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https://www.readbyqxmd.com/read/28324691/comparison-of-three-different-types-of-cilostazol-loaded-solid-dispersion-physicochemical-characterization-and-pharmacokinetics-in-rats
#1
Omer Mustapha, Kyung Soo Kim, Shumaila Shafique, Dong Shik Kim, Sung Giu Jin, Youn Gee Seo, Yu Seok Youn, Kyung Taek Oh, Chul Soon Yong, Jong Oh Kim, Han-Gon Choi
The aim of this research was to compare three different types of cilostazol-loaded solid dispersion system including solvent-evaporated, solvent-wetted and surface-attached solid dispersion. The effect of polymers and surfactants on the aqueous solubility of cilostazol was investigated, leading to the selection of polyvinylpyrrolidone (PVP) and sodium lauryl sulphate (SLS). Employing a spray-drying technique, numerous surface-attached, solvent-evaporated and solvent-wetted solid dispersions were prepared with various amounts PVP and SLS using water, 90% ethanol and acetone, respectively...
March 9, 2017: Colloids and Surfaces. B, Biointerfaces
https://www.readbyqxmd.com/read/28324268/a-phase-ii-study-of-combined-ridaforolimus-and-dalotuzumab-compared-with-exemestane-in-patients-with-estrogen-receptor-positive-breast-cancer
#2
José Baselga, Serafin M Morales, Ahmad Awada, Joanne L Blum, Antoinette R Tan, Marianne Ewertz, Javier Cortes, Beverly Moy, Kathryn J Ruddy, Tufia Haddad, Eva M Ciruelos, Peter Vuylsteke, Scot Ebbinghaus, Ellie Im, Lamar Eaton, Kumudu Pathiraja, Christine Gause, David Mauro, Mary Beth Jones, Hope S Rugo
PURPOSE: Combining the mTOR inhibitor ridaforolimus and the anti-IGFR antibody dalotuzumab demonstrated antitumor activity, including partial responses, in estrogen receptor (ER)-positive advanced breast cancer, especially in high proliferation tumors (Ki67 > 15%). METHODS: This randomized, multicenter, international, phase II study enrolled postmenopausal women with advanced ER-positive breast cancer previously treated with a nonsteroidal aromatase inhibitor (NCT01234857)...
March 21, 2017: Breast Cancer Research and Treatment
https://www.readbyqxmd.com/read/28324215/surgical-treatment-of-osteoporotic-thoraco-lumbar-compressive-fractures-the-use-of-pedicle-screw-with-augmentation-pmma
#3
Massimo Girardo, P Cinnella, G Gargiulo, P Viglierchio, A Rava, S Aleotti
INTRODUCTION: The osteoporosis prevalence in population is age related. The aim of this single-center observational study was evaluate the middle- to long-term performance of cement (PMMA) augmented fenestrated pedicle screws in elderly patients with thoraco-lumbar compressive fractures by osteoporosis. MATERIALS AND METHODS: From 2011 to 2015 we treated 52 patients (20 males and 32 females) suffering from somatic osteoporotic fractures (T10-L2). The average age was 73...
March 21, 2017: European Spine Journal
https://www.readbyqxmd.com/read/28324032/risk-of-diabetes-treated-in-early-adulthood-following-growth-hormone-treatment-for-short-stature-in-childhood
#4
Amélie Poidvin, Alain Weill, Emmanuel Ecosse, Joel Coste, Jean-Claude Carel
Context.: Growth hormone (GH) is known to be diabetogenic, but the risk of diabetes in individuals treated with GH in childhood has been little evaluated and conflicting results have been obtained. Objective.: To investigate the prevalence of diabetes and gestational diabetes in a population-based cohort of French patients treated with GH for short stature in childhood. Design, Setting and Participants.: Population-based cohort of 5100 children with idiopathic isolated GH deficiency, idiopathic short stature, or short stature in children born short for gestational age who started GH treatment between 1985 and 1996...
January 12, 2017: Journal of Clinical Endocrinology and Metabolism
https://www.readbyqxmd.com/read/28323859/diacerein-inhibits-the-pro-atherogenic-pro-inflammatory-effects-of-il-1-on-human-keratinocytes-endothelial-cells
#5
Girish C Mohan, Huayi Zhang, Lei Bao, Benjamin Many, Lawrence S Chan
We investigated IL-1-induced regulation of genes related to inflammation and atherogenesis in human keratinocytes and endothelial cells, and if 'diacerein', an oral IL-1 inhibiting drug currently approved for use in osteoarthritis, would reverse IL-1's effects on these cells. Primary human keratinocytes and coronary artery endothelial cells were treated with either IL-1α or IL-1β, with and without diacerein. Using PCR-array, we assessed differential gene-expression regulated by IL-1 and diacerein. We identified 34 pro-atherogenic genes in endothelial cells and 68 pro-inflammatory genes in keratinocytes significantly (p<0...
