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Molecular Pharmaceutics

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https://www.readbyqxmd.com/read/28548840/acceleration-of-crystal-growth-of-amorphous-griseofulvin-by-low-concentration-poly-ethylene-oxide-aspects-of-crystallization-kinetics-and-molecular-mobility
#1
Qin Shi, Chen Zhang, Yuan Su, Jie Zhang, Dongshan Zhou, Ting Cai
This study aims to investigate the crystallization behavior and molecular dynamics of amorphous griseofulvin (GSF) in the presence of low-concentration poly (ethylene oxide) (PEO). We observe that the addition of 3 % w/w PEO remarkably increases the crystal growth rate of GSF by two orders of magnitude, in both the supercooled liquid and glassy states. The liquid dynamics of amorphous GSF in the presence and absence of PEO are characterized by dielectric spectroscopy. With an increase of the PEO content, the α-relaxation times of the systems decrease, indicating the increase of global molecular mobility...
May 26, 2017: Molecular Pharmaceutics
https://www.readbyqxmd.com/read/28499338/hyaluronic-acid-molecular-weight-dependent-modulation-of-mucin-nanostructure-for-potential-mucosal-therapeutic-applications
#2
Irene M Hansen, Morten F Ebbesen, Liselotte Kaspersen, Troels Thomsen, Konrad Bienk, Yunpeng Cai, Birgitte Mølholm Malle, Kenneth A Howard
This study investigates the effects of different molecular weight hyaluronic acids (HAs) on the mucosal nanostructure using a pig stomach mucin hydrogel as a mucosal barrier model. Microparticles (1.0 μm) and nanoparticles (200 nm) were used as probes, and their movement in mucin was studied by a three-dimensional confocal microscopy-based particle tracking technique and by Nanoparticle Tracking Analysis (NTA) after addition of high-molecular weight (900 kDa) and low-molecular weight (33 kDa) HA. This demonstrated a molecular weight-dependent HA modulation of the mucin nanostructure with a 2...
May 26, 2017: Molecular Pharmaceutics
https://www.readbyqxmd.com/read/28544850/pcpp-adjuvanted-respiratory-syncytial-virus-rsv-sf-subunit-vaccine-self-assembled-supramolecular-complexes-enable-enhanced-immunogenicity-and-protection
#3
Corinne Cayatte, Alexander Marin, Gaurav Manohar Rajani, Kirsten Schneider-Ohrum, Angie Snell Bennett, Jason D Marshall, Alexander K Andrianov
PCPP, a well-defined polyphosphazene macromolecule, has been studied as an immunoadjuvant for a soluble form of the post-fusion glycoprotein (RSV sF) of RSV, which is an attractive vaccine candidate for inducing RSV-specific immunity in mice and humans. We demonstrate that RSV sF-PCPP formulations induce high neutralization titers to RSV comparable to Alum formulations even at a low PCPP dose and protect animals against viral challenge both in the lung and upper respiratory tract. PCPP formulations were also characterized by Th1-biased responses, compared to Th2-biased responses that are more typical for RSV sF alone or RSV sF-Alum formulations, suggesting an inherent immunostimulating activity of the polyphosphazene adjuvant...
May 25, 2017: Molecular Pharmaceutics
https://www.readbyqxmd.com/read/28544846/genomic-dna-interactions-mechanize-peptidotoxin-mediated-anti-cancer-nanotherapy
#4
Santosh K Misra, Aaron S Schwartz-Duval, Dipanjan Pan
Host defense peptides (HDPs) are a class of evolutionarily conserved substances of the innate immune response that has been identified as major players in the defense system in many living organisms. Some of the HDPs are also referred as peptidotoxins which offer immense potential for anti-cancer therapy. However, their therapeutic potential is yet to be fully translated mainly due to their off-target toxicity. Here we show that their nano-enabled delivery may become beneficial in controlling their delivery in intra-cellular space...
May 25, 2017: Molecular Pharmaceutics
https://www.readbyqxmd.com/read/28538101/chemical-endgroup-modified-diblock-copolymers-elucidate-anchor-and-chain-mechanism-of-membrane-stabilization
#5
Evelyne M Houang, Karen J Haman, Mihee Kim, Wenjia Zhang, Dawn A Lowe, Yuk Yin Sham, Timothy P Lodge, Benjamin J Hackel, Frank S Bates, Joseph M Metzger
Block copolymers can be synthesized in an array of architectures and compositions to yield diverse chemical properties. The triblock copolymer Poloxamer 188 (P188), the family archetype, consisting of a hydrophobic polypropylene oxide core flanked by hydrophilic polyethylene oxide chains, can stabilize cellular membranes during stress. However, little is known regarding the molecular basis of membrane interaction by copolymers in living organisms. By leveraging diblock architectural design, discrete end-group chemistry modifications can be tested...
