journal
MENU ▼
Read by QxMD icon Read
search

Pharmaceutical Research

journal
https://www.readbyqxmd.com/read/27928647/triple-drug-combination-of-zidovudine-efavirenz-and-lamivudine-loaded-lactoferrin-nanoparticles-an-effective-nano-first-line-regimen-for-hiv-therapy
#1
Prashant Kumar, Yeruva Samrajya Lakshmi, Anand K Kondapi
PURPOSE: To enhance efficacy, bioavailability and reduce toxicity of first-line highly active anti-retroviral regimen, zidovudine + efavirenz + lamivudine loaded lactoferrin nanoparticles were prepared (FLART-NP) and characterized for physicochemical properties, bioactivity and pharmacokinetic profile. METHODS: Nanoparticles were prepared using sol-oil protocol and characterized using different sources such as FE-SEM, AFM, NanoSight, and FT-IR. In-vitro and in-vivo studies have been done to access the encapsulation-efficiency, cellular localization, release kinetics, safety analysis, biodistribution and pharmacokinetics...
December 7, 2016: Pharmaceutical Research
https://www.readbyqxmd.com/read/27928646/preparation-physicochemical-characterization-and-anti-fungal-evaluation-of-nystatin-loaded-plga-glucosamine-nanoparticles
#2
Ghobad Mohammadi, Amineh Shakeri, Ali Fattahi, Pardis Mohammadi, Ali Mikaeili, Alireza Aliabadi, Khosro Adibkia
PURPOSE: Nystatin loaded PLGA and PLGA-Glucosamine nanoparticles were formulated. PLGA were functionalized with Glucosamine (PLGA-GlcN) to enhance the adhesion of nanoparticles to Candida Albicans (C.albicans) cell walls. METHOD: Quasi-emulsion solvent diffusion method was employed using PLGA and PLGA-GlcN with various drug-polymer ratios for the preparation of nanoparticles. The nanoparticles were evaluated for size, zeta potential, polydispersity index, drug crystallinity, loading efficiency and release properties...
December 7, 2016: Pharmaceutical Research
https://www.readbyqxmd.com/read/27896592/why-have-clinical-trials-of-antioxidants-to-prevent-neurodegeneration-failed-a-cellular-investigation-of-novel-phenothiazine-type-antioxidants-reveals-competing-objectives-for-pharmaceutical-neuroprotection
#3
Maike J Ohlow, Selina Sohre, Matthias Granold, Mathias Schreckenberger, Bernd Moosmann
PURPOSE: Only a fraction of the currently established low-molecular weight antioxidants exhibit cytoprotective activity in living cells, which is considered a prerequisite for their potential clinical usefulness in Parkinson's disease or stroke. Post hoc structure-activity relationship analyses have predicted that increased lipophilicity and enhanced radical stabilization could contribute to such cytoprotective activity. METHODS: We have synthesized a series of novel phenothiazine-type antioxidants exhibiting systematic variation in their lipophilicity and radical stabilization...
November 28, 2016: Pharmaceutical Research
https://www.readbyqxmd.com/read/27896591/design-and-in-vitro-evaluation-of-bispecific-complexes-and-drug-conjugates-of-anticancer-peptide-lyp-1-in-human-breast-cancer
#4
Selin Seda Timur, Prashant Bhattarai, Reyhan Neslihan Gürsoy, İmran Vural, Ban-An Khaw
PURPOSE: LyP-1, a nine-amino-acid tumor homing peptide, selectively binds to its cognate receptor, p32. Overexpression of p32 in certain tumors should allow use of LyP-1 as a targeting agent for the delivery of therapeutic or diagnostic agents. Peptide conjugates are developed for enhanced pre-targeting of MDA-MB-231 breast cancer cells with peptide-antibody bispecific complexes and targeting with multiple-drug/-fluorophore-conjugated nano-polymers. METHODS: LyP-1-anti-DTPA bispecific antibody complexes (LyP-1-bsAbCx) were generated by conjugation of anti-DTPA antibody and LyP-1...
