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Journal of Pharmacy and Pharmacology

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https://www.readbyqxmd.com/read/28631822/mesoporous-silica-based-dosage-forms-improve-bioavailability-of-poorly-soluble-drugs-in-pigs-case-example-fenofibrate
#1
Joseph P O'Shea, Kalpa Nagarsekar, Alena Wieber, Vanessa Witt, Elisabeth Herbert, Caitriona M O'Driscoll, Christoph Saal, Dieter Lubda, Brendan T Griffin, Jennifer B Dressman
OBJECTIVES: Mesoporous silicas (SLC) have demonstrated considerable potential to improve bioavailability of poorly soluble drugs by facilitating rapid dissolution and generating supersaturation. The addition of certain polymers can further enhance the dissolution of these formulations by preventing drug precipitation. This study uses fenofibrate as a model drug to investigate the performance of an SLC-based formulation, delivered with hydroxypropyl methylcellulose acetate succinate (HPMCAS) as a precipitation inhibitor, in pigs...
June 20, 2017: Journal of Pharmacy and Pharmacology
https://www.readbyqxmd.com/read/28631819/protective-effects-of-tannic-acid-on-pressure-overload-induced-cardiac-hypertrophy-and-underlying-mechanisms-in-rats
#2
Li Chu, Pinya Li, Tao Song, Xue Han, Xuan Zhang, Qiongtao Song, Tao Liu, Yuanyuan Zhang, Jianping Zhang
OBJECTIVES: The aim of this study was to examine the cardioprotective effects and latent mechanism of tannic acid (TA) on cardiac hypertrophy. METHODS: Abdominal aortic banding (AAB) was used to induce pressure overload-induced cardiac hypertrophy in male Wistar rats, sham-operated rats served as controls. AAB rats were treated with TA (20 and 40 mg/kg) or captoril. KEY FINDINGS: Abdominal aortic banding rats that received TA showed ameliorated pathological changes in cardiac morphology and coefficients, decreased cardiac hypertrophy and apoptosis, a reduction in over expressions of angiotensin type 1 receptor (AT1 R), angiotensin type 2 receptor (AT2 R), phosphorylation of extracellular signal-regulated kinase 1/2 (ERK1/2) and transforming growth factor-β (TGF-β) mRNA, and modified expression of matrix metal proteinase-9 (MMP-9) mRNA in AAB rat hearts...
June 20, 2017: Journal of Pharmacy and Pharmacology
https://www.readbyqxmd.com/read/28631808/fabrication-of-%C3%AE-cyclodextrin-mediated-single-bimolecular-inclusion-complex-characterization-molecular-docking-in-vitro-release-and-bioavailability-studies-for-gefitinib-and-simvastatin-conjugate
#3
Souvik Basak, Sandip Mondal, Suddhasattya Dey, Plaban Bhattacharya, Achintya Saha, Vinay Deep Punetha, Ali Abbas, Nanda Gopal Sahoo
OBJECTIVES: Introduction of multiple molecules in a single inclusion complex, albeit cheaper, lacks conclusive attempts in earlier drug delivery reports. This manuscript emphasizes simultaneous incorporation of two anticancer drugs, gefitinib (G) and simvastatin (S), in a single molecule of β-cyclodextrin for the first time to achieve effective drug delivery. METHODS: The inclusion complex (GSBCD) was prepared by cosolvent evaporation technique using β-cyclodextrin (BCD) as carrier...
June 20, 2017: Journal of Pharmacy and Pharmacology
https://www.readbyqxmd.com/read/28620994/amphiphilic-naproxen-prodrugs-differential-scanning-calorimetry-study-on-their-interaction-with-phospholipid-bilayers
#4
Maria Chiara Giuffrida, Rosario Pignatello, Francesco Castelli, Maria Grazia Sarpietro
OBJECTIVES: Naproxen, a nonsteroid anti-inflammatory drug studied for Alzheimer's disease, was conjugated with lipoamino acids (LAA) directly or through a diethylamine (EDA) spacer to improve the drug lipophilicity and the interaction with phospholipid bilayers. METHODS: The interaction of naproxen and its prodrugs with biomembrane models consisting of dimyristoylphosphatidylcholine multilamellar vesicles was studied by differential scanning calorimetry. The transfer of prodrugs from a lipophilic carrier to a biomembrane model was also studied...
June 16, 2017: Journal of Pharmacy and Pharmacology
https://www.readbyqxmd.com/read/28620954/propentofylline-phosphodiesterase-and-adenosine-reuptake-inhibitor-modulates-lymphocyte-subsets-and-lymphocyte-activity-after-in-vivo-administration-in-non-immunized-and-srbc-immunized-mice
#5
Marianna Szczypka, Magdalena Lis, Agnieszka Suszko-Pawłowska, Aleksandra Pawlak, Angelika Sysak, Bożena Obmińska-Mrukowicz
OBJECTIVES: The aim of the study was to investigate immunomodulatory effect of in-vivo administered propentofylline on the subsets and activity of murine lymphocytes. METHODS: Propentofylline (3 mg/kg) was administered orally to 8-week-old Balb/c mice, once or six times at 12-h intervals. The lymphocyte subsets, regulatory T cells, IL-5 and TNF levels were determined 12 h and 24 h after a single dose or after the sixth dose of the drug in non-immunized mice. Humoral immune response in sheep red blood cells (SRBC)-immunized mice was determined 4, 7 and 14 days after immunization...
June 16, 2017: Journal of Pharmacy and Pharmacology
https://www.readbyqxmd.com/read/28620922/supraspinal-inhibitory-effects-of-chimeric-peptide-mcrt-on-gastrointestinal-motility-in-mice
#6
Chunbo He, Hailan Li, Jing Zhang, Yanping Kang, Fang Jia, Shouliang Dong, Lanxia Zhou
OBJECTIVES: Chimeric peptide MCRT, based on morphiceptin and PFRTic-NH2 , was a bifunctional ligand of μ- and δ-opioid receptors (MOR-DOR) and produced potent analgesia in tail-withdrawal test. The study focused on the supraspinal effects of morphiceptin, PFRTic-NH2 and MCRT on gastrointestinal motility. Moreover, opioid receptor antagonists, naloxone (non-selective), cyprodime (MOR selective) and naltrindole (DOR selective) were utilized to explore the mechanisms. METHODS: Intracerebroventricular administration was achieved via the implanted cannula...
June 16, 2017: Journal of Pharmacy and Pharmacology
https://www.readbyqxmd.com/read/28620913/efficacy-of-oral-lipid-based-formulations-of-apomorphine-and-its-diester-in-a-parkinson-s-disease-rat-model
#7
Nrupa Borkar, Daniel R Andersson, Mingshi Yang, Anette Müllertz, René Holm, Huiling Mu
OBJECTIVES: Apomorphine is used to symptomatically treat Parkinson's disease (PD). Oral delivery of apomorphine is generally limited by its short plasma half-life and a hepatic first-pass metabolism. This study was aimed at evaluating the behavioural response of apomorphine and its prodrug administered in oral lipid-based formulations. METHODS: The behavioural response of apomorphine and its prodrug administered in oral lipid-based formulations was evaluated using a 6-hydroxydopamine-lesioned rat model simulating PD symptomatology...
June 16, 2017: Journal of Pharmacy and Pharmacology
https://www.readbyqxmd.com/read/28612503/distinctive-in-vitro-signal-transduction-profile-of-nlx-112-a-potent-and-efficacious-serotonin-5-ht1a-receptor-agonist
#8
Adrian Newman-Tancredi, Jean-Claude Martel, Cristina Cosi, Peter Heusler, Fabrice Lestienne, Mark A Varney, Didier Cussac
OBJECTIVES: NLX-112 (befiradol, F13640) is a selective serotonin 5-HT1A receptor agonist. Although it has been tested in vivo, little has been reported on its in vitro signal transduction profile. METHODS: NLX-112 was tested on G-protein activation, inhibition of adenylyl cyclase, ERK1/2 phosphorylation (pERK) and receptor internalization in recombinant cell lines. NLX-112 was also tested on G-protein activation in rat hippocampal membranes. Gα subunit mRNA expression in cell lines and rat brain tissue was quantified by quantitative PCR...
June 14, 2017: Journal of Pharmacy and Pharmacology
https://www.readbyqxmd.com/read/28590566/phenotypic-switching-prevention-and-proliferation-migration-inhibition-of-vascular-smooth-muscle-cells-by-the-ruthenium-nitrosyl-complex-trans-ru-no-cl-cyclam-pf6-2
#9
Mariana G de Oliveira, Fabio G Doro, Elia Tfouni, Marta H Krieger
OBJECTIVES: Vascular smooth muscle cell (VSMC) migration and proliferation at sites of vascular injury are both critical steps in the development of intimal hyperplasia (IH). Local delivery of nitric oxide (NO) largely prevents these events. Among the NO donors, tetraazamacrocyclic nitrosyl complexes, such as trans-[Ru(NO)Cl(cyclam)](PF6 )2 (cyclamNO), gained attention for their features, which include the possibility of being embedded in solid matrices, and ability to participate in a nitrite/NO catalytic conversion cycle...
June 7, 2017: Journal of Pharmacy and Pharmacology
https://www.readbyqxmd.com/read/28590055/enhanced-dissolution-and-bioavailability-of-nateglinide-by-microenvironmental-ph-regulated-ternary-solid-dispersion-in-vitro-and-in-vivo-evaluation
#10
Sarika Wairkar, Ram Gaud, Namdeo Jadhav
OBJECTIVES: Nateglinide, an Antidiabetic drug (BCS II), shows pH-dependent solubility and variable bioavailability. The purpose of study was to increase dissolution and bioavailability of Nateglinide by development of its microenvironmental pH-regulated ternary solid dispersion (MeSD). METHODS: MeSD formulation of Nateglinide, poloxamer-188 and Na2 CO3 was prepared by melt dispersion in 1 : 2 : 0.2 w/w ratio and further characterised for solubility, In-vitro dissolution, microenvironmental pH, crystallinity/amorphism, physicochemical interactions, bioavailability in Wistar rats...
June 7, 2017: Journal of Pharmacy and Pharmacology
https://www.readbyqxmd.com/read/28573734/il-17a-blockade-or-deficiency-does-not-affect-progressive-renal-fibrosis-following-renal-ischaemia-reperfusion-injury-in-mice
#11
Anja Thorenz, Nicole Völker, Jan Hinrich Bräsen, Rongjun Chen, Mi-Sun Jang, Song Rong, Hermann Haller, Torsten Kirsch, Gertrud Vieten, Christian Klemann, Faikah Gueler
OBJECTIVES: IL-17A contributes to acute kidney injury and fibrosis. Therefore, we asked whether IL-17A deficiency or treatment with a IL-17A blocking antibody impacts severe renal ischaemia reperfusion injury (IRI) and the progression to chronic kidney disease (CKD). METHODS: IL-17A-deficient and wild-type (WT) mice underwent transient unilateral renal pedicle clamping for 45 min to induce IRI and subsequent renal fibrosis. Furthermore, a neutralizing anti-IL-17A antibody (mAb) was injected into WT mice before induction of renal IRI intravenously...
June 2, 2017: Journal of Pharmacy and Pharmacology
https://www.readbyqxmd.com/read/28560778/daily-oral-administration-of-low-dose-methotrexate-has-greater-antirheumatic-effects-in-collagen-induced-arthritis-rats
#12
Aoi Koyama, Aki Tanaka, Hideto To
OBJECTIVES: Methotrexate (MTX) is administered once or thrice weekly to patients with rheumatoid arthritis (RA). Even though RA continually progresses, MTX is not administered daily. Therefore, we investigated whether the daily administration of a low dose of MTX inhibits the progression of arthritis in collagen-induced arthritis (CIA) rats. METHODS: Methotrexate was orally administered once weekly, thrice weekly and once daily to CIA rats, and arthritis scores were measured...
May 31, 2017: Journal of Pharmacy and Pharmacology
https://www.readbyqxmd.com/read/28560741/method-development-for-the-determination-of-elements-in-hypericum-perforatum-l-st-john-s-wort-herb-and-preparations-using-inductively-coupled-plasma-optical-emission-spectroscopy-and-microwave-digestion
#13
Jade D Owen, Sara J Evans, Amira Guirguis, Kathryn Kellett, Jacqueline L Stair
OBJECTIVES: A method was developed to analyze St John's wort (Hypericum perforatum L.) herb and preparations using inductively coupled plasma-optical emission spectroscopy (ICP-OES) to determine the quantity of 11 elements (Al, B, Ba, Ca, Cu, Fe, Mg, Mn, Ni, Sr and Zn). METHODS: This study includes the evaluation of digestion acids and calibration methods, as well as instrumental parameters such as choice of nebulizer and emission wavelength. KEY FINDINGS: Two nebulizers (Conikal and SeaSpray) performed similarly for most elements, and two optimum wavelengths were determined for each element...
May 31, 2017: Journal of Pharmacy and Pharmacology
https://www.readbyqxmd.com/read/28555835/antiproliferative-and-antimicrobial-efficacy-of-the-compounds-isolated-from-the-roots-of-oenothera-biennis-l
#14
Shilpi Singh, Vijaya Dubey, Dhananjay Kumar Singh, Kaneez Fatima, Ateeque Ahmad, Suaib Luqman
BACKGROUND: Oenothera biennis L., commonly known as evening primrose, harbours the flavonoids, steroids, tannins, fatty acids and terpenoids responsible for a diverse range of biological activity, such as antitumour, anti-arthritic and anti-inflammatory effects. In addition to the previous reports from aerial parts of this plant, studies related to antiproliferative or antimicrobial activity from the roots are warranted. OBJECTIVE: To investigate antiproliferative and antimicrobial activity of compounds/mixture (1-8) isolated and characterized from the roots of O...
May 29, 2017: Journal of Pharmacy and Pharmacology
https://www.readbyqxmd.com/read/28543298/synthesis-and-preclinical-pharmacokinetic-study-of-dha-10-a-novel-potential-antifungal-pogostone-analogue
#15
Ming Liu, Yanfen Zhou, Jianwei Zhu, Bo Ma, Zheng Fang, Qi Zhang
OBJECTIVES: The emergence of fungal disease calls for the urgency of development of novel drug. In this study, we developed a novel pogostone analogue, DHA-10 and investigated its preclinical pharmacokinetics, tissue distribution, excretion and protein binding rate in rats. METHODS: DHA-10 was synthesized with dehydroacetic acid (DHA) as the starting material and the structure confirmed by NMR and HRMS. The LC-MS/MS was applied to quantitative analysis of DHA-10 concentrations in the biological samples...
May 23, 2017: Journal of Pharmacy and Pharmacology
https://www.readbyqxmd.com/read/28543088/3d-quantitative-structure-activity-relationship-and-docking-studies-of-coumarin-derivatives-as-tissue-kallikrein-7-inhibitors
#16
Xin Zheng, Mengxi He, Xiao Tan, Jun Zheng, Fangyu Wang, Sen Liu
OBJECTIVES: Kallikrein 7 (KLK7) is a secreted serine protease that plays important roles in skin desquamation and tumour progression, which makes it an attracting drug target. To guide the design of KLK7 inhibitors, a series of coumarin-based inhibitors were used to perform 3D-quantitative structure-activity relationship analysis. METHODS: 3D conformations of 37 inhibitors were generated and used to construct CoMFA and CoMSIA models. Then a complex model between the inhibitors and KLK7 was built with molecular docking...
May 23, 2017: Journal of Pharmacy and Pharmacology
https://www.readbyqxmd.com/read/28543032/influence-of-different-wild-garlic-allium-ursinum-extracts-on-the-gastrointestinal-system-spasmolytic-antimicrobial-and-antioxidant-properties
#17
Dragana R Pavlović, Milica Veljković, Nikola M Stojanović, Marija Gočmanac-Ignjatović, Tatjana Mihailov-Krstev, Suzana Branković, Dušan Sokolović, Mirjana Marčetić, Niko Radulović, Mirjana Radenković
OBJECTIVES: As there are no previous studies of the European wild-garlic (Allium ursinum) effects on the gastrointestinal system, despite its traditional applications in gastrointestinal disorders' treatment and regular use in the human diet, we have quantified and compared spasmolytic, antimicrobial and antioxidant activities of its different leaf extracts. METHODS: Wild-garlic extracts were tested for spasmolytic activity on isolated rat ileum, antimicrobial activity on selected Gram-positive and Gram-negative bacteria and fungi by microdilution method and antioxidant capacity by DPPH radical-scavenging assay...
May 23, 2017: Journal of Pharmacy and Pharmacology
https://www.readbyqxmd.com/read/28542928/crosstalk-between-e2f1-and-p53-transcription-factors-in-doxorubicin-induced-dna-damage-evidence-for-preventive-protective-effects-of-silymarin
#18
Seyedeh-Khadijeh Shafiei-Roudbari, Hassan Malekinejad, Hamed Janbaz-Aciabar, Mazdak Razi
OBJECTIVES: To study the effects of silymarin in various forms of applications on the molecular mechanism(s) of doxorubicin-induced testicular toxicity in male rats. METHODS: Following DOX administration with or without SMN in male rats, sperm quality assays were conducted. Moreover, total antioxidant capacity and nitric oxide content of testis were determined. Expression profile of p53 and E2F1 was analysed by PCR technique. Ultimately, the rate of DNA fragmentation in the testes was quantitatively measured...
May 23, 2017: Journal of Pharmacy and Pharmacology
https://www.readbyqxmd.com/read/28542915/effect-of-aqueous-extract-and-anthocyanins-of-calyces-of-hibiscus-sabdariffa-malvaceae-in-rats-with-adenine-induced-chronic-kidney-disease
#19
Badreldin H Ali, Lucie Cahliková, Lubomir Opletal, Turan Karaca, Priyadarsini Manoj, Aishwarya Ramkumar, Yousuf M Al Suleimani, Mohammed Al Za'abi, Abderrahim Nemmar, Lucie Chocholousova-Havlikova, Miroslav Locarek, Tomas Siatka, Gerald Blunden
OBJECTIVES: The aim of this work was to assess the possible beneficial effects of aqueous extracts of Hibiscus sabdariffa L. calyces and anthocyanins isolated therefrom in an adenine-induced chronic kidney disease (CKD) model. METHODS: Rats were orally given, for 28 consecutive days, either adenine alone or together with either aqueous extract of H. sabdariffa calyces (5 and 10%) or anthocyanins (50, 100 and 200 mg/kg of anthocyanin concentrate). For comparative purposes, two groups of rats were given lisinopril (10 mg/kg)...
May 23, 2017: Journal of Pharmacy and Pharmacology
https://www.readbyqxmd.com/read/28542812/modulating-nasal-mucosal-permeation-using-metabolic-saturation-and-enzyme-inhibition-techniques
#20
Varsha Dhamankar, Maureen D Donovan
OBJECTIVE: Presystemic elimination resulting from local enzymatic degradation can play a key role in limiting the bioavailability of intranasally administered drugs. The aim of this study was to evaluate the transfer of a metabolically susceptible drug across the nasal mucosa to illustrate the relative contributions of drug diffusivity and metabolic susceptibility on overall nasal mucosal permeation and to understand the effects of changes in enzymatic activity on the transfer across nasal epithelial and submucosal tissues...
May 23, 2017: Journal of Pharmacy and Pharmacology
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