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Molecular Pharmaceutics

Adrienn Kazsoki, P Eacute Ter Szab Oacute, Attila Domján, Attila Balázs, Tamás Bozó, Miklós Kellermayer, Attila Farkas, Diána Balogh-Weiser, Balázs Pinke, András Darcsi, Szabolcs Béni, János Madarász, Lajos Szente, Romana Zelko
The electrospun nanofiber-based orally dissolving webs are promising candidates for rapid drug release, which is due to the high surface area to volume ratio of the fibers and the high amorphization efficacy of the fiber formation process. Although latter is responsible for the physical and/or chemical instability of these systems. The primary aim of the present study was to elucidate how the addition of polysorbate 80 (PS80) and hydroxypropyl-β-cyclodextrin (HP-β-CD) influenced the electrospinning process, the properties and behavior of the obtained nanofibers...
July 19, 2018: Molecular Pharmaceutics
Jitendra Wankar, Francesca Bonvicini, Gabor Benkovics, Valentina Marassi, Milo Malanga, Eva Fenyvesi, Giovanna Angela Gentilomi, Pierluigi Reschiglian, Barbara Roda, Ilse Manet
Clofazimine (CLZ) is an antibiotic with promising behavior against gram positive bacteria however the drug is completely insoluble in water and accumulates in fat tissues. We explored nanocarriers, labeled and not with rhodamine, consisting of negatively charged sulfobutylether-β-cyclodextrins for CLZ loading. A new oligomeric carrier was obtained crosslinking βCyD with epichlorohydrin followed by sulfonation in strongly alkaline aqueous medium. The oligomeric carrier has MW of 53 kDa, and forms small nanoparticles of few tens of nm...
July 19, 2018: Molecular Pharmaceutics
Eric Kissi, Georgia Kasten, Korbinian Loebmann, Thomas Rades, Holger Grohganz
The improved physical stability associated with co-amorphous drug-amino acid (AA) formulations may indicate a decrease in mobility of the amorphous drug molecules, compared to the neat amorphous form of the drug. Since the characteristic glass transition temperatures (Tgα and Tgβ) represent molecular mobility in amorphous systems, we aimed to characterise Tgα and Tgβ, and to determine their role in physical stability as well as their potential usefulness to determine the presence of an excess component (either drug or AA) in co-amorphous systems...
July 18, 2018: Molecular Pharmaceutics
Se-Na Kim, Song Ah Ko, Chun Gwon Park, Seung Ho Lee, Beom Kang Huh, Yoh Han Park, Young Kook Kim, Ahnul Ha, Ki Ho Park, Young Bin Choy
To treat glaucoma, conventional eye drops are often prescribed. However, the eye drops have limited effectiveness as a result of low drug bioavailability due to their rapid clearance from the preocular space. To resolve this, we proposed amino-functionalized mesoporous silica (AMS) particles as delivery carriers of the glaucoma drug, brimonidine. Because of the presence of mesopores, brimonidine (BMD) could be encapsulated in the AMS with a loading amount of 41.73 μg/mg (i.e., drug loading capacity of about 4...
July 18, 2018: Molecular Pharmaceutics
Shrawan Baghel, Helen Cathcart, Niall J O'Reilly
The formulation of oral amorphous solid dispersions (ASD) includes the use of excipients to improve physical stability and enhance bioavailability. Combinations of excipients (polymers and surfactants) are often employed in pharmaceutical products to improve the delivery of poorly water-soluble drugs. However, additive interactions in multi-component ASD systems have not been extensively studied and may promote crystallization in an unpredictable manner, which in turn may affect the physical stability and dissolution profile of the product...
July 18, 2018: Molecular Pharmaceutics
David A Hirsh, Yongchao Su, Haichen Nie, Wei Xu, Dirk Stueber, Narayan Variankaval, Robert W Schurko
Reliable methods for the characterization of drug substances are critical for evaluating their stability and bioavailability, especially in dosage formulations under varying storage conditions and usage. Such methods must provide information on the molecular identities and structures of drug substances and any potential by-products of the formulation process, as well as providing a means of quantifying the relative amounts of these substances. For example, active pharmaceutical ingredients (APIs) are often formulated as ionic salts to improve the pharmaceutical properties of dosage forms; however, exposure of such formulations to elevated temperature and/or humidity can trigger the conversion of an ionic salt of an API to a neutral form with different properties, through a process known as disproportionation...
July 17, 2018: Molecular Pharmaceutics
Qi Li, Jiayong Yang, Yilin Chen, Xinyi Zhou, Dengyue Chen, Yang Li, Xuan Zhu
Combination cancer therapy with various kinds of therapeutic approaches could improve the effectiveness of treatment while reducing side effects. Herein, we elaborately developed a theranostics nano-platform based on magnetic polydopamine (MPDA) coated with hyaluronic acid-methotrexate conjugates (MPDA@HA-MTX) for chemo-photothermal treatment (PTT). In this nano-platform, Fe3O4 served as the core was applied as contrast agent for T2-weighted magnetic resonance imaging (MRI) and early-phase magnet targeting...