November 28, 2016: Pharmaceutical Research
https://www.readbyqxmd.com/read/27896590/improvement-in-thermal-stability-of-sucralose-by-%C3%AE-cyclodextrin-metal-organic-frameworks
#5
Nana Lv, Tao Guo, Botao Liu, Caifen Wang, Vikaramjeet Singh, Xiaonan Xu, Xue Li, Dawei Chen, Ruxandra Gref, Jiwen Zhang
PURPOSE: To explain thermal stability enhancement of an organic compound, sucralose, with cyclodextrin based metal organic frameworks. METHODS: Micron and nanometer sized basic CD-MOFs were successfully synthesized by a modified vapor diffusion method and further neutralized with glacial acetic acid. Sucralose was loaded into CD-MOFs by incubating CD-MOFs with sucralose ethanol solutions. Thermal stabilities of sucralose-loaded basic CD-MOFs and neutralized CD-MOFs were investigated using thermogravimetric analysis (TGA), differential scanning calorimetry (DSC) and high performance liquid chromatography with evaporative light-scattering detection (HPLC-ELSD)...
November 28, 2016: Pharmaceutical Research
https://www.readbyqxmd.com/read/27896589/lipid-nanoparticles-loaded-with-an-antisense-oligonucleotide-gapmer-against-bcl-2-for-treatment-of-lung-cancer
#6
Xinwei Cheng, Qibing Liu, Hong Li, Chen Kang, Yang Liu, Tianqi Guo, Ke Shang, Chengyun Yan, Guang Cheng, Robert J Lee
PURPOSE: Bcl-2 is an anti-apoptotic gene that is frequently overexpressed in human cancers. G3139 is an antisense oligonucleotide against bcl-2 that has shown limited efficacy in clinical trials. Here, we report the synthesis of a new antisense oligonucleotide containing additional chemical modifications and its delivery using nanoparticles. METHODS: An oligonucleotide G3139-GAP was synthesized, which has 2'-O-methyl nucleotides at the 5' and 3' ends based on a "gapmer" design...
November 28, 2016: Pharmaceutical Research
https://www.readbyqxmd.com/read/27896588/electrosprayed-myocet-like-liposomes-an-alternative-to-traditional-liposome-production
#7
Michael A Collier, Eric M Bachelder, Kristy M Ainslie
PURPOSE: Although doxorubicin (DXR) has been on the market for many years as an anti-cancer drug, a number of serious dose-limiting toxicities hinder its widespread use. To reduce the known toxicities of soluble DXR, various liposomes have been designed including Doxil, Caelyx, and Myocet. Myocet, a non-PEGylated liposomal formulation containing DXR, was found to reduce the toxicities associated with soluble DXR and has been used in Europe and Canada (but not the US) as a first line therapy...
November 28, 2016: Pharmaceutical Research
https://www.readbyqxmd.com/read/27873146/comparison-of-dialysis-and-solvatofluorochromism-based-methods-to-determine-drug-release-rates-from-polymer-nanoassemblies
#8
Derek Reichel, Younsoo Bae
PURPOSE: To compare traditional dialysis- and novel solvatofluorochromism (SFC)-based methods for accurate determination of drug release profiles for nanoparticle drug carriers. METHODS: Polymer nanoassemblies (PNAs) varying in drug release patterns were prepared using poly(ethylene glycol), poly(ethylenimine), hydrophobic excipients (palmitate and deoxycholate), and model hydrophobic anticancer drugs with clinical relevance (carfilzomib and docetaxel). Nile blue (NB) was used as a model SFC dye quenching fluorescence in water yet emitting strong fluorescence in the presence of hydrophobic drugs within PNAs...
November 21, 2016: Pharmaceutical Research
https://www.readbyqxmd.com/read/27864744/a-generic-multi-compartmental-cns-distribution-model-structure-for-9-drugs-allows-prediction-of-human-brain-target-site-concentrations
#9