May 24, 2017: Molecular Pharmaceutics
https://www.readbyqxmd.com/read/28493712/stimulus-responsive-degradable-polylactide-based-block-copolymer-nanoassemblies-for-controlled-enhanced-drug-delivery
#6
Kamaljeet K Bawa, Jung Kwon Oh
Polylactide (PLA) is biocompatible and FDA-approved for clinical use and thus has been a choice of the materials valuable for extensive applications in biomedical fields. However, conventionally designed PLA-based amphiphilic block copolymer (ABP) nanoassemblies exhibit slow and uncontrolled release of encapsulated drugs because of the slow biodegradation of hydrophobic PLA in physiological conditions. To improve potentials for clinical use and commercialization of conventional PLA-based nanoassemblies, stimulus-responsive degradation (SRD) platform has been introduced into the design of PLA-based nanoassemblies for enhanced/controlled release of encapsulated drugs...
May 23, 2017: Molecular Pharmaceutics
https://www.readbyqxmd.com/read/28502177/leveraging-colloidal-aggregation-for-drug-rich-nanoparticle-formulations
#7
Ahil N Ganesh, Jennifer Logie, Christopher K McLaughlin, Benjamin L Barthel, Tad H Koch, Brian K Shoichet, Molly S Shoichet
While limited drug loading continues to be problematic for chemotherapeutics formulated in nanoparticles, we found that we could take advantage of colloidal drug aggregation to achieve high loading when combined with polymeric excipients. We demonstrate this approach with two drugs, fulvestrant and pentyl-PABC doxazolidine (PPD; a prodrug of doxazolidine, which is a DNA cross-linking anthracycline), and two polymers, polysorbate 80 (UP80) and poly(d,l-lactide-co-2-methyl-2-carboxytrimethylene carbonate)-graft-poly(ethylene glycol) (PLAC-PEG; a custom-synthesized, self-assembling amphiphilic polymer)...
May 19, 2017: Molecular Pharmaceutics
https://www.readbyqxmd.com/read/28475834/expanding-transdermal-delivery-with-lipid-nanoparticles-a-new-drug-in-nlc-in-adhesive-design
#8
M Mendes, S C C Nunes, J J Sousa, A A C C Pais, C Vitorino
A monolithic drug-in-NLC-in-adhesive transdermal patch, with a novel design, was developed for codelivery of olanzapine (OL) and simvastatin (SV). Nanostructured lipid carriers (NLC) and enhancers were used as passive strategies, while the pretreatment of the skin with Dermaroller was tested as an active approach. The formulation was optimized for composition in a quality by design basis, in terms of enhancer and adhesive, with focus on permeation behavior, adhesion properties, and cytotoxicity. Propylene glycol promoted the best permeation rate for both drugs, with enhancement ratios of 8...
May 19, 2017: Molecular Pharmaceutics
https://www.readbyqxmd.com/read/28520445/telodendrimers-for-physical-encapsulation-and-covalent-linking-of-individual-or-combined-therapeutics
#9
Ashok Kakkar, Jason Choi, Alexandre Moquin, Enzo Bomal, Li Na, Dusica Maysinger
New therapeutics for glioblastoma multiforme and our ability to deliver them using efficient nanocarriers, constitute topical areas of research. We report a comparative study of temozolomide and quercetin in the treatment of glioblastoma (GBM) in 3D, and their incorporation into micelles obtained from synthetically articulated architectural copolymers, and a commercially available linear polymer poly(ethylene glycol)-poly(lactic-co-glycolic acid) (PEG-PLGA). A versatile synthetic methodology to telodendrimers which can be easily adapted to the needs of other therapeutic interventions, is presented...
May 18, 2017: Molecular Pharmaceutics
https://www.readbyqxmd.com/read/28520436/controlling-structure-and-function-of-polymeric-drug-delivery-nanoparticles-using-microfluidics
#10
Aman Bains, Yimeng Cao, Sundiata Kly, Jeremy E Wulff, Matthew G Moffitt
We demonstrate control of multiscale structure and drug delivery function for paclitaxel (PAX)-loaded polycaprolactone-block-poly(ethylene oxide) (PCL-b-PEO) polymeric nanoparticles (PNPs) via synthesis and flow-directed shear processing in a two-phase gas-liquid microfluidic reactor. This strategy takes a page from the engineering of commodity plastics, where processing rather than polymer chemistry provides an experimental handle on properties and function. PNPs formed from copolymers with three different PCL block lengths show sizes, morphologies, and loading efficiencies that depend on both the PCL block length and the microfluidic flow rate...
