5,399,503 results match your criteria Drug and Therapeutics Bulletin[Journal]

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Take-home naloxone is a global issue, in practice and in research: A response to Heavey et al.

Int J Drug Policy 2018 Dec 12;63:111-112. Epub 2018 Dec 12.

MRC Biostatistics Unit, Cambridge, UK.

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December 2018
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Possible involvement of Fas/FasL-dependent apoptotic pathway in α-bisabolol induced cardiotoxicity in zebrafish embryos.

Chemosphere 2018 Dec 8;219:557-566. Epub 2018 Dec 8.

Biology Institute, Qilu University of Technology (Shandong Academy of Sciences), 28789 East Jingshi Road, Jinan, 250103, Shandong Province, PR China; Key Laboratory for Drug Screening Technology of Shandong Academy of Sciences, 28789 East Jingshi Road, Jinan, 250103, Shandong Province, PR China. Electronic address:

α-Bisabolol, an unsaturated monocyclic sesquiterpene alcohol, is a common ingredient in many pharmaceuticals and personal care products (PPCPs). Despite being widely used, little is known about its toxic effects on organisms and aquatic environment. In this study, we investigated the developmental toxicity of α-Bisabolol, especially its effects on the cardiac development using zebrafish embryos as a model. Read More

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December 2018

Functionalized rifampicin-loaded nanostructured lipid carriers enhance macrophages uptake and antimycobacterial activity.

Colloids Surf B Biointerfaces 2018 Dec 4;175:306-313. Epub 2018 Dec 4.

Laboratório de Fitotecnologia, Escola de Farmácia, Universidade Federal de Ouro Preto, Ouro Preto, Brazil. Electronic address:

Tuberculosis is an infectious bacterial disease that causes millions of deaths worldwide. Current treatment recommended by WHO is effective, however it is an extensive and arduous process associated to severe adverse effects, which induces a low patient compliance and the emerging of multidrug resistant tuberculosis. Thus, as a main goal of this study, rifampicin nanoparticles were surface functionalized with a tuftsin-modifed peptide to selectively recognize receptors located on infected alveolar macrophages, enhancing nanoparticles uptake by these cells and improving antimycobacterial activity. Read More

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December 2018

Preparation of pH-responsive avermectin/feather keratin-hyaluronic acid with anti-UV and sustained-release properties.

Colloids Surf B Biointerfaces 2018 Dec 6;175:291-299. Epub 2018 Dec 6.

School of Chemistry and Chemical Engineering, Zhongkai University of Agriculture and Engineering, Guangzhou, PR China. Electronic address:

In an effort to improve the utilization of pesticides, an environmentally friendly carrier material was prepared to encapsulate pesticides and to prevent pesticides from decomposing under natural conditions with sustained-release effect. The carrier of feather keratin-hyaluronic acid (FK-HA) was prepared by Maillard reaction. Using avermectin (AVM) as a model drug, AVM/FK-HA was obtained by heating. Read More

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December 2018

Checkpoint-modulating immunotherapies in tumor treatment: Targets, drugs, and mechanisms.

Int Immunopharmacol 2018 Dec 12;67:160-175. Epub 2018 Dec 12.

Wuya College of Innovation, Key Laboratory of Structure-Based Drug Design & Discovery, Ministry of Education, Shenyang Pharmaceutical University, Shenyang 110016, China; Hubei Key Laboratory of Natural Medicinal Chemistry and Resource Evaluation, School of Pharmacy, Tongji Medical College, Huazhong University of Science and Technology, Wuhan 430030, China. Electronic address:

Tumor immunotherapy, as a new treatment of cancer, has been developing on the basis of tumor immunology. Tumor immunotherapy stimulates and enhances the function of immune system in human bodies, in order to control and kill tumor cells. It is often used as an adjuvant therapy combined with surgery, chemotherapy, radiotherapy and other conventional methods. Read More

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December 2018

An update on Drug Repurposing: Re-written saga of the drug's fate.

Biomed Pharmacother 2018 Dec 12;110:700-716. Epub 2018 Dec 12.

Pharamacological Modelling and Simulation Centre, M.S.Ramaiah University of Applied Sciences, Bangalore, Karnataka, India; Department of Pharmacy Practice, Faculty of Pharmacy, M.S.Ramaiah University of Applied Sciences, Bangalore, Karnataka, India.

Drug repurposing is an unconventional drug discovery approach to explore new therapeutic benefits of existing, shelved and the drugs in clinical trials. This approach is currently emerging to overcome the bottleneck constraints faced during traditional drug discovery in grounds of financial support, timeline and resources. In this direction, several efforts were made for the construction of stratagems based on bioinformatics and computational tools to intensify the repurposing process off-late. Read More

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December 2018

The role of histone deacetylase inhibitors in metastatic breast cancer.

Breast 2018 Dec 6;43:130-134. Epub 2018 Dec 6.

