964,609 results match your criteria Pharmaceutical Development and Regulation[Journal]


Characterization of healthy and nonmelanoma-induced mouse utilizing the Stokes-Mueller decomposition.

J Biomed Opt 2018 Dec;23(12):1-8

International University-Vietnam National University HCMC, Department of Biomedical Engineering, Ho, Vietnam.

Skin cancer is one of the most common cancers, including melanoma and nonmelanoma cancer. Melanoma can be easily detected by the observation of abnormal moles, but nonmelanoma signs and symptoms are not apparent in the early stages. We use the Stokes-Mueller matrix decomposition method to detect nonmelanoma at the early stage by decomposing the characteristics of polarized light interacting with normal and cancerous tissues. Read More

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December 2018
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UV-B-activated B16 melanoma cells or HaCaT keratinocytes increase melanogenesis via ANGPTL2 induction, an activity antagonized by Chrysanthemum extract.

Exp Dermatol 2018 Dec 16. Epub 2018 Dec 16.

Department of Molecular Genetics, Graduate School of Medical Sciences, Kumamoto University, Kumamoto, Japan.

Sunburn causes inflammation, which increases melanin production in skin and causes hyperpigmentation. Angiopoietin-like protein (ANGPTL) 2 is an inflammatory mediator induced in sun-exposed skin areas. However, whether ANGPTL2 functions in melanin production remains unclear. Read More

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December 2018
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In vitro and in vivo evidence of tyrosinase inhibitory activity of a synthesized (Z)-5-(3-hydroxy-4-methoxybenzylidene)-2-thioxothiazolidin-4-one (5-HMT).

Exp Dermatol 2018 Dec 15. Epub 2018 Dec 15.

Molecular Inflammation Research Center for Aging Intervention (MRCA), College of Pharmacy, Pusan National University, Busan, 46241, Republic of Korea.

Tyrosinase is a key enzyme that catalyzes the initial rate-limiting steps of melanin synthesis. Due to its critical role in melanogenesis, various attempts were made to find potent tyrosinase inhibitors although many were not safe and effective in vivo. We evaluated tyrosinase inhibitory activity of six compounds. Read More

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December 2018
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Immunohistochemical study of four fish tumors.

J Aquat Anim Health 2018 Dec 16. Epub 2018 Dec 16.

Dept. of Veterinary Sciences, Polo Universitario dell'Annunziata, University of Messina, 98168, Messina, Italy.

The present study supports the usefulness of ancillary techniques such as immunohistochemistry as a valid diagnostic tool in the field of fish oncology. The immunohistochemical patterns observed in four neoplasms, in four individual teleosts belonging to different species are here described. Cytokeratin, vimentin, actin, S-100, calretinin, and melan A antibodies were used. Read More

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December 2018

Fucoxanthin prevents lipopolysaccharide-induced depressive-like behavior in mice via AMPK- NF-κB pathway.

Metab Brain Dis 2018 Dec 15. Epub 2018 Dec 15.

Department of Pharmacy, Institute of toxicology and pharmacology, Zhejiang Pharmaceutical College, Ningbo, 315000, China.

Fucoxanthin (FX), a natural carotenoid abundant in edible brown seaweeds, has been shown the great anti-oxidant, anti-inflammatory and anti-diabetic effects in vivo and in vitro. The present study was designed to investigate the effects of FX on lipopolysaccharide (LPS)-induced behavioral defects in mice. In depressive behavior tests, the increased immobility time of forced swimming test and tail suspension test by LPS treatment in mice, which were significantly reversed by FX treatment (200 mg/kg, i. Read More

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December 2018

Gut microbiome approaches to treat obesity in humans.

Appl Microbiol Biotechnol 2018 Dec 16. Epub 2018 Dec 16.

Department of Food and Nutrition, School of Pharmaceutical Sciences, State University of São Paulo (UNESP), Araraquara, SP, Brazil.

The rising worldwide prevalence of obesity has become a major concern having many implications for the public health and the economy. It is well known that many factors such as lifestyle, increased intake of foods high in fat and sugar and a host's genetic profile can lead to obesity. Besides these factors, recent studies have pointed to the gut microbiota composition as being responsible for the development of obesity. Read More

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December 2018

The effect of hyperosmolality application time on production, quality, and biopotency of monoclonal antibodies produced in CHO cell fed-batch and perfusion cultures.

Appl Microbiol Biotechnol 2018 Dec 15. Epub 2018 Dec 15.

Shanghai Taiyin Biotech Co., Ltd., Shanghai, 201203, China.

Hyperosmolality has been commonly investigated due to its effects on the production and quality characteristics of monoclonal antibodies (mAbs) produced in CHO cell fed-batch cultures. However, the application of hyperosmolality at different times and its effect on biopotency have seldom been researched, especially in perfusion culture. In our study, different degrees of hyperosmolality induced by sodium chloride were investigated in anti-IgE rCHO cell fed-batch cultures and anti-CD52 rCHO cell perfusion cultures during the initial and stable phases. Read More

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December 2018

Salivary Nickel and Chromium Levels in Orthodontic Patients with and Without Periodontitis: a Preliminary Historical Cohort Study.

Biol Trace Elem Res 2018 Dec 15. Epub 2018 Dec 15.

Pharmaceutical Chemistry, North Branch, Islamic Azad University, Tehran, Iