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https://www.readbyqxmd.com/read/29679751/solubilitydetermination-of-raloxifene-hydrochloride-in-ten-pure-solvents-at-various-temperatures-thermodynamics-based-analysis-and-solute-solvent-interactions
#1
Abdul Ahad, Faiyaz Shakeel, Omar Ali Alfaifi, Mohammad Raish, Ajaz Ahmad, Fahad I Al-Jenoobi, Abdullah M Al-Mohizea
The purpose of the present study was to determine the solubility of raloxifene hydrochloride (RHCl) in ten solvents: water, ethanol, isopropyl alcohol (IPA), ethylene glycol (EG), propylene glycol (PG), polyethylene glycol-400 (PEG-400), Transcutol, 1-butanol, dimethyl sulfoxide (DMSO), and ethyl acetate (EA) at temperatures of 298.2-323.2 K and a pressure of 0.1 MPa. The solubility data obtained was fitted upon "Apelblat and Van't Hoff" equations. The maximum mole fraction solubility of RHCl was obtained in DMSO (5...
April 18, 2018: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/29679725/achyranthis-bidentatae-radix-enhanced-articular-distribution-and-anti-inflammatory-effect-of-berberine-in-sanmiao-wan-using-an-acute-gouty-arthritis-rat-model
#2
Juan Wu, Jingya Li, Wei Li, Bei Sun, Jin Xie, Wenming Cheng, Qunlin Zhang
ETHNOPHARMACOLOGICAL RELEVANCE: Sanmiao Wan (SMW) has been a basic prescription employed for the treatment for gout in the clinic since Yuan dynasty. Achyranthis bidentatae radix (ABR) is designed as a lower-guiding drug in SMW to augment the articular accumulation of active ingredients and improve the anti-inflammatory effect. AIM OF THE STUDY: Present study was undertaken to investigate the dose-response relationship of berberine in SMW between the articular concentration and anti-inflammatory effect in the knee joint under the lower-guiding of ABR...
April 18, 2018: Journal of Ethnopharmacology
https://www.readbyqxmd.com/read/29679708/the-impact-of-polymers-on-3d-microstructure-and-controlled-release-of-sildenafil-citrate-from-hydrophilic-matrices
#3
Anna Krupa, Zbisław Tabor, Jacek Tarasiuk, Beata Strach, Krzysztof Pociecha, Elżbieta Wyska, Sebastian Wroński, Ewelina Łyszczarz, Renata Jachowicz
Sildenafil citrate has short biological half-life in humans. Thus, matrix tablets of controlled release were designed and prepared by compaction on the basis of hydrophilic polymers, i.e. HPMC, sodium alginate, carbomer, poloxamer and their mixtures. The impact of these polymers on sildenafil release in vitro and its pharmacokinetics in vivo was evaluated. Since drug release rate from hydrophilic matrices can be govern by the porosity of the matrix, the microstructure of tablets was studied using X-ray microcomputed tomography...
April 18, 2018: European Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/29679668/a-novel-peptide-ligand-rap12-of-lrp1-for-glioma-targeted-drug-delivery
#4
Huitong Ruan, Zhilan Chai, Qing Shen, Xishan Chen, Bingxia Su, Cao Xie, Changyou Zhan, Shengyu Yao, Huan Wang, Mingfei Zhang, Man Ying, Weiyue Lu
The receptor associated protein (RAP) is a 39 kDa chaperone protein, binding tightly to low-density lipoprotein receptor-related protein-1 (LRP1) that is overexpressed in glioma, tumor neovasculature, vasculogenic mimicry (VM), the blood-brain barrier (BBB) and the blood-brain tumor barrier (BBTB). Herein, we miniaturized the RAP protein into a short peptide RAP12 (EAKIEKHNHYQK) aiding by computer-aided peptide design technique. RAP12 contained the essential lysines at the positions 253 and 256. The binding affinity of RAP12 to LRP1 was theoretically and experimentally evaluated...
April 18, 2018: Journal of Controlled Release: Official Journal of the Controlled Release Society
https://www.readbyqxmd.com/read/29679667/systemic-delivery-of-bace1-sirna-through-neuron-targeted-nanocomplexes-for-treatment-of-alzheimer-s-disease
#5
Pengzhen Wang, Xiaoyao Zheng, Qian Guo, Peng Yang, Xiaoying Pang, Kang Qian, Wei Lu, Qizhi Zhang, Xinguo Jiang
β-site amyloid precursor protein cleaving enzyme 1 (BACE1) is a key enzyme to cleave the amyloid precursor protein to develop Alzheimer's disease (AD). Reducing BACE1 expression in central neuron through RNA interference technology shows great promise to overcome AD. However, to obtain an efficient and neurons-specific delivery of siRNA against BACE1 through systemic administration remains challenging. Here, we design and prepare siRNA nano-carriers based on PEGylated poly(2-(N,N-dimethylamino) ethyl methacrylate) (PEG-PDMAEMA) modified with both the CGN peptide for blood-brain barrier (BBB) penetration and the Tet1 peptide for neuron-specific binding...
April 18, 2018: Journal of Controlled Release: Official Journal of the Controlled Release Society
https://www.readbyqxmd.com/read/29679647/a-new-micro-holder-device-for-local-drug-delivery-during-in-vivo-whole-cell-recordings
#6
María Sáez, Maya Ketzef, Javier Alegre-Cortés, Ramón Reig, Gilad Silberberg
Focal administration of pharmacological agents during in vivo recordings is a useful technique to study the functional properties of neural microcircuits. However, the lack of visual control makes this task difficult and inaccurate, especially when targeting small and deep regions where spillover to neighboring regions is likely to occur. An additional problem with recording stability arises when combining focal drug administration with in vivo intracellular recordings, which are highly sensitive to mechanical vibrations...
April 18, 2018: Neuroscience
https://www.readbyqxmd.com/read/29679606/regulatory-pitfalls-and-opportunities-when-repurposing-for-inhalation-therapy
#7
Svetlana Lyapustina
This article reviews regulatory considerations for companies wishing to develop drugs for delivery via the respiratory tract (e.g., by oral inhalation or intranasally) using molecules previously approved for a different therapeutic indication and/or a different delivery route. Conceptually, such repurposing has many medical and business advantages, but turning promising ideas into real products requires overcoming a number of practical challenges. Obtaining regulatory approval to market a candidate product comes at the end of a product development, but being aware of the regulatory requirements is necessary before the development even starts...
April 18, 2018: Advanced Drug Delivery Reviews
https://www.readbyqxmd.com/read/29679596/observational-studies-of-inhaled-corticosteroid-effectiveness-in-copd-lessons-learned
#8
Samy Suissa, Pierre Ernst
BACKGROUND: Randomized controlled trials at times investigate findings suggested by observational studies. For example, the TORCH trial, which did not show a mortality reduction with inhaled corticosteroids (ICS) in chronic obstructive pulmonary disease (COPD), was motivated by some observational studies that suggested considerable reductions in mortality with these drugs. Reasons for these discrepancies are unclear. METHODS: We searched the literature to identify all observational studies, including cohort and case-control studies, investigating the effectiveness of ICS on major outcomes in COPD patients, including death and hospitalization for COPD...
April 18, 2018: Chest
https://www.readbyqxmd.com/read/29679485/identification-and-structure-elucidation-of-the-proresolving-mediators-provides-novel-leads-for-resolution-pharmacology
#9
REVIEW
Jesmond Dalli, Charles N Serhan
Inflammatory diseases are a major socioeconomic burden, with the incidence of such conditions on the rise, especially in western societies. For decades, the primary treatment paradigm for many of these conditions was to develop drugs that inhibit or antagonize the production and biological actions of molecules that were thought to be the culprits in propagating disease, these include cytokines and eicosanoids. This approach is effective in controlling disease propagation; however, long-term exposure to these anti-inflammatories is also associated with many side effects, some of which severe, including immune-suppression...
April 21, 2018: British Journal of Pharmacology
https://www.readbyqxmd.com/read/29679445/development-of-coumarin-and-benzofuran-conjugated-hybrids-as-the-versatile-multi-targeted-compounds-for-the-treatment-of-alzheimer-s-disease
#10
Asha Hiremathad, Karam Chand, Rangappa S Keri
Alzheimer's disease (AD), the most common cause of dementia, is a neurodegenerative disorder characterized by progressive deterioration of memory and cognition. The evidenced multi-factorial nature of AD has been considered the main reason for the absence of cure so far. Therefore, the development of novel hybrids to treat the disease is very much essential. Focusing on this, a novel series of coumarin-benzofuran conjugated hybrids have been designed and screened as anti-Alzheimer's disease agents. The strategy is to obtain an effective mimetic of donepezil, which is acetylcholnesterase inhibitor...
April 20, 2018: Chemical Biology & Drug Design
https://www.readbyqxmd.com/read/29679356/regional-variations-in-immunosuppressive-therapy-in-patients-with-primary-nephrotic-syndrome-the-japan-nephrotic-syndrome-cohort-study
#11
Ryohei Yamamoto, Enyu Imai, Shoichi Maruyama, Hitoshi Yokoyama, Hitoshi Sugiyama, Kosaku Nitta, Tatsuo Tsukamoto, Shunya Uchida, Asami Takeda, Toshinobu Sato, Takashi Wada, Hiroki Hayashi, Yasuhiro Akai, Megumu Fukunaga, Kazuhiko Tsuruya, Kosuke Masutani, Tsuneo Konta, Tatsuya Shoji, Takeyuki Hiramatsu, Shunsuke Goto, Hirofumi Tamai, Saori Nishio, Arimasa Shirasaki, Kojiro Nagai, Kunihiro Yamagata, Hajime Hasegawa, Hidemo Yasuda, Shizunori Ichida, Tomohiko Naruse, Kei Fukami, Tomoya Nishino, Hiroshi Sobajima, Satoshi Tanaka, Toshiyuki Akahori, Takafumi Ito, Terada Yoshio, Ritsuko Katafuchi, Shouichi Fujimoto, Hirokazu Okada, Eiji Ishimura, Junichiro James Kazama, Keiju Hiromura, Tetsushi Mimura, Satashi Suzuki, Yosuke Saka, Tadashi Sofue, Yusuke Suzuki, Yugo Shibagaki, Kiyoki Kitagawa, Kunio Morozumi, Yoshiro Fujita, Makoto Mizutani, Takashi Shigematsu, Naoki Kashihara, Hiroshi Sato, Seiichi Matsuo, Ichiei Narita, Yoshitaka Isaka
BACKGROUND: The lack of high-quality clinical evidences hindered broad consensus on optimal therapies for primary nephrotic syndromes. The aim of the present study was to compare prevalence of immunosuppressive drug use in patients with primary nephrotic syndrome across 6 regions in Japan. METHODS: Between 2009 and 2010, 380 patients with primary nephrotic syndrome in 56 hospitals were enrolled in a prospective cohort study [Japan Nephrotic Syndrome Cohort Study (JNSCS)], including 141, 151, and 38 adult patients with minimal change disease (MCD), membranous nephropathy (MN), and focal segmental glomerulosclerosis (FSGS), respectively...
April 20, 2018: Clinical and Experimental Nephrology
https://www.readbyqxmd.com/read/29679159/notch-1-sirna-and-methotrexate-towards-a-multifunctional-approach-in-rhematoid-arthritis-management-a-nanomedicine-approach
#12
Guang Zhao, Haifei Zhang
PURPOSE: Rheumatoid arthritis (RA) is a chronic inflammatory disease and Notch pathway plays a pivotal role in synoviocytes involved in progression of RA. METHODS: Herein, we have designed a self-assembled polymeric micelles based on polycaprolactone-polyethylene glycol (PCL-PEG) and polyethylenimine-polyethylene glycol (PEI-PEG) was prepared and loaded with methotrexate and Notch-1 siRNA for the effective treatment of rheumatoid arthritis. RESULTS: The MTX/siRNA-loaded polymeric micelles (siM-PM) showed appreciable cellular uptake in Raw264...
April 20, 2018: Pharmaceutical Research
https://www.readbyqxmd.com/read/29679157/immediate-release-3d-printed-tablets-produced-via-fused-deposition-modeling-of-a-thermo-sensitive-drug
#13
Wiebke Kempin, Vanessa Domsta, Georg Grathoff, Iris Brecht, Beatrice Semmling, Susan Tillmann, Werner Weitschies, Anne Seidlitz
PURPOSE: Dissolution speeds of tablets printed via Fused Deposition Modeling (FDM) so far are significantly lower compared to powder or granule pressed immediate release tablets. The aim of this work was to print an actual immediate release tablet by choosing suitable polymers and printing designs, also taking into account lower processing temperatures (below 100°C) owing to the used model drug pantoprazole sodium. METHODS: Five different pharmaceutical grade polymers polyvinylpyrrolidone (PVP K12), polyethylene glycol 6000 (PEG 6000), Kollidon® VA64, polyethylene glycol 20,000 (PEG 20,000) and poloxamer 407 were successfully hot-melt-extruded to drug loaded filaments and printed to tablets at the required low temperatures...
April 20, 2018: Pharmaceutical Research
https://www.readbyqxmd.com/read/29678842/biotin-at-high-concentration-interferes-with-the-loci-digoxin-assay-but-the-petinia-phenytoin-assay-is-not-affected
#14
Joe J Rodriguez, Fernando Acosta, Lavern Bourgeois, Amitava Dasgupta
Many automated immunoassays incorporate biotinylated antibodies and streptavidin-coated magnetic beads in the assay design. Biotin at elevated concentrations may interfere with these immunoassays. We evaluated potential interference of biotin on serum digoxin (LOCI assay utilizing biotinylated antibody) and phenytoin (PETINIA assay; no biotinylated antibody) measurements using the Vista 1500 analyzer. Aliquots of drug-free serum pool were supplemented with various biotin concentrations (range: 1 ng/mL to 250 ng/mL) followed by measuring apparent digoxin and phenytoin levels using appropriate immunoassays...
March 2018: Annals of Clinical and Laboratory Science
https://www.readbyqxmd.com/read/29678735/recent-developments-of-nanotherapeutics-for-targeted-and-long-acting-combination-hiv-chemotherapy
#15
REVIEW
Yu Gao, John C Kraft, Danni Yu, Rodney J Y Ho
Combination antiretroviral therapy (cART) given orally has transformed HIV from a terminal illness to a manageable chronic disease. Yet despite the recent development of newer and more potent drugs for cART and suppression of virus in blood to undetectable levels, residual virus remains in tissues. Upon stopping cART, virus rebounds and progresses to AIDS. Current oral cART regimens have several drawbacks including (1) challenges in patient adherence due to pill fatigue or side-effects, (2) the requirement of life-long daily drug intake, and (3) limited penetration and retention in cells within lymph nodes...
April 17, 2018: European Journal of Pharmaceutics and Biopharmaceutics
https://www.readbyqxmd.com/read/29678733/pharmacokinetics-of-lipid-drug-conjugates-loaded-into-liposomes
#16
REVIEW
Rea D Signorell, Paola Luciani, Davide Brambilla, Jean-Christophe Leroux
Drugs that are neither lipophilic nor suitable for encapsulation via remote loading procedures are generally characterized by low entrapment efficiencies and poor retention in liposomes. One approach to circumvent this problem consists in covalently linking a lipid to the drug molecule in order to permit its insertion into the vesicle membrane. The nature of the conjugated lipid and linker, as well as the composition of the liposomal bilayer were found to have a profound impact on the pharmacokinetic properties and biodistribution of the encapsulated drugs as well as on their biological activity...