IEO, European Institute of Oncology IRCCS, Milan, Italy; Department of Oncology and Hematology, University of Milano, Milan, Italy. Electronic address:

Histone deacetylase inhibitors (HDACi) are a relatively new class of drug that plays an important role in the epigenetic and non-epigenetic regulation in cancer, inducing death, apoptosis and cell cycle arrest in cancer cells. Although HDACi are approved only for hematologic malignancies, there are several trials in the breast cancer setting with promising results. In this review, we summarize the latest studies with HDACi in breast cancer from the emerging data in the translational research until its possible applicability in the clinical practice. Read More

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December 2018

Molecular simulation of the structure of folate and antifolates at physiological conditions.

J Mol Graph Model 2018 Dec 4;87:172-184. Epub 2018 Dec 4.

Laboratory of Quantum and Computational Chemistry, Faculty of Chemistry and Pharmacy, University of Sofia, 1 James Bourchier Blvd, 1164, Sofia, Bulgaria. Electronic address:

The study is focused on description of folate and several antifolates at physiological conditions. Knowledge of the molecular structure and dynamics is important for understanding their biological activity and therapeutic application. They are modelled in saline by atomistic molecular dynamics simulations and characterized in detail. Read More

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December 2018

Predictive factors associated with driving under the influence among Brazilian drug-using drivers.

Accid Anal Prev 2018 Dec 12;123:256-262. Epub 2018 Dec 12.

Center for Drug and Alcohol Research, Hospital de Clínicas de Porto Alegre, Rua Professor Álvaro Alvim, 400, 90420-020, Porto Alegre, RS, Brazil.

The incidence of driving under the influence of psychoactive substances (DUI) and its recidivism can be curtailed by the proper identification of specific and predictive characteristics among drug users. In this sense, interpersonal violence (IV), psychiatric comorbidity and impulsivity seem to play an important role in DUI engagement according to previous studies. There are, however, limited data originated from low and middle income countries. Read More

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December 2018

Medical populism.

Soc Sci Med 2018 Dec 7;221:1-8. Epub 2018 Dec 7.

University of Canberra, Australia. Electronic address:

Medical emergencies are staple features of today's 24/7 culture of breaking news. As politics becomes increasingly stylised, audiences fragmented, and established knowledge claims contested, health crises have become even more vulnerable to politicisation. We offer the vocabulary of medical populism to make sense of this phenomenon. Read More

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December 2018

Study on anti-hyperuricemia effects and active ingredients of traditional Tibetan medicine TongFengTangSan (TFTS) by ultra-high-performance liquid chromatography coupled with quadrupole time-of-flight mass spectrometry.

J Pharm Biomed Anal 2018 Nov 17;165:213-223. Epub 2018 Nov 17.

Jiangxi University of Traditional Chinese Medicine, No. 1688 Meiling Road, Nanchang, 330004, PR China. Electronic address:

TongFengTangSan (TFTS), a traditional Tibetan medicine comprising of Tinospora sinensis (TS), Terminalia chebula Retz (TC) and Trogopterori faeces (TF), is used to treat joint diseases like gout, gout arthritis, swelling, pain etc. Despite the significant therapeutic effects of TFTS, its pharmacological components have not been analyzed so far. Therefore, the chemical composition of the effective part of TFTS was analyzed by ultra-high-performance liquid chromatography coupled with quadrupole time-of-flight mass spectrometry (UHPLC-Q-TOF-MS/MS). Read More

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November 2018

A convenient strategy to overcome interference in LC-MS/MS analysis: Application in a microdose absolute bioavailability study.

J Pharm Biomed Anal 2018 Dec 10;165:198-206. Epub 2018 Dec 10.

Bioanalytical Sciences, Bristol-Myers Squibb, Princeton, NJ, 08543, USA.

Stable isotope labeled (SIL) compounds have been commonly used as internal standards (IS) to ensure the accuracy and quality of liquid chromatography-mass spectrometry (LC-MS) bioanalytical assays. Recently, the application of SIL drugs and LC-MS assays to microdose absolute bioavailability (BA) studies has gained increasing attention. This approach can provide significant cost and time saving, and higher data quality compared to the accelerator mass spectrometry (AMS)-based method, since it avoids the use of radioactive drug, high-cost AMS instrumentation and complex measurement processes. Read More

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December 2018
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Recent advances in bio-affinity chromatography for screening bioactive compounds from natural products.

J Pharm Biomed Anal 2018 Dec 7;165:182-197. Epub 2018 Dec 7.

Institute of Pharmaceutical Analysis, College of Pharmacy, Jinan University, Guangzhou, 510632, China; Guangdong Province Key Laboratory of Pharmacodynamic Constituents of TCM and New Drugs Research, College of Pharmacy, Jinan University, Guangzhou, 510632, China. Electronic address:

Natural products are one of the most important sources of leading compounds in drug discovery. Until now, rapid screening and identification of biologically active components from natural products remain a technical challenge. Bio-affinity chromatography (BAC) based approaches hold great promise in screening potential bioactive ligands from complex samples. Read More

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December 2018

Binding of norharmane with RNA reveals two thermodynamically different binding modes with opposing heat capacity changes.

J Colloid Interface Sci 2018 Dec 4;538:587-596. Epub 2018 Dec 4.