July 16, 2018: Molecular Pharmaceutics
Alexander Wurzer, Julia Pollmann, Alexander Schmidt, Dominik Reich, Hans-Jürgen Wester, Johannes Notni
Radiopharmaceuticals targeting the enzyme prostate-specific membrane antigen (PSMA; synonyms: glutamate carboxypeptidase II, NAALADase; EC have recently emerged as powerful agents for diagnosis and therapy (theranostics) of prostate carcinoma (PCa). The radiation doses for therapeutic application of such compounds are limited by substantial uptakes in kidneys and salivary glands, with excess doses reportedly leading to radiotoxicity-related adverse effects, such as kidney insufficiency or xenostomia...
July 16, 2018: Molecular Pharmaceutics
Yijia Yin, Qian Hu, Chenfeng Xu, Qi Qiao, Xianya Qin, Qingle Song, Yang Peng, Yongdan Zhao, Zhiping Zhang
A dual-sensitive nanoparticle delivery system was constructed by incorporating acid sensitive hydrazone linker into thermosensitive nanoparticles (TSNs) for co-encapsulating doxorubicin (DOX) and interferon γ (IFNγ), to realize co-delivery of chemotherapy and immunotherapy agents against melanoma. DOX, a chemotherapeutic drug, was conjugated to TSNs by a pH-sensitive chemical bond and IFNγ, a potent immune-modulator, was absorbed into TSNs through the thermosensitivity and electrostatics of nanoparticles...
July 16, 2018: Molecular Pharmaceutics
Lili Wu, Weichao Han, Yulian Chen, Tao Zhang, Junjin Liu, Shilong Zhong, Han Liu, Congcong Han, Zhongyi Zhang, Shu-Wen Liu, Lan Tang
Emodin is a main anthraquinone compound which exists in Chinese traditional medicines including Polygonum multiflorum and Rhubarb. It is documented to have obvious liver and kidney toxicity. This study aims to (a) estimate gender differences of hepatotoxicity and toxicokinetics in rats after oral administration of emodin (60 and 150 mg/kg/d) for consecutive 28 days; (b) clarify relative mechanisms caused by glucuronidation and disposition. Hepatotoxicity was significantly higher in female rats than that in male rats as evidenced by histopathological and biochemical tests...
July 16, 2018: Molecular Pharmaceutics
Mario Ficker, Matthijs J M Theeuwen, Anna Janaszewska, Michal Gorzkiewicz, Søren W Svenningsen, Barbara Klajnert-Maculewicz, Jørn B Christensen
COX-2 inhibitors such as Non-steroidal anti-inflammatory drugs (NSAIDs) are the most common treatment for chronic inflammatory diseases like arthritis and atherosclerosis. However, they are associated with severe side effects such as cardiovascular events or stomach bleeding, due to co-inhibition of other enzymes (COX1) and off target accumulation. PAMAM-dendrimers can solubilize these lipophilic drugs and increase their bioavailability; furthermore PAMAM dendrimers seem to have some per se accumulation in inflammatory sides...
July 16, 2018: Molecular Pharmaceutics
Tao Xi, Hai Liu, Wei Liu, Zhoulin Tan, Zhiqin Zeng, Huimin Yang, Shuanghui Luo, Linlin Wang, Yingying Xing
The immunogenicity of oral subunit vaccines is poor partly due to the harsh milieu of gastrointestinal (GI) tract. For some pathogens that restrictedly inhabit in GI tract, a vaccine that works in situ may provide more potent protection than that vaccinates parenterally. Yet, none appropriate delivery system is available for oral subunit vaccines. In this study, we designed HP55/Poly(n-butylcyanoacrylate) (PBCA) nanoparticles (NPs) to carry Helicobacter pylori (H. pylori) subunit vaccine CCF for oral administration in a prophylactic mice model...
July 16, 2018: Molecular Pharmaceutics
Daheui Choi, Jin Chan Park, Ha Na Lee, Ji-Hoi Moon, Hyo-Won Ahn, Kwangyong Park, Jinkee Hong
Chalcone derivatives have been investigated for therapeutic agent such as anticancer, antioxidant and anti-inflammatory fields. In this study, we also have synthesized 4 different type of chalcone derivatives and demonstrated in vitro bioactivities. We divided into 2 groups of chalcones on the basis of similar substituents at aromatic rings and tested cell viability and proliferation potentials, indicating that methoxy substituent on A ring could enhance cytotoxicity and anti-proliferation potential depending on chalcone concentration...