May 18, 2017: Molecular Pharmaceutics
https://www.readbyqxmd.com/read/28489944/studying-the-crystallization-of-various-polymorphic-forms-of-nifedipine-from-binary-mixtures-with-the-use-of-different-experimental-techniques
#11
O Madejczyk, E Kaminska, M Tarnacka, M Dulski, K Jurkiewicz, K Kaminski, M Paluch
In this paper the crystal growth of nifedipine from pure system and from binary mixtures composed of active substance (API) and two acetylated disaccharides, maltose and sucrose (NIF-acMAL, NIF-acSUC, 5:1 weight ratio), was investigated. Optical snapshots supported by X-ray diffraction (XRD) and Fourier transform infrared spectroscopy (FTIR) measurements showed that mainly β and α forms of nifedipine grow up in all investigated samples. They also revealed that the morphology of growing crystals strongly depends on the presence of modified carbohydrates and temperature conditions...
May 18, 2017: Molecular Pharmaceutics
https://www.readbyqxmd.com/read/28481116/overcoming-the-road-blocks-advancement-of-block-copolymer-micelles-for-cancer-therapy-in-the-clinic
#12
Loujin Houdaihed, James C Evans, Christine Allen
With countless preclinical studies on block copolymer micelles (BCMs) successfully demonstrating the superiority of these advanced drug delivery formulations over conventional formulations, it remains somehow discouraging that only a few have reached clinical evaluation and practice. With a critical eye, this review aims to compare and summarize the preclinical and clinical data available on several BCM formulations and to identify their primary role in drug delivery as "carrier" or "solubilizer". This review focuses on polymeric micelles that have reached clinical evaluation and/or are being pursued commercially...
May 18, 2017: Molecular Pharmaceutics
https://www.readbyqxmd.com/read/28514853/targeting-the-central-nervous-system-cns-a-review-of-rabies-virus-targeting-strategies
#13
Mira Oswald, Simon Geissler, Achim Goepferich
The transport of drugs across the blood-brain barrier is challenging. The use of peptide sequences derived from viruses with a central nervous system (CNS) tropism is one elegant option. A prominent example is the rabies virus glycopeptide-29 (RVG-29), which is said to enable a targeted brain delivery. Although the entry mechanism of the rabies virus into the CNS is very well characterized, it is unknown whether RVG-29-functionalized drug delivery systems (DDSs) follow this pathway. RVG-29-functionalized DDSs present themselves with modifications of the RVG-29 peptide sequence and different physicochemical properties compared to the rabies virus...
May 17, 2017: Molecular Pharmaceutics
https://www.readbyqxmd.com/read/28514851/blood-brain-barrier-penetrating-biologic-tnf-%C3%AE-inhibitor-for-alzheimer-s-disease
#14
Rudy Chang, Jillian Knox, Jae Chang, Aram Derbedrossian, Vitaly Vasilevko, David Cribbs, Ruben J Boado, William M Pardridge, Rachita Sumbria
OBJECTIVE: Tumor necrosis factor alpha (TNF-α) driven processes are involved at multiple stages of Alzheimer's disease (AD) pathophysiology and disease progression. Biologic TNF-α inhibitors (TNFIs) are the most potent class of TNFIs but cannot be developed for AD since these macromolecules do not cross the blood-brain barrier (BBB). A BBB-penetrating TNFI was engineered by the fusion of the extracellular domain of the type II human TNF receptor (TNFR) to a chimeric monoclonal antibody (MAb) against the mouse transferrin receptor (TfR), designated as the cTfRMAb-TNFR fusion protein...
May 17, 2017: Molecular Pharmaceutics
https://www.readbyqxmd.com/read/28513167/quercetin-luteolin-phloretin-and-morin-are-dietary-flavonoid-inhibitors-of-monocarboxylate-transporter-6
#15
Robert Spencer Jones, Mark Parker, Marilyn Emily Morris
Monocarboxylate transporter 6 (MCT6; SLC16A5) has been recognized for its role as a xenobiotic transporter, with characterized substrates probenecid, bumetanide, and nateglinide. To date, the impact of commonly ingested dietary compounds on MCT6 function has not been investigated and therefore, the objective of this study was to evaluate a variety of flavonoids for their potential MCT6-specific interactions. Flavonoids are a large group of polyphenolic phytochemicals found in commonly consumed plant-based products that have been recognized for their dietary health benefits...