Department of Chemistry, Indian Institute of Science Education and Research Bhopal, Bhopal Bypass Road, Bhauri, Bhopal 426066, Madhya Pradesh, India. Electronic address:

The binding interaction of a prospective anti-cancer photosensitizer, norharmane (NHM, 9H-pyrido[3,4-b]indole) with double stranded RNA reveals a primarily intercalative mode of binding. Steady-state and time-resolved fluorescence spectroscopic results demonstrate the occurrence of drug-RNA binding interaction as manifested through environment-sensitive prototropic equilibrium of NHM. However, the key finding of the present study lies in unraveling the complexities in the NHM-RNA binding thermodynamics. Read More

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December 2018

Key role of cyromazine in the distribution of antibiotic resistance genes and bacterial community variation in aerobic composting.

Bioresour Technol 2018 Dec 3;274:418-424. Epub 2018 Dec 3.

College of Natural Resources and Environment, Northwest A&F University, Yangling, Shaanxi 712100, China.

The risks that have not been noted so far have come from the use of non-antibiotics. In this study, non-antibiotic drug (cyromazine) was used in composting to investigate its possible effects on the distribution of ARGs and changes of bacterial community. Results showed that cyromazine increased the abundances of highly-risky ARGs (bla and bla), and heavy metal resistance genes (MRGs). Read More

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December 2018
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Telephone-delivered cognitive behavioral therapy for veterans with chronic pain following traumatic brain injury: Rationale and study protocol for a randomized controlled trial study.

Contemp Clin Trials 2018 Dec 12. Epub 2018 Dec 12.

Department of Rehabilitation Medicine, Box 356490, University of Washington, Seattle, Washington 98195-6490, USA; VA Puget Sound Healthcare System, 1660 S. Columbian Way, RCS-117, Seattle, WA 98108, USA. Electronic address:

Background And Objectives: Chronic pain is a highly prevalent and potentially disabling condition in Veterans who have had a traumatic brain injury (TBI) and access to non-pharmacological pain treatments such as cognitive behavioral therapy is limited and variable. The purpose of this randomized controlled trial (RCT) is to evaluate the efficacy of a telephone-delivered cognitive behavioral therapy (T-CBT) for pain in Veterans with a history of TBI.

Methods: Veterans with a history of TBI and chronic pain of at least six months duration (N = 160) will be randomized to either T-CBT or a telephone-delivered pain psychoeducational active control condition (T-Ed). Read More

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December 2018

Improved anti-colorectal carcinomatosis effect of tannic acid co-loaded with oxaliplatin in nanoparticles encapsulated in thermosensitive hydrogel.

Eur J Pharm Sci 2018 Dec 12. Epub 2018 Dec 12.

State Key Laboratory of Biotherapy and Cancer Center and Department of Neurosurgery, West China Hospital, Sichuan University and Collaborative Innovation Center for Biotherapy, Chengdu 610041, PR China. Electronic address:

Tannic acid, a hydrolysable tannin, exists commonly in food plants. Tannic acid has already been shown various anticancer mechanisms such as inhibiting the proliferation, inducing a higher apoptotic rate and slowing down the metastasis of different cancers. Moreover, tannic acid was reported to reduce the side effects caused by chemotherapeutics on patients. Read More

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December 2018

Synthesis and characterization of nanostructured lipid-poloxamer organogels for enhanced skin local anesthesia.

Eur J Pharm Sci 2018 Dec 12. Epub 2018 Dec 12.

Human and Natural Sciences Center, Federal University of ABC, Santo André, SP, Brazil. Electronic address:

The aim of this study was to synthesize a novel drug delivery system using organogels (ORGs) and characterize its physicochemical properties, in vitro and ex vivo permeation abilities, cytotoxicity and in vivo local anesthetic effects. The ORG formulations contained a mixture of oleic acid-lanolin (OA-LAN), poloxamer (PL407), and the commonly used local anesthetic lidocaine (LDC). The main focus was to evaluate the impact of LAN and PL407 concentrations on the ORG structural features and their biopharmaceutical performance. Read More

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December 2018
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Molecular structure and impact of amorphization strategies on intrinsic dissolution of spray dried indomethacin.

Eur J Pharm Sci 2018 Dec 12. Epub 2018 Dec 12.

Department of Pharmacy, University of Copenhagen, Universitetsparken 2, DK-2100 Copenhagen, Denmark. Electronic address:

Amorphous systems prepared with different strategies, such as solid dispersion with colloidal particles or soluble polymers and inclusion complex, have been used for improving solubility and dissolution of poorly water soluble drugs. The purpose of this study was to obtain a deeper understanding of the impact of three different amorphous systems prepared by spray drying with silica, polyvinylpyrrolidone (PVP) or 2-hydroxypropyl-β-cyclodextrin (HPβCD) using indomethacin (IND) as a model drug. IND was spray dried with silica, PVP or HPβCD at different mass ratios, and the obtained powders were characterized with respect to colloidal silica particle redispersion, morphology, thermal properties, solid state properties and physical stability. Read More

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December 2018

Enhancement of the apparent solubility and bioavailability of Tadalafil nanoparticles via antisolvent precipitation.