July 16, 2018: Molecular Pharmaceutics
Yoni Donner, Stéphane Kazmierczak, Kristen Fortney
Computational drug repositioning requires assessment of the functional similarities among compounds. Here, we report a new method for measuring compound functional similarity based on gene expression data. This approach takes advantage of deep neural networks to learn an embedding that substantially denoises expression data, making replicates of the same compound more similar. Our method uses unlabeled data in the sense that it only requires compounds to be labeled by identity rather than detailed pharmacological information, which is often unavailable and costly to obtain...
July 12, 2018: Molecular Pharmaceutics
Tannaz Ramezanli, Bozena B Michniak-Kohn
In this study we aimed to develop a semisolid formulation of polymeric nanoparticles loaded with adapalene to enhance the efficacy and improve the skin tolerability in acne therapy. An amphiphilic and biocompatible copolymer that self-assembles to nanospheres (known as TyroSpheres) was used to encapsulate adapalene and increase its solubility. A water soluble viscous agent was applied to prepare gel formulation of adapalene loaded-TyroSpheres (Adapalene-TyroSphere). Particle size, morphology, homogeneity and rheological characteristics of the Adapalene-TyroSphere gel formulations were studied...
July 11, 2018: Molecular Pharmaceutics
Mulham Alfatama, Lee Yong Lim, Tin Wui Wong
Simple alginate, alginate-stearic acid and alginate-C18 conjugate nanoparticles, and tripolyphosphate-crosslinked chitosan-oleic acid conjugate-coated calcium alginate beads as the vehicle of nanoparticles were designed. Their size, zeta potential, morphology, drug load, drug release, matrix molecular characteristics, mucus penetration, HT-29 cell line cytotoxicity and intracellular trafficking, in vivo blood glucose lowering and insulin delivery profiles were characterized. Alginate-C18 conjugate nanoparticles were non-toxic...
July 11, 2018: Molecular Pharmaceutics
Aaron J Courtenay, Maelíosa T C McCrudden, Kathryn J McAvoy, Helen O McCarthy, Ryan F Donnelly
Bevacizumab is a recombinant humanised monoclonal antibody used clinically as a combination chemotherapeutic. Antibody therapeutics are usually formulated as parenteral injections, owing to their low oral bioavailability. Microneedle technology provides a transdermal alternative for drug-delivery using micron-scale needle structures to penetrate directly through the stratum corneum into the dermal interstitium. This study describes the design, formulation and in vitro characterisation of both dissolving and hydrogel-forming microneedle array platforms for transdermal delivery of bevacizumab...
July 11, 2018: Molecular Pharmaceutics
Paresh P Chothe, Shu-Pei Wu, Zhengqi Ye, Niresh Hariparsad
The use of in vitro data for the quantitative prediction of transporter-mediated clearance is critical. Central to this evaluation is the use of hepatocytes since they contain the full complement of transporters and metabolic enzymes. In general, uptake clearance (CLuptake) is evaluated by measuring appearance of compound in the cell. Passive clearance (CLpd) is often determined by conducting parallel studies at 4°C or by attempting to saturate uptake pathways. Both approaches have their limitations. Recent studies have proposed the use Rifamycin-SV (RFV) as a pan-inhibitor of hepatic uptake pathways...
July 11, 2018: Molecular Pharmaceutics
Mariya A Pindrus, Steven J Shire, Sandeep Yadav, Devendra S Kalonia
PURPOSE: To determine the effect of solution conditions, especially low ionic strength, on the dynamics of molecular diffusion and protein-protein interactions in monoclonal antibody solutions. METHODS: The interaction parameter, kD, was calculated from diffusion data obtained from Dynamic Light Scattering (DLS) measurements performed using a Zetasizer®. Theoretical considerations were utilized to evaluate the hard sphere and electrostatic contribution to molecular interactions...
July 11, 2018: Molecular Pharmaceutics
Gaoang Ren, Wei Bao, Zhiping Zeng, Weidong Zhang, Ce Shang, Maosi Wang, Ying Su, Xiao-Kun Zhang, Hu Zhou
Bexarotene, an agonist of retinoid X receptor alpha (RXRα), has been shown to increase the expression of apoE, ABCA1 and ABCG1 by activating RXR/LXR and RXR/PPAR heterodimers, resulting in amyloid β (Aβ)-protein clearance in the brain of an Alzheimer's Disease (AD) mouse model and reversal of mouse cognitive deficits. Nitrostyrene derivative Z-10 is the first identified nitro-ligand of RXRα. We hypothesized that Z-10 and its derivatives have the similar effect as bexarotene. A series of Z-10 derivatives were synthesized by introducing methyl, hydroxyl, and methoxy groups in 2- or 4- position of naphthalene ring, respectively...
July 11, 2018: Molecular Pharmaceutics
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