2017: PloS One
https://www.readbyqxmd.com/read/28323508/nefopam-hydrochloride-loaded-microspheres-for-post-operative-pain-management-synthesis-physicochemical-characterization-and-in-vivo-evaluation
#6
Neelam Sharma, Sandeep Arora, Jitender Madan
Once-daily oral dosage of nefopam hydrochloride loaded sustained release microspheres (NPH-MS) was investigated as novel therapeutic strategy for post-operative pain management. Microspheres were synthesized using poly-3-hydroxybutyrate and poly-(ɛ-caprolactone) by double emulsion solvent evaporation technique. NPH-MS were characterized through FTIR, PXRD and SEM. In-vitro drug release study revealed sustained behavior till 24 h. Haemolysis was <5% which signified haemocompatibility of formulation. ED50 in rat tail-flick anti-nociceptive test was found ∼18...
March 21, 2017: Artificial Cells, Nanomedicine, and Biotechnology
https://www.readbyqxmd.com/read/28323493/microparticles-containing-erlotinib-loaded-solid-lipid-nanoparticles-for-treatment-of-non-small-cell-lung-cancer
#7
Zahra Bakhtiary, Jaleh Barar, Ayuob Aghanejad, Amir Ata Saei, Elhameh Nemati, Jafar Ezzati Nazhad Dolatabadi, Yadollah Omidi
Non-small cell lung cancer (NSCLC) patients with sensitizing mutations in the exons 18-21 of the epithelial growth factor receptor (EGFR) geneshowincreased kinase activity of EGFR. Hence, tyrosine kinase inhibitors (TKIs) such as erlotinib (ETB) havecommonly been used as the second line therapeutic option in metastatic NSCLC. While the ETB is available as an oral dosage form, the local delivery of this TKI to the diseased cells of the lung may ameliorate its therapeutic impacts. In the current study, we report on the development of ETB-loaded solid lipid nanoparticle (SLN) based formulation of dry powder inhaler (ETB-SLN DPI)...
March 21, 2017: Drug Development and Industrial Pharmacy
https://www.readbyqxmd.com/read/28323414/design-of-insulin-loaded-nanoparticles-enabled-by-multistep-control-of-nanoprecipitation-and-zinc-chelation
#8
Sunandini Chopra, Nicolas Bertrand, Jong-Min Lim, Amy Wang, Omid C Farokhzad, Rohit Karnik
Nanoparticle (NP) carriers provide new opportunities for controlled delivery of drugs, and have potential to address challenges such as effective oral delivery of insulin. However, due to the difficulty of efficiently loading insulin and other proteins inside polymeric NPs, their use has been mostly restricted to the encapsulation of small molecules. To better understand the processes involved in encapsulation of proteins in NPs, we study how buffer conditions, ionic chelation, and preparation methods influence insulin loading in poly(lactic-co-glycolic acid)-b-poly(ethylene glycol) (PLGA-PEG) NPs...
March 21, 2017: ACS Applied Materials & Interfaces
https://www.readbyqxmd.com/read/28319996/oral-direct-acting-agent-therapy-for-hepatitis-c-virus-infection-a-systematic-review
#9
Oluwaseun Falade-Nwulia, Catalina Suarez-Cuervo, David R Nelson, Michael W Fried, Jodi B Segal, Mark S Sulkowski
Background: Rapid improvements in hepatitis C virus (HCV) therapy have led to the approval of multiple oral direct-acting antiviral (DAA) regimens by the U.S. Food and Drug Administration (FDA) for treatment of chronic HCV infection. Purpose: To summarize published literature on the efficacy and safety of oral DAAs for treatment of persons with chronic HCV infection. Data Sources: MEDLINE and EMBASE from inception through 1 November 2016. Study Selection: 42 English-language studies from controlled and single-group registered clinical trials of adults with HCV infection that evaluated at least 8 weeks of an FDA-approved interferon-free HCV regimen that included at least 2 DAAs...
March 21, 2017: Annals of Internal Medicine
https://www.readbyqxmd.com/read/28319830/anti-proliferative-effect-of-metformin-on-a-feline-injection-site-sarcoma-cell-line-independent-of-mtor-inhibition
#10
J Pierro, C Saba, K McLean, R Williams, E Karpuzoglu, R Prater, K Hoover, R Gogal
Metformin is an oral hypoglycemic drug that has been shown to inhibit cancer cell proliferation via up-regulation of AMPK (AMP-activated protein kinase), and possibly inhibition of mTOR (mammalian target of rapamycin). The purpose of this study was to evaluate the effects of metformin on a feline injection site sarcoma cell line. Cells from a feline injection site sarcoma cell line were treated with metformin at varied concentrations. A dose-dependent decrease in cell viability following metformin treatment was observed, with an IC50 of 8...