Eur J Pharm Sci 2018 Dec 12. Epub 2018 Dec 12.

School of Pharmaceutical Sciences, Guangzhou University of Chinese Medicine, Guangzhou 510006, PR China. Electronic address:

The ability to increase the bioavailability and dissolution of poorly soluble hydrophobic drugs has been a major challenge for pharmaceutical development. This study shows that the dissolution rate, apparent solubility and oral bioavailability of tadalafil (Td) can be improved by nano-sized amorphous particles prepared by using antisolvent precipitation. Acetone and an acetone-water solution (v:v, 9:1) were selected as solvents, with deionized water as the antisolvent. Read More

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December 2018
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Chitosan-hydroxypropyl methylcellulose tioconazole films: A promising alternative dosage form for the treatment of vaginal candidiasis.

Int J Pharm 2018 Dec 12. Epub 2018 Dec 12.

Instituto de Química Rosario (IQUIR, CONICET-UNR), Suipacha 531, Rosario S2002LRK, Argentina; Área Técnica Farmacéutica, Facultad de Ciencias Bioquímicas y Farmacéuticas, Universidad Nacional de Rosario, Suipacha 531, Rosario S2002LRK, Argentina. Electronic address:

Vaginal candidiasis is considered a frequent opportunistic mucosal infection and the second most common cause of vaginitis after bacterial vaginosis. In this work, different vaginal films based on chitosan, hydroxypropyl methylcellulose and blends of these polymers containing tioconazole, were developed and thoroughly characterized to improve the conventional therapeutics of vaginal candidiasis. Mechanical properties, swelling, adhesiveness, morphology, antifungal activity, hemocompatibility and cytotoxicity were evaluated. Read More

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December 2018

Revival of a Potent Therapeutic Maytansinoid Agent using a Strategy that Combines Covalent Drug Conjugation with Sequential Nanoparticle Assembly.

Int J Pharm 2018 Dec 12. Epub 2018 Dec 12.

The First Affiliated Hospital, Collaborative Innovation Center for Diagnosis and Treatment of Infectious Diseases, Key Laboratory of Combined Multi-Organ Transplantation, Ministry of Public Health, School of Medicine, Zhejiang University, Hangzhou, 310003, PR China. Electronic address:

Maytansine and its related analogues are a class of highly potent anti-proliferation agents that have failed to be exploited as clinical drugs for human therapy due to unacceptable systemic toxicity. Here, we delineate a novel strategy that combines rational drug conjugation with subsequent nanoparticle assembly to systemically deliver this highly potent and toxic drug. To demonstrate this concept, we covalently coupled the thiolated maytansine derivative, the DM1 agent, to amphiphilic block co-polymers, polyethylene glycol (PEG)-block-polylactide (PLA), in varying molecular weights to generate two prodrug constructs (i. Read More

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December 2018

Automated small-scale in vitro transfer model as screening tool for the prediction of in vivo-dissolution and precipitation of poorly solubles.

Int J Pharm 2018 Dec 12. Epub 2018 Dec 12.

Institute of Pharmacy, Department of Biopharmaceutics and Pharmaceutical Technology, University of Greifswald, Felix-Hausdorff-Strasse 3, 17489 Greifswald, Germany. Electronic address:

Precipitation testing, especially for weakly basic APIs, represents a key parameter in drug substance characterization during early development stages, where the amount of API available is limited. Therefore, it was the aim of this study to develop an automated small-scale in vitro transfer model to characterize the supersaturation and precipitation behavior of two poorly water-soluble drugs. Following automation and scale-down of the standard transfer model, the developed small-scale model was used to assess the impact of gastrointestinal variability, i. Read More

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December 2018

Gelatinized core liposomes: A new Trojan horse for the development of a novel timolol maleate glaucoma medication.

Int J Pharm 2018 Dec 12. Epub 2018 Dec 12.

Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy , Ain Shams University, African Union Street Authority Street, Abbassia, 11566 Cairo, Egypt.

Glaucoma treatment with ocular medications requires overcoming the corneal barrier to drug penetration. Liposomes have a great corneal penetration ability and affinity while suffering from poor stability and low entrapment of hydrophilic drugs accompanied by rapid drug release. This work aims to develop a new, effective and stable glaucoma medication with sustained drug release properties; Timolol maleate gelatinized core liposomes. Read More

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December 2018

A comprehensive analysis and optimization of continuous twin-screw granulation processes via sequential experimentation strategy.

Int J Pharm 2018 Dec 12. Epub 2018 Dec 12.

Department of Pharmaceutics, Rutgers University, Piscataway, NJ 08854, USA; Department of Chemical and Biochemical Engineering, Rutgers University, Piscataway, NJ 08854, USA. Electronic address:

Nowadays twin-screw granulation has been emerging as an attractive continuous wet granulation technique. This study was geared towards better process design and understanding with emphasis on bridging the knowledge gap between input and output variables by employing sequential experimentation strategy. A low-dose formulation for granulation experiments contained anhydrous caffeine as the model drug. Read More

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December 2018

P-glycoprotein (MDR1/ABCB1) and Breast Cancer Resistance Protein (BCRP/ABCG2) limit brain accumulation of the FLT3 inhibitor quizartinib in mice.

