 21, 2017: Pharmaceutics
https://www.readbyqxmd.com/read/29039750/modeling-of-body-weight-metrics-for-effective-and-cost-efficient-conventional-factor-viii-dosing-in-hemophilia-a-prophylaxis
#12
Alanna McEneny-King, Pierre Chelle, Severine Henrard, Cedric Hermans, Alfonso Iorio, Andrea N Edginton
The total body weight-based dosing strategy currently used in the prophylactic treatment of hemophilia A may not be appropriate for all populations. The assumptions that guide weight-based dosing are not valid in overweight and obese populations, resulting in overdosing and ineffective resource utilization. We explored different weight metrics including lean body weight, ideal body weight, and adjusted body weight to determine an alternative dosing strategy that is both safe and resource-efficient in normal and overweight/obese adult patients...
October 17, 2017: Pharmaceutics
https://www.readbyqxmd.com/read/29036899/targeting-strategies-for-the-combination-treatment-of-cancer-using-drug-delivery-systems
#13
REVIEW
Janel Kydd, Rahul Jadia, Praveena Velpurisiva, Aniket Gad, Shailee Paliwal, Prakash Rai
Cancer cells have characteristics of acquired and intrinsic resistances to chemotherapy treatment-due to the hostile tumor microenvironment-that create a significant challenge for effective therapeutic regimens. Multidrug resistance, collateral toxicity to normal cells, and detrimental systemic side effects present significant obstacles, necessitating alternative and safer treatment strategies. Traditional administration of chemotherapeutics has demonstrated minimal success due to the non-specificity of action, uptake and rapid clearance by the immune system, and subsequent metabolic alteration and poor tumor penetration...
October 14, 2017: Pharmaceutics
https://www.readbyqxmd.com/read/29023392/disposition-metabolism-and-histone-deacetylase-and-acetyltransferase-inhibition-activity-of-tetrahydrocurcumin-and-other-curcuminoids
#14
Júlia T Novaes, Ryan Lillico, Casey L Sayre, Kalyanam Nagabushnam, Muhammed Majeed, Yufei Chen, Emmanuel A Ho, Ana Luísa de P Oliveira, Stephanie E Martinez, Samaa Alrushaid, Neal M Davies, Ted M Lakowski
Tetrahydrocurcumin (THC), curcumin and calebin-A are curcuminoids found in turmeric (Curcuma longa). Curcuminoids have been established to have a variety of pharmacological activities and are used as natural health supplements. The purpose of this study was to identify the metabolism, excretion, antioxidant, anti-inflammatory and anticancer properties of these curcuminoids and to determine disposition of THC in rats after oral administration. We developed a UHPLC-MS/MS assay for THC in rat serum and urine. THC shows multiple redistribution phases with corresponding increases in urinary excretion rate...
October 12, 2017: Pharmaceutics
https://www.readbyqxmd.com/read/29023376/altered-protein-expression-of-cardiac-cyp2j-and-hepatic-cyp2c-cyp4a-and-cyp4f-in-a-mouse-model-of-type-ii-diabetes-a-link-in-the-onset-and-development-of-cardiovascular-disease
#15
Benoit Drolet, Sylvie Pilote, Carolanne Gélinas, Alida-Douce Kamaliza, Audrey Blais-Boilard, Jessica Virgili, Dany Patoine, Chantale Simard
Arachidonic acid can be metabolized by cytochrome P450 (CYP450) enzymes in a tissue- and cell-specific manner to generate vasoactive products such as epoxyeicosatrienoic acids (EETs-cardioprotective) and hydroxyeicosatetraenoic acids (HETEs-cardiotoxic). Type II diabetes is a well-recognized risk factor for developing cardiovascular disease. A mouse model of Type II diabetes (C57BLKS/J-db/db) was used. After sacrifice, livers and hearts were collected, washed, and snap frozen. Total proteins were extracted...
October 12, 2017: Pharmaceutics
https://www.readbyqxmd.com/read/29019915/revolutionizing-therapeutic-drug-monitoring-with-the-use-of-interstitial-fluid-and-microneedles-technology
#16
REVIEW
Tony K L Kiang, Sahan A Ranamukhaarachchi, Mary H H Ensom
While therapeutic drug monitoring (TDM) that uses blood as the biological matrix is the traditional gold standard, this practice may be impossible, impractical, or unethical for some patient populations (e.g., elderly, pediatric, anemic) and those with fragile veins. In the context of finding an alternative biological matrix for TDM, this manuscript will provide a qualitative review on: (1) the principles of TDM; (2) alternative matrices for TDM; (3) current evidence supporting the use of interstitial fluid (ISF) for TDM in clinical models; (4) the use of microneedle technologies, which is potentially minimally invasive and pain-free, for the collection of ISF; and (5) future directions...
October 11, 2017: Pharmaceutics
https://www.readbyqxmd.com/read/28994701/study-of-statin-and-loratadine-induced-muscle-pain-mechanisms-using-human-skeletal-muscle-cells
#17
Yat Hei Leung, Jacques Turgeon, Veronique Michaud
Many drugs can cause unexpected muscle disorders, often necessitating the cessation of an effective medication. Inhibition of monocarboxylate transporters (MCTs) may potentially lead to perturbation of l-lactic acid homeostasis and muscular toxicity. Previous studies have shown that statins and loratadine have the potential to inhibit l-lactic acid efflux by MCTs (MCT1 and 4). The main objective of this study was to confirm the inhibitory potentials of atorvastatin, simvastatin (acid and lactone forms), rosuvastatin, and loratadine on l-lactic acid transport using primary human skeletal muscle cells (SkMC)...
October 10, 2017: Pharmaceutics
https://www.readbyqxmd.com/read/28954416/predicting-oral-drug-absorption-mini-review-on-physiologically-based-pharmacokinetic-models
#18
REVIEW
Louis Lin, Harvey Wong
Most marketed drugs are administered orally, despite the complex process of oral absorption that is difficult to predict. Oral bioavailability is dependent on the interplay between many processes that are dependent on both compound and physiological properties. Because of this complexity, computational oral physiologically-based pharmacokinetic (PBPK) models have emerged as a tool to integrate these factors in an attempt to mechanistically capture the process of oral absorption. These models use inputs from in vitro assays to predict the pharmacokinetic behavior of drugs in the human body...
September 26, 2017: Pharmaceutics
https://www.readbyqxmd.com/read/28954402/tissue-specific-modulation-of-cyp2c-and-cyp3a-mrna-levels-and-activities-by-diet-induced-obesity-in-mice-the-impact-of-type-2-diabetes-on-drug-metabolizing-enzymes-in-liver-and-extra-hepatic-tissues
#19
Sarah Maximos, Michel Chamoun, Sophie Gravel, Jacques Turgeon, Veronique Michaud
Various diseases such as type 2 diabetes (T2D) may alter drug clearance. The objective of this study was to evaluate the effects of T2D on CYP450 expressions and activities using high-fat diet (HFD) as a model of obesity-dependent diabetes in C57BL6 mice. The cyp450 mRNA expression levels for 15 different isoforms were determined in the liver and extra-hepatic tissues (kidneys, lungs and heart) of HFD-treated animals (n = 45). Modulation of cyp450 metabolic activities by HFD was assessed using eight known substrates for specific human ortholog CYP450 isoforms: in vitro incubations were conducted with liver and extra-hepatic microsomes...
September 26, 2017: Pharmaceutics
https://www.readbyqxmd.com/read/28946666/nanotechnologies-in-pancreatic-cancer-therapy
#20
REVIEW
Ayesha Manzur, Adeolu Oluwasanmi, Darren Moss, Anthony Curtis, Clare Hoskins
Pancreatic cancer has been classified as a cancer of unmet need. After diagnosis the patient prognosis is dismal with few surviving over 5 years. Treatment regimes are highly patient variable and often the patients are too sick to undergo surgical resection or chemotherapy. These chemotherapies are not effective often because patients are diagnosed at late stages and tumour metastasis has occurred. Nanotechnology can be used in order to formulate potent anticancer agents to improve their physicochemical properties such as poor aqueous solubility or prolong circulation times after administration resulting in improved efficacy...
September 25, 2017: Pharmaceutics
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