Yumi Yamamoto, Pyry A Välitalo, Dirk-Jan van den Berg, Robin Hartman, Willem van den Brink, Yin Cheong Wong, Dymphy R Huntjens, Johannes H Proost, An Vermeulen, Walter Krauwinkel, Suruchi Bakshi, Vincent Aranzana-Climent, Sandrine Marchand, Claire Dahyot-Fizelier, William Couet, Meindert Danhof, Johan G C van Hasselt, Elizabeth C M de Lange
PURPOSE: Predicting target site drug concentration in the brain is of key importance for the successful development of drugs acting on the central nervous system. We propose a generic mathematical model to describe the pharmacokinetics in brain compartments, and apply this model to predict human brain disposition. METHODS: A mathematical model consisting of several physiological brain compartments in the rat was developed using rich concentration-time profiles from nine structurally diverse drugs in plasma, brain extracellular fluid, and two cerebrospinal fluid compartments...
November 18, 2016: Pharmaceutical Research
https://www.readbyqxmd.com/read/27858218/bleomycin-coated-microneedles-for-treatment-of-warts
#10
Han Sol Lee, Ha Ryeong Ryu, Joo Young Roh, Jung-Hwan Park
PURPOSE: Bleomycin-coated microneedles were devised for delivery of bleomycin into the sub-epidermal skin layer for the treatment of warts in order to provide patient convenience and reduce patient pain and fear. METHOD: Poly-lactic-acid (L-PLA) microneedles were fabricated by a molding process and then the tips were partially coated using a dip-coating method based on a microstructure well. The mechanical strength of the pre-coated polymer microneedles was observed by inserting them in porcine foot and back skin...
November 17, 2016: Pharmaceutical Research
https://www.readbyqxmd.com/read/27858217/alternative-animal-and-non-animal-models-for-drug-discovery-and-development-bonus-or-burden
#11
Irlan Almeida Freires, Janaina de Cássia Orlandi Sardi, Ricardo Dias de Castro, Pedro Luiz Rosalen
Mammalian models have served as a basis for R&D over the past decades. Nevertheless, these models are expensive, laborious, may yield results that cannot always be translated into the human in vivo situation and, more recently, have reverberated great social and ethical dilemmas. Hence, the prospect of changes in the global scientific scenario and the Three Rs principle (Reduction, Replacement and Refinement) have encouraged the development of alternative methods to the use of mammals. Despite the efforts, suitable alternative tests are not available in all areas of biomedical research, as regulatory acceptance requires time, prior validation and robust financial and scientific investment...
November 17, 2016: Pharmaceutical Research
https://www.readbyqxmd.com/read/27848167/increased-active-tumor-targeting-by-an-%C3%AE-v%C3%AE-3-targeting-and-cell-penetrating-bifunctional-peptide-mediated-dendrimer-based-conjugate
#12
Pengkai Ma, Huajun Yu, Xuemei Zhang, Hongjie Mu, Yongchao Chu, Ling Ni, Pingping Xing, Yiyun Wang, Kaoxiang Sun
PURPOSE: A bifunctional RGDTAT peptide-modified PEG-PAMAM dendrimer conjugate RGDTAT-PEG-PAMAM (RTPP) was established for the targeted treatment of αvβ3-overexpressing tumor cells. METHODS: The RGDTAT peptide was synthesized and attached to PAMAM using PEG to construct the RTPP conjugate. The methotrexate (MTX) encapsulated RTPPM complex was prepared and characterized by dynamic light scattering (DLS), transmission electron microscopy (TEM) and in vitro release...
November 15, 2016: Pharmaceutical Research
https://www.readbyqxmd.com/read/27844187/multifractal-characterization-of-pharmaceutical-hot-melt-extrudates
#13
Camille Adler, Alexandra Teleki, Martin Kuentz