Int J Pharm 2018 Dec 12. Epub 2018 Dec 12.

The Netherlands Cancer Institute, Division of Pharmacology, Plesmanlaan 121, 1066 CX Amsterdam, The Netherlands. Electronic address:

Quizartinib, a second-generation FLT3 inhibitor, is in clinical development for the treatment of acute myeloid leukemia. We studied its pharmacokinetic interactions with the multidrug efflux transporters ABCB1 and ABCG2 and the multidrug metabolizing enzyme CYP3A, using in vitro transport assays and knockout and transgenic mouse models. Quizartinib was transported by human ABCB1 in vitro, and by mouse (m)Abcb1 and mAbcg2 in vivo. Read More

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December 2018

Effects of cellular differentiation in human primary bronchial epithelial cells: Metabolism of 4-(methylnitrosamine)-1-(3-pyridyl)-1-butanone.

Toxicol In Vitro 2018 Dec 12. Epub 2018 Dec 12.

Division of Genetic and Molecular Toxicology, Division of Biochemical Toxicology, National Center for Toxicological Research, U.S Food and Drug Administration, Jefferson, AR 72079, United States. Electronic address:

Many of the toxicants in tobacco smoke undergo biotransformation in the lungs of smokers, both to reactive and to detoxified derivatives. Human air-liquid-interface (ALI) airway tissue models have emerged as an advanced in vitro model for evaluating the toxicity of inhaled substances; however, the metabolic potential of these cultures has not been evaluated extensively. In this study, we compared the metabolic activities of an ALI tissue model to the undifferentiated normal human primary bronchial epithelial (NHBE) cells from which it was derived. Read More

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December 2018
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Paris saponin VII reverses chemoresistance in breast MCF-7/ADR cells.

J Ethnopharmacol 2018 Dec 12. Epub 2018 Dec 12.

Laboratory of Oncological Pharmacology, Department of Pharmacology, School of Pharmacy, Southwest Medical University, Luzhou, 646000, Sichuan, PR China; Key Laboratory of Gastrointestinal Pharmacology of Chinese Materia Medica of the State Administration of Traditional Chinese Medicine, Department of Pharmacology, School of Pharmacy, The Fourth Military Medical University, Xi'an 710032, Shaanxi, PR China. Electronic address:

Ethnopharmacological Relevance: The development of a multidrug-resistant (MDR) phenotype is a main obstacle to the successful treatment of breast cancer. Saponins of several herbs are considered as promising candidates for drug resistance treatment. We extracted Paris saponin VII (PS VII) from Trillium tschonoskii Maxim. Read More

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December 2018
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Emex spinosa (L.) Campd. ethyl acetate fractions effects on inflammatory mediators and oxidative stressmarkers in carrageenan induced paw oedema in mice.

J Ethnopharmacol 2018 Dec 12. Epub 2018 Dec 12.

Biopesticides Laboratory (LPIP), Center of Biotechnology of Sfax, University of Sfax, P.O. Box. 1177, 3018 Sfax, TUNISIA. Electronic address:

Ethnopharmacological Relevance: Emex spinosa (L.) Campd. (E. Read More

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December 2018

Idebenone and T2D: A new insulin-sensitizing drug for personalized therapy.

Pharmacol Res 2018 Dec 12. Epub 2018 Dec 12.

International Center for T1D, Pediatric Clinical Research Center Romeo ed Enrica Invernizzi, "L. Sacco" Department of Biomedical and Clinical Sciences, University of Milan, Milan, Italy; Transplantation Research Center, Nephrology Division, Brigham and Women's Hospital, Boston, MA, United States; Endocrinology Division, ASST Fatebenefratelli-Sacco, Milan, Italy. Electronic address:

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December 2018

Sustained release of recombinant thrombomodulin from cross-linked gelatin/hyaluronic acid hydrogels potentiate wound healing in diabetic mice.

Eur J Pharm Biopharm 2018 Dec 12. Epub 2018 Dec 12.

nstitute of Clinical Pharmacy and Pharmaceutical Sciences, Southern Taiwan University of Science and Technology, Tainan, Taiwan. Electronic address:

Thrombomodulin (TM) is a type-I transmembrane glycoprotein expressed on the surfaces of endothelial cells and epidermal keratinocytes. It is known to regulate blood coagulation, inflammation, and cell-cell adhesion. A recombinant TM, which contains an epidermal growth factor - like domain and serine/threonine-riches domain, has been demonstrated to stimulate cell proliferation and migration of keratinocytes and wound healing. Read More

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December 2018

Biogenic nanomaterials: Synthesis, characterization, growth mechanism, and biomedical applications.

J Microbiol Methods 2018 Dec 12. Epub 2018 Dec 12.

School of Pharmacy, Sungkyunkwan University, 2066 Seoburo, Jangan-gu, Suwon, Gyeonggido 16419, Republic of Korea. Electronic address:

The biosynthesis of nanomaterials is a huge and intensifying field of research due to their application in various areas, in particular the biomedical and pharmaceutical fields. In this review, we focused on the biosynthesis of both metallic and semiconductor nanomaterials and their application in biomedicine and pharmaceutics. In order to meet an exponentially increasing need for nanostructured materials, the biological route for the synthesis of nanomaterials will have to be explored, offering advantages over chemical and physical methods as a simpler, more cost effective, and environmentally friendly method, and for which there is no need to use high pressure and temperatures or toxic chemicals. Read More

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December 2018

Protocol for evaluation of topical ophthalmic drug products in different compartments of fresh eye tissues in a rabbit model.

J Pharmacol Toxicol Methods 2018 Dec 12. Epub 2018 Dec 12.

Office of Translational Science, Office of Clinical Pharmacology, Division of Applied Regulatory Science, U.S. Food and Drug Administration, Center for Drug Evaluation and Research, White Oak Federal Research Center, 10903 New Hampshire Ave, Silver Spring, MD 20993, USA. Electronic address:

Topical ophthalmic drugs are the most commonly used dosage form to treat diseases of the anterior segment of the eye. Although this dosage form has the advantages of ease of application, small volume dose, and rapid action and is largely devoid of systemic adverse effects, the bioavailability is low due to pre-corneal anatomical barriers and the nature of the drug formulation itself. Some complex generic formulations (suspensions, ointments, gels) for topical ophthalmic products face impediments to rapid regulatory approval because of the complex nature of the formulations and difficulties in determining bioequivalence with the innovator product. Read More

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December 2018

Development of Nanoparticles for Drug Delivery to Brain Tumor: The Effect of Surface Materials on Penetration into Brain Tissue.

J Pharm Sci 2018 Dec 12. Epub 2018 Dec 12.

Department of Chemical and Biomolecular Engineering, National University of Singapore, 4 Engineering Drive 4, Singapore, 117585, Singapore. Electronic address:

Surface modified PLGA nanoparticles were fabricated via nanoprecipitation for obtaining therapeutic concentration of paclitaxel (PTX) in brain tumor. The cellular uptake and cytotoxicity of NPs were evaluated on C6 glioma cells in vitro and BALB/c mice were used to study the brain penetration and bio-distribution upon intravenous administration. Results showed that by finely tuning nanoprecipitation parameters, PLGA nanoparticles coated with surfactants with a size around 150nm could provide a sustained release of PTX for >2 weeks. Read More

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December 2018

Non-covalent hitchhiking on endogenous carriers as a protraction mechanism for antiviral macromolecular prodrugs.

J Control Release 2018 Dec 12. Epub 2018 Dec 12.

Department of Chemistry, Aarhus University, 8000 Aarhus C, Denmark. Electronic address:

Albumin is a highly successful tool of drug delivery providing drastically extended body and blood residence time for the associated cargo, but it only traffics single drug copies at a time. In turn, macromolecular prodrugs (MP) are advantaged in carrying a high drug payload but offering only a modest extension of residence time to the conjugated drugs. In this work, we engineer MP to contain terminal groups that bind to albumin via non-covalent association and reveal that this facile measure affords a significant protraction for the associated polymers. Read More

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December 2018

Molecular mechanism involved in cyclophosphamide-induced cardiotoxicity: Old drug with a new vision.

Life Sci 2018 Dec 12. Epub 2018 Dec 12.

Department of Pharmacology, School of Pharmaceutical Education and Research, Jamia Hamdard, New Delhi 110062, India. Electronic address:

Cyclophosphamide (CP) is an important anticancer drug which belongs to the class of alkylating agent. Cyclophosphamide is mostly used in bone marrow transplantation, rheumatoid arthritis, lupus erythematosus, multiple sclerosis, neuroblastoma and other types of cancer. Dose-related cardiotoxicity is a limiting factor for its use. Read More

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December 2018

Women's perspectives about cannabis use during pregnancy and the postpartum period: An integrative review.

Prev Med 2018 Dec 12. Epub 2018 Dec 12.

University of British Columbia, Vancouver, BC, Canada.

Cannabis is the most commonly used illicit drug among general and pregnant populations. Despite recommendations to abstain from cannabis use, its use is increasing during the perinatal period. In this integrative review, we aim to understand women's perspectives about the health aspects of perinatal cannabis use. Read More

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December 2018
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Levetiracetam combined with ACEA, highly selective cannabinoid CB1 receptor agonist changes neurogenesis in mouse brain.

Neurosci Lett 2018 Dec 12. Epub 2018 Dec 12.

Isobolographic Analysis Laboratory, Institute of Rural Health, Jaczewskiego 2, 20-950 Lublin, Poland.