May 17, 2017: Molecular Pharmaceutics
https://www.readbyqxmd.com/read/28485947/impact-of-supramolecular-aggregation-on-the-crystallization-kinetics-of-organic-compounds-from-the-supercooled-liquid-state
#16
Arjun Kalra, Patrick Tishmack, Joseph W Lubach, Eric J Munson, Lynne S Taylor, Stephen R Byrn, Tonglei Li
Despite numerous challenges in their theoretical description and practical implementation, amorphous drugs are of growing importance to the pharmaceutical industry. One such challenge is to gain molecular level understanding of the propensity of a molecule to form and remain as a glassy solid. In this study, a series of structurally similar diarylamine compounds was examined to elucidate the role of supramolecular aggregation on crystallization kinetics from supercooled liquid state. The structural similarity of the compounds makes it easier to isolate the molecular features that affect crystallization kinetics and glass forming ability of these compounds...
May 17, 2017: Molecular Pharmaceutics
https://www.readbyqxmd.com/read/28471177/topical-formulation-of-self-assembled-antiviral-prodrug-nanomicelles-for-targeted-retinal-delivery
#17
Abhirup Mandal, Kishore Cholkar, Varun Khurana, Ankit Shah, Vibhuti Agrahari, Rohit Bisht, Dhananjay Pal, Ashim K Mitra
Topical drug administration for back of the eye delivery is extremely challenging due to the presence of protection mechanisms and physiological barriers. Self-assembled polymeric nanomicelles have emerged as promising vehicles for drug delivery. Apart from serving as an inert nanocarrier for therapeutic agents, polymeric nanomicelles are known to bypass mononuclear phagocytic system (MPS) and efflux transporters thereby improving drug bioavailability. In this investigation, a highly efficacious biotinylated lipid prodrug of cyclic cidofovir (B-C12-cCDF) was formulated within polymeric nanomicelles as a carrier for targeted retinal delivery...
May 17, 2017: Molecular Pharmaceutics
https://www.readbyqxmd.com/read/28510455/clinically-relevant-multidrug-transporters-are-regulated-by-micrornas-along-the-human-intestine
#18
Henrike Bruckmueller, Paul Martin, Meike Kaehler, Sierk Haenisch, Marek Ostrowski, Marek Drozdzik, Werner Siegmund, Ingolf Cascorbi, Stefan Oswald
Intestinal drug transporters are crucial determinants for absorption and oral bioavailability of drugs. In healthy tissue donators, a recent study revealed profound discrepancies between mRNA expression and protein abundance as well as differences in the protein content between small and large intestine for clinically relevant multidrug transporters as the ATP binding cassette transporter subfamily B member 1 (ABCB1) and subfamily C member 3 (ABCC3) and the solute carrier family 15 member 1 (SLC15A1, PEPT1)...
May 16, 2017: Molecular Pharmaceutics
https://www.readbyqxmd.com/read/28506066/de-novo-computational-design-for-development-of-a-peptide-ligand-oriented-to-vegfr-3-with-high-affinity-and-long-circulation
#19
Hong M Li, Zhi P Dong, Qi Y Wang, Li X Liu, Bing X Li, Xiao N Ma, Ming S Lin, Tao Lu, Yue Wang
The overexpression of VEGFR-3 is correlated with a worse prognosis in lung cancer and has been regarded as a rational target for specific drug delivery. Here, VEGFR-3 homing peptide library was efficiently established by computational design. Strong fluorescent signal of selected peptides were observed in A549 cells, but much weaker in other cells. The positive immunostaining overlapped with VEGFR-3 confirmed high affinity and selectivity of one novel peptide (CP-7). In addition, cell uptake of FITC-CP-7 peptide was significantly blocked by co-injection of excess CP-7 peptide...
May 16, 2017: Molecular Pharmaceutics
https://www.readbyqxmd.com/read/28505463/in-vivo-pretargeted-imaging-of-her2-and-tag-72-expression-using-the-halotag-enzyme
#20
James C Knight, Michael Mosley, H Tetsuo Uyeda, Mei Cong, Frank Fan, Stephen Faulkner, Bart Cornelissen
A novel pretargeted SPECT imaging strategy based on the HaloTag enzyme has been evaluated for the first time in a living system. To determine the efficacy of this approach, two clinically relevant cancer biomarkers, HER2 and TAG-72, were selected to represent models of internalizing and non-internalizing antigens, respectively. In MDA-MB-231/H2N (HER2-expressing) and LS174T (TAG-72-expressing) xenograft tumors in mice, pretargeting experiments were performed in which HaloTag-conjugated derivatives of the antibodies Trastuzumab (anti-HER2) or CC49 (anti-TAG-72) were utilized as primary agents, and the small molecule HaloTag ligands 111In-HTL-1, -2, and -3 were evaluated as secondary agents...
May 15, 2017: Molecular Pharmaceutics
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