PURPOSE: Multifractal geometry has become a powerful tool to describe complex structures in many fields. Our first aim was to combine imaging and multifractal analysis to better understand the microstructure of pharmaceutical extrudates. A second objective was to study erosion/dispersion behavior of the formulations because it would condition release of any drug. METHODS: Different formulations containing a lipid, a polymer and different silica based inorganic carriers were produced by hot-melt extrusion at various screw speeds...
November 14, 2016: Pharmaceutical Research
https://www.readbyqxmd.com/read/27837522/contrasting-the-influence-of-cationic-amino-acids-on-the-viscosity-and-stability-of-a-highly-concentrated-monoclonal-antibody
#14
Barton J Dear, Jessica J Hung, Thomas M Truskett, Keith P Johnston
PURPOSE: To explain the effects of cationic amino acids and other co-solutes on the viscosity, stability and protein-protein interactions (PPI) of highly concentrated (≥200 mg/ml) monoclonal antibody (mAb) solutions to advance subcutaneous injection. METHODS: The viscosities of ≥200 mg/ml mAb1 solutions with various co-solutes and pH were measured by capillary rheometry in some cases up to 70,000 s(-1). The viscosities are analyzed in terms of dilute PPI characterized by diffusion interaction parameters (k D ) from dynamic light scattering (DLS)...
November 11, 2016: Pharmaceutical Research
https://www.readbyqxmd.com/read/27822852/the-tritiated-water-skin-barrier-integrity-test-considerations-for-acceptance-criteria-with-and-without-14-c-octanol
#15
Paul A Lehman, Kacie Beatch, Sam G Raney, Thomas J Franz
PURPOSE: A study was designed to assess barrier integrity simultaneously using separate compounds (probes) for polar and non-polar pathways through the skin, (3)H2O and (14)C-octanol, respectively; and to determine whether the two probe approach could better define barrier integrity. METHODS: A 5-min dose of water containing (3)H2O and (14)C -octanol was applied to ex vivo human skin mounted in Franz diffusion cells. The receptor solution was sampled at 30 min, analyzed for (3)H and (14)C content, and the correlation between water and octanol absorption was determined by statistical tests suitable for non-normally distributed data...
November 7, 2016: Pharmaceutical Research
https://www.readbyqxmd.com/read/27822851/spect-ct-comparison-of-lung-deposition-using-a-system-combining-a-vibrating-mesh-nebulizer-with-a-valved-holding-chamber-and-a-conventional-jet-nebulizer-a-randomized-cross-over-study
#16
Jonathan Dugernier, Michel Hesse, Rita Vanbever, Virginie Depoortere, Jean Roeseler, Jean-Bernard Michotte, Pierre-François Laterre, François Jamar, Gregory Reychler
PURPOSE: To compare in vivo the total and regional pulmonary deposition of aerosol particles generated by a new system combining a vibrating-mesh nebulizer with a specific valved holding chamber and constant-output jet nebulizer connected to a corrugated tube. METHODS: Cross-over study comparing aerosol delivery to the lungs using two nebulizers in 6 healthy male subjects: a vibrating-mesh nebulizer combined with a valved holding chamber (Aerogen Ultra®, Aerogen Ltd...
November 7, 2016: Pharmaceutical Research
https://www.readbyqxmd.com/read/27822850/population-pharmacokinetics-pk-and-pharmacodynamics-pd-analysis-of-ly3015014-a-monoclonal-antibody-to-protein-convertase-subtilisin-kexin-type-9-pcsk9-in-healthy-subjects-and-hypercholesterolemia-patients
#17
Tong Shen, Douglas E James, Kathryn A Krueger