The aim of the study was to evaluate the impact of second generation antiepileptic drug levetiracetam (LEV) with arachidonyl-2'-chloroethylamide (ACEA) on proliferating neural precursor cells in mouse brain. Additionally, we established the relationship between treatment with ACEA in combination with LEV and hippocampal neurogenesis in mouse brain. All experiments were performed on male CB57/BL mice injected i. Read More

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December 2018

Efficacy and Safety of Non-Invasive Intravesical Instillation of Onabotulinum Toxin-A for Overactive Bladder and Interstitial Cystitis/Bladder Pain Syndrome: Systematic Review and Meta-analysis.

Urology 2018 Dec 12. Epub 2018 Dec 12.

Department of Urology, Soonchunhyang University Seoul Hospital, Soonchunhyang University Medical College, Seoul, South Korea. Electronic address:

Objective: To investigate the efficacy and safety of non-invasive intravesical instillation of OBTX-A through systematic review and meta-analysis. Recently, several studies of non-invasive intravesical instillation of Onabotulinum Toxin-A (OBTX-A) have been published. However, its efficacy is not well validated yet compared to well-known efficacy of minimally invasive intravesical injection of OBTX-A. Read More

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December 2018
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Preparation and drug release property of tanshinone IIA loaded chitosan-montmorillonite microspheres.

Int J Biol Macromol 2018 Dec 12. Epub 2018 Dec 12.

College of Chemical Engineering, Zhejiang University of Technology, Hangzhou 310014, China. Electronic address:

In this study, a biocompatible chitosan/montmorillonite (CS/MMT) composite microsphere was developed as a carrier for loading and sustained-release of the hydrophobic drug of tanshinone IIA. Though the compatibility between hydrophobic drugs and hydrophilic matrix was fairly poor, tanshinone IIA was successfully loaded on the microsphere by the solvent exchange process during chitosan matrix dehydration. The microstructure of the resulting microspheres was characterized with several techniques, such as X-ray diffraction (XRD), thermo-gravimetric analysis (TGA), Fourier transform infrared spectroscopy (FT-IR), and scanning electron microscope (SEM). Read More

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December 2018

Resveratrol modulates fibrillogenesis in a poly‑l‑lysine peptide.

Int J Biol Macromol 2018 Dec 12. Epub 2018 Dec 12.

Faculty of Chemistry, University of Wroclaw, F. Joliot-Curie 14, 50-383 Wroclaw, Poland.

Resveratrol (Res) is an effective inhibitor of amyloid fibril formation and reduces neuron cell toxicity. The effect of Res on the fibrillogenesis of a polar polypeptide, poly‑l‑lysine (PLL), was studied by Fourier-transform infrared spectroscopy, vibrational circular dichroism and transmission electron microscopy. Res molecules exhibited strong and specific inhibition of β-sheet-rich fibrils formed by PLL. Read More

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December 2018

Superparamagnetic Iron Oxides as MPI Tracers: A Primer and Review of early applications.

Authors:
J W M Bulte

Adv Drug Deliv Rev 2018 Dec 12. Epub 2018 Dec 12.

Russell H. Morgan Department of Radiology and Radiological Science, Division of MR Research, Cellular Imaging Section and Vascular Biology Program, Institute for Cell Engineering, Department of Chemical & Biomolecular Engineering, Department of Biomedical Engineering, and Department of Oncology, The Johns Hopkins University School of Medicine, Baltimore, MD 21205, USA. Electronic address:

Magnetic particle imaging (MPI) has recently emerged as a non-invasive, whole body imaging technique that detects superparamagnetic iron oxide (SPIO) nanoparticles similar as those used in magnetic resonance imaging (MRI). Based on tracer "hot spot" detection instead of providing contrast on MRI scans, MPI has already proven to be truly quantitative. Without the presence of endogenous background signal, MPI can also be used in certain tissues where the endogenous MRI signal is too low to provide contrast. Read More

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December 2018

Targeting the CD40-CD40L pathway in autoimmune diseases: Humoral immunity and beyond.

Adv Drug Deliv Rev 2018 Dec 12. Epub 2018 Dec 12.

MedImmune, Gaithersburg, MD 20878, United States. Electronic address:

CD40 is a TNF receptor superfamily member expressed on both immune and non-immune cells. Interactions between B cell-expressed CD40 and its binding partner, CD40L, predominantly expressed on activated CD4+ T cells, play a critical role in promoting germinal center formation and the production of class-switched antibodies. Non-hematopoietic cells expressing CD40 can also engage CD40L and trigger a pro-inflammatory response. Read More

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December 2018

Differential executive functioning in young adulthood as a function of experienced child abuse.

Int J Psychophysiol 2018 Dec 12. Epub 2018 Dec 12.

University of North Dakota, United States of America.

Introduction: Previous research has shown cognitive dysfunction in adults with a history of child abuse. The purpose of the present study was to measure differences that exist in executive functioning skills between individuals who have been abused as children versus those without the history of childhood abuse.

Methods: The present study recruited 43 students from the University of North Dakota (33 women) between ages 18 and 23 years of age. Read More

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December 2018

Resveratrol promotes apoptosis through the induction of dual specificity phosphatase 1 and sensitizes prostate cancer cells to cisplatin.

Food Chem Toxicol 2018 Dec 12. Epub 2018 Dec 12.

Departamento de Bioquímica-Instituto de Investigaciones Biomédicas "Alberto Sols", Universidad Autónoma de Madrid-Consejo Superior de Investigaciones Científicas, Madrid, Spain. Electronic address:

Resveratrol is a polyphenol with chemopreventive properties against prostate cancer; however, the mechanisms underlying its actions are not completely understood. Previously, we demonstrated that DUSP1 induces apoptosis in prostate cancer cells; therefore in the present study we investigated the role of this phosphatase on resveratrol effects. Moreover, we analysed the efficiency of combined treatment of resveratrol and the chemotherapeutic drug cisplatin on cellular viability and apoptosis and its relation with DUSP1 in prostate cancer cells. Read More

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December 2018
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Epinecidin-1: A marine fish antimicrobial peptide with therapeutic potential against Trichomonas vaginalis infection in mice.

Peptides 2018 Dec 12. Epub 2018 Dec 12.

Department and Graduate Institute of Aquaculture, National Kaohsiung University of Science and Technology, Kaohsiung 811, Taiwan. Electronic address:

Trichomoniasis is caused by infection with the protozoan parasite Trichomonas vaginalis, and prolonged persistence may lead to serious ill effects in patients. Thus, the development of new therapeutic strategies to combat drug-resistant T. vaginalis would be clinically beneficial. Read More

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December 2018

Role of mu-opioid agonist efficacy on antinociceptive interactions between mu agonists and the nociceptin opioid peptide agonist Ro 64-6198 in rhesus monkeys.

Eur J Pharmacol 2018 Dec 12. Epub 2018 Dec 12.

Department of Pharmacology and Toxicology, School of Medicine, Virginia Commonwealth University, Richmond, VA, USA. Electronic address:

Mu-opioid receptor agonists are clinically effective analgesics, but also produce undesirable effects that limit their clinical utility. The nociceptin opioid peptide (NOP) receptor system also modulates nociception, and NOP agonists might be useful adjuncts to enhance the analgesic effects or attenuate the undesirable effects of mu-opioid agonists. The present study determined behavioral interactions between the NOP agonist (-)-Ro 64-6198 and mu-opioid ligands that vary in mu-opioid receptor efficacy (17-cyclopropylmethyl-3,14β-dihyroxy-4,5α-epoxy-6α-[(3 ́-isoquinolyl)acetamindo]morphinan (NAQ) < buprenorphine < nalbuphine < morphine = oxycodone < methadone) in male rhesus monkeys. Read More

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December 2018

2-Bromopalmitate sensitizes osteosarcoma cells to adriamycin-induced apoptosis via the modulation of CHOP.

Eur J Pharmacol 2018 Dec 12. Epub 2018 Dec 12.

Institute of Pharmacology and Toxicology, Zhejiang Province Key Laboratory of Anti-Cancer Drug Research, College of Pharmaceutical Sciences, Zhejiang University, Hangzhou, China, 310058. Electronic address:

Osteosarcoma is the most common primary malignant bone tumour, but the survival rate of patients has plateaued since the mid-1980s. Adriamycin is an integral component of the current first-line chemotherapies used for osteosarcoma, but dose-dependent severe side effects often limit its clinical application. Here, we propose a potential combination regimen in which adriamycin plus 2-bromopalmitate, a palmitoylation inhibitor, exhibited powerful therapeutic effects on osteosarcoma. Read More

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December 2018
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LeishInDB: a web-accessible resource for small molecule inhibitors against Leishmania sp.

Acta Trop 2018 Dec 12. Epub 2018 Dec 12.

Department of Molecular Biology/Bioinformatics Centre, Rajendra Memorial Research Institute of Medical Science, Indian Council for Medical Research, Agamkuan, Patna, Bihar 800007. India.

Despite the availability of drugs to treat Leishmaniasis, various other factors including drug resistance and adverse side effects encourage the researchers to search for new strategies and alternatives for treating Leishmaniasis. Repurposing and devising combination therapy with the existing small molecules would serve as an alternative strategy to address the issue, especially the drug resistance. Hence, here we report LeishInDB, a web-accessible resource of small molecule inhibitors having a varying degree of activity towards Leishmania sp. Read More

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December 2018

Darpp-32 and t-Darpp protein products of PPP1R1B: old dogs with new tricks.

Biochem Pharmacol 2018 Dec 12. Epub 2018 Dec 12.

Department of Chemistry and Biochemistry, California State University, Los Angeles, CA, USA. Electronic address:

The PPP1R1B gene is located on chromosome 17q12 (39,626,208-39,636,626[GRCh38/hg38]), which codes for multiple transcripts and two experimentally-documented proteins Darpp-32 and t-Darpp. Darpp-32 (Dopamine and cAMP Regulated Phosphoprotein), discovered in the early 1980s, is a protein whose phosphorylation is upregulated in response to cAMP in dopamine-responsive tissues in the brain. It's phosphorylation profile modulates its ability to bind and inhibit Protein Phosphatase 1 activity, which, in turn, controls the activity of hundreds of phosphorylated proteins. Read More

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December 2018
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