March 6, 2017: Research in Veterinary Science
https://www.readbyqxmd.com/read/28319807/targeting-nf-kappa-b-signaling-by-artesunate-restores-sensitivity-of-castrate-resistant-prostate-cancer-cells-to-antiandrogens
#11
Jessica J Nunes, Swaroop K Pandey, Anjali Yadav, Sakshi Goel, Bushra Ateeq
Androgen deprivation therapy (ADT) is the most preferred treatment for men with metastatic prostate cancer (PCa). However, the disease eventually progresses and develops resistance to ADT in majority of the patients, leading to the emergence of metastatic castration-resistant prostate cancer (mCRPC). Here, we assessed artesunate (AS), an artemisinin derivative, for its anticancer properties and ability to alleviate resistance to androgen receptor (AR) antagonists. We have shown AS in combination with bicalutamide (Bic) attenuates the oncogenic properties of the castrate-resistant (PC3, 22RV1) and androgen-responsive (LNCaP) PCa cells...
March 16, 2017: Neoplasia: An International Journal for Oncology Research
https://www.readbyqxmd.com/read/28319002/hba1c-in-relation-to-incident-diabetes-and-diabetes-related-complications-in-non-diabetic-adults-at-baseline
#12
Patricia Anne Metcalf, Cam Kyle, Tim Kenealy, Rod T Jackson
AIMS: We compared the utility of glycated hemoglobin (HbA1c) and oral glucose tolerance (oGTT) in non-diabetic patients for identifying incident diabetes; all-cause mortality; cardiovascular disease (CVD) mortality; CVD, coronary heart disease (CHD), and ischemic stroke events; and diabetes microvascular complications. METHODS: Data from a New Zealand community setting were prospectively linked to hospitalization, mortality, pharmaceutical and laboratory test results data...
February 21, 2017: Journal of Diabetes and its Complications
https://www.readbyqxmd.com/read/28318814/integrated-yoga-and-naturopathy-module-in-management-of-metabolic-syndrome-a-case-report
#13
Swathi Gowda, Sriloy Mohanty, Apar Saoji, Raghuram Nagarathna
A 50-year-old male participant with sedentary lifestyle, diagnosed with Metabolic Syndrome (MetS) [obesity, Type-2 diabetes mellitus, hypertension] and hypothyroidism since 2013, was administered integrated Yoga and Naturopathy (IYN) for 6 weeks as a tailor made individualized protocol at the residential integrative medical facility in Bangalore between October and November 2015. The results showed reduction in weight (97.9 kg to 74.6 kg), Body Mass Index (BMI) (35.1 kg/m(2) to 27.86 kg/m(2)), total cholesterol (192 mg% to 145 mg%), triglycerides (153 mg% to 90 mg%), Low Density Lipoprotein (LDL) (124 mg% to 81 mg%), High Density Lipoprotein (HDL) (40 mg% to 46 mg%), fasting blood glucose (110 mg/dl to 75 mg/dl), postprandial glucose (267 mg/dl to 100 mg/dl), glycated hemoglobin (HbA1c) (7...
March 16, 2017: Journal of Ayurveda and Integrative Medicine
https://www.readbyqxmd.com/read/28318631/the-antihelmenthic-phosphate-niclosamide-impedes-renal-fibrosis-by-inhibiting-homeodomain-interacting-protein-kinase-2-expression
#14
Xiaoyan Chang, Xin Zhen, Jixing Liu, Xiaomei Ren, Zheng Hu, Zhanmei Zhou, Fengxin Zhu, Ke Ding, Jing Nie
Renal fibrosis is the final common pathway of all varieties of progressive chronic kidney disease. However, there are no effective therapies to prevent or slow the progression of renal fibrosis. Niclosamide is a US Food and Drug Administration-approved oral antihelminthic drug used for treating most tapeworm infections. Here, we demonstrated that phosphate niclosamide, the water-soluble form of niclosamide, significantly reduced proteinuria, glomerulosclrotic lesions, and interstitial fibrosis in a murine model of adriamycin nephropathy...