PURPOSE: LY3015014 is a humanized immunoglobulin G4 (IgG4) monoclonal antibody that binds to the catalytic domain of PCSK9 and reduce low-density lipoprotein cholesterol (LDL-C) in patients with hypercholesterolemia that is poorly controlled by maximally tolerated statin therapy. The objective of this pharmacokinetic/pharmacodynamics (PK/PD) analysis was to characterize the PK and PD properties of LY3015014 and assess the effect of covariates on the LY3015014 PK-PD profiles. METHODS: Single and multiple dose data from three phase1 studies in healthy subjects (n = 133), as well as a phase 2 study in hypercholesterolemia patients (n = 527) were combined into a single dataset for analysis...
November 7, 2016: Pharmaceutical Research
https://www.readbyqxmd.com/read/27822849/physicochemical-properties-of-solid-phospholipid-particles-as-a-drug-delivery-platform-for-improving-oral-absorption-of-poorly-soluble-drugs
#18
Kohsaku Kawakami, Aoi Miyazaki, Mayuko Fukushima, Keiko Sato, Yuko Yamamura, Kohta Mohri, Shinji Sakuma
PURPOSE: A novel drug delivery platform, mesoporous phospholipid particle (MPP), is introduced. Its physicochemical properties and ability as a carrier for enhancing oral absorption of poorly soluble drugs are discussed. METHODS: MPP was prepared through freeze-drying a cyclohexane/t-butyl alcohol solution of phosphatidylcholine. Its basic properties were revealed using scanning electron microscopy, x-ray diffraction, thermal analysis, hygroscopicity measurement, and so on...
November 7, 2016: Pharmaceutical Research
https://www.readbyqxmd.com/read/27815791/comparative-study-of-different-nano-formulations-of-curcumin-for-reversal-of-doxorubicin-resistance-in-k562r-cells
#19
Tapan K Dash, V Badireenath Konkimalla
PURPOSE: Curcumin is very well established as a chemo-therapeutic, chemo-preventive and chemo-sensitizing agent in diverse disease conditions. As the isolated pure form has poor solubility and pharmacokinetic problems, therefore it is encapsulated in to several nano-formulations to improve its bioavailability. Here in the current study, we aim to compare different nano-formulations of curcumin for their chemo-sensitizing activity in doxorubicin (DOX) resistant K562 cells. METHODS: Four different curcumin formulations were prepared namely DMSO assisted curcumin nano-dispersion (CurD, 260 nm), liposomal curcumin (CurL, 165 nm), MPEG-PCL micellar curcumin (CurM, 18 nm) and cyclodextrin encapsulated curcumin (CurN, 37 nm)...
November 4, 2016: Pharmaceutical Research
https://www.readbyqxmd.com/read/27800572/intracellular-delivery-of-nanobodies-for-imaging-of-target-proteins-in-live-cells
#20
Ruth Röder, Jonas Helma, Tobias Preiß, Joachim O Rädler, Heinrich Leonhardt, Ernst Wagner
PURPOSE: Cytosolic delivery of nanobodies for molecular target binding and fluorescent labeling in living cells. METHODS: Fluorescently labeled nanobodies were formulated with sixteen different sequence-defined oligoaminoamides. The delivery of formulated anti-GFP nanobodies into different target protein-containing HeLa cell lines was investigated by flow cytometry and fluorescence microscopy. Nanoparticle formation was analyzed by fluorescence correlation spectroscopy...
October 31, 2016: Pharmaceutical Research
journal
journal
28799
1
2
Fetch more papers »
Fetching more papers... Fetching...
Read by QxMD. Sign in or create an account to discover new knowledge that matter to you.
Remove bar
Read by QxMD icon Read
×

Search Tips

Use Boolean operators: AND/OR

diabetic AND foot
diabetes OR diabetic

Exclude a word using the 'minus' sign

Virchow -triad

Use Parentheses

water AND (cup OR glass)

Add an asterisk (*) at end of a word to include word stems

Neuro* will search for Neurology, Neuroscientist, Neurological, and so on

Use quotes to search for an exact phrase

"primary prevention of cancer"
(heart or cardiac or cardio*) AND arrest -"American Heart Association"