April 17, 2018: European Journal of Pharmaceutics and Biopharmaceutics
https://www.readbyqxmd.com/read/29678675/towards-tailored-management-of-malignant-brain-tumors-with-nanotheranostics
#17
REVIEW
Juan Aparicio-Blanco, Ana-Isabel Torres-Suárez
Malignant brain tumors still represent an unmet medical need given their rapid progression and often fatal outcome within months of diagnosis. Given their extremely heterogeneous nature, the assumption that a single therapy could be beneficial for all patients is no longer plausible. Hence, early feedback on drug accumulation at the tumor site and on tumor response to treatment would help tailor therapies to each patient's individual needs for personalized medicine. In this context, at the intersection between imaging and therapy, theranostic nanomedicine is a promising new technique for individualized management of malignant brain tumors...
April 17, 2018: Acta Biomaterialia
https://www.readbyqxmd.com/read/29678463/design-synthesis-and-antineoplastic-activity-of-novel-hybrids-of-podophyllotoxin-and-indirubin-against-human-leukaemia-cancer-cells-as-multifunctional-anti-mdr-agents
#18
Jing Wang, Li Long, Yongzheng Chen, Yingshu Xu, Lei Zhang
To overcome cancer drug resistance, in present study, a series of podophyllotoxin-indirubin hybrids were designed, synthesized, and evaluated for anticancer efficacy against two human chronic myeloid leukemia cell cultures. Among them, compound Da-1 was the most potent in resistent K562/VCR cells with an IC50 value of 0.076 ± 0.008 μM. Preliminary mechanism studies showed that Da-1 significantly induced apoptosis and cell cycle arrest at the G2 phase. Decrease in mitochondrial membrane potential, accompanied by activated PARP cleavage, was observed in K562/VCR cells after incubation with Da-1...
April 10, 2018: Bioorganic & Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/29678461/design-synthesis-evaluation-and-molecular-docking-of-ursolic-acid-derivatives-containing-a-nitrogen-heterocycle-as-anti-inflammatory-agents
#19
Zhi-Yu Wei, Ke-Qiang Chi, Ke-Si Wang, Jie Wu, Li-Ping Liu, Hu-Ri Piao
Ursolic acid derivatives containing oxadiazole, triazolone, and piperazine moieties were synthesized in an attempt to develop potent anti-inflammatory agents. Structures of the synthesized compounds were elucidated by 1 H NMR, 13 C NMR, and HRMS. Most of the synthesized compounds showed pronounced anti-inflammatory effects at 100 mg/kg. In particular, compound 11b, which displayed the most potent anti-inflammatory activity of all of the compounds prepared, with 69.76% inhibition after intraperitoneal administration, was more potent than the reference drugs indomethacin and ibuprofen...
April 11, 2018: Bioorganic & Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/29678286/g-protein-coupled-receptors-gpcrs-in-the-treatment-of-diabetes-current-view-and-future-perspectives
#20
REVIEW
Guido Sebastiani, Elena Ceccarelli, Maria Grazia Castagna, Francesco Dotta
G-protein coupled receptors (GPCRs) represent the largest receptor family in the genome and are of great interest for the design of novel drugs in a wide variety of diseases including neurologic disorders, obesity and Type 2 diabetes mellitus. The latter is a chronic disease characterized by insulin resistance and impaired insulin secretion, affecting >400 million patients worldwide. Here we provide an overview on: a) The molecular basis of GPCR signalling and of its involvement in the regulation of insulin secretion and of glucose homeostasis; b) the role of GPCRs in type 2 diabetes pathophysiology and as therapeutic targets of current and future glucose-lowering drugs...
April 2018: Best Practice & Research. Clinical Endocrinology & Metabolism
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