March 16, 2017: Kidney International
https://www.readbyqxmd.com/read/28317813/association-between-pulmonary-tuberculosis-and-type-2-diabetes-in-sudanese-patients
#15
Mona Ahmed, Ibtihal Omer, Sannaa M A Osman, Eltayib H Ahmed-Abakur
INTRODUCTION: Tuberculosis (TB) and diabetes mellitus (DM) are both important health issues, and the association between DM and TB may be the next challenge for global TB control worldwide, type 2 DM (T2DM) responsible for 90% of DM cases. Persons with diabetes have a significantly increased risk of active TB, which is two to three times higher than in persons without diabetes. The aim of this study was to determine the association between pulmonary tuberculosis (PTB) and T2DM among Sudanese patients and also to determine the association between hemoglobin A1c (HbA1c) percentage in diabetic patients and development of PTB and effect of duration of T2DM in developing PTB...
January 2017: International Journal of Mycobacteriology
https://www.readbyqxmd.com/read/28317409/ombitasvir-and-paritaprevir-boosted-with-ritonavir-and-combined-with-dasabuvir-for-chronic-hepatitis-c
#16
Robert Flisiak, Marta Flisiak-Jackiewicz
Hepatitis C is a leading cause of cirrhosis and hepatocellular carcinoma responsible for almost 700,000 deaths worldwide annually. Until 2014, management of HCV infections was based on interferon alfa containing regimens, with efficacy of 40-70% and a high adverse event rate. Interferon-free therapeutic options improved sustained viral response (SVR) rate to >90% and safety profile to placebo-like levels. Areas covered: This article describes all-oral regimen consisting of three direct acting antivirals (DAA) - ombitasvir (OBV), paritaprevir (PTV) and dasabuvir (DSV), which in clinical practice is boosted with ritonavir (r) and sometimes with ribavirin (RBV)...
March 20, 2017: Expert Review of Gastroenterology & Hepatology
https://www.readbyqxmd.com/read/28317200/self-limiting-non-medical-pharmaceutical-opioid-use-among-young-people-in-sydney-australia-an-exploratory-study
#17
George C Dertadian, Thomas C Dixon, Jennifer Iversen, Lisa Maher
INTRODUCTION AND AIMS: Indicators suggest an escalation in opioid use globally, with recent HIV outbreaks linked to non-medical pharmaceutical opioid (NMPO) use. Little is known about how young Australians engage in NMPO use. DESIGN AND METHODS: During 2015, we conducted qualitative interviews with young people (16-29 years) who reported oral NMPO use at least twice in the past 90 days. The study included a sample of injecting (n = 14) and oral (n = 22) users...
March 20, 2017: Drug and Alcohol Review
https://www.readbyqxmd.com/read/28317174/revisiting-the-role-of-gut-wall-in-the-fate-of-orally-administered-drugs-why-now-and-to-what-effect
#18
EDITORIAL
Amin Rostami-Hodjegan, Ikumi Tamai, K Sandy Pang
No abstract text is available yet for this article.
March 2017: Biopharmaceutics & Drug Disposition
https://www.readbyqxmd.com/read/28317117/comparative-pharmacokinetic-evaluation-of-lopinavir-and-lopinavir-loaded-solid-lipid-nanoparticles-in-hepatic-impaired-rat-model
#19
Punna Rao Ravi, Rahul Vats
OBJECTIVE: Drug-induced hepatotoxicity is a major cause of concern in patients receiving HIV/TB co-treatment. Lopinavir (LPV), an anti-HIV drug, shows poor plasma exposure due to hepatic first-pass metabolism. In this study, we investigated the effect of hepatotoxicity on pharmacokinetics of free LPV and LPV-loaded solid lipid nanoparticles (LPV SLNs) in male Wistar rats. METHODS: Hepatic impairment model in rats was developed by injecting CCl4 (i.p., 2 ml/kg). Comparative pharmacokinetic (n = 5) and tissue distribution studies (n = 3) were conducted following oral administration (20 mg/kg) of free LPV and LPV SLNs in normal and hepatic impaired rats...
March 19, 2017: Journal of Pharmacy and Pharmacology
https://www.readbyqxmd.com/read/28315465/early-preclinical-evaluation-of-dihydropyrimidin-thi-ones-as-potential-anticonvulsant-drug-candidates
#20
Mariana Matias, Gonçalo Campos, Samuel Silvestre, Amílcar Falcão, Gilberto Alves
Although significant advances are occurring in epilepsy research, about 30% of epileptic patients are still inadequately controlled by standard drug therapy. For this reason, it continues to be important to develop new chemical entities through which epilepsy could be effectively controlled. In this study, the anticonvulsant activity of forty-two dihydropyrimidin(thi)ones was explored and their efficacy was evaluated in rodents against the maximal electroshock seizure (MES) and subcutaneous pentylenetetrazole tests...
March 14, 2017: European Journal of Pharmaceutical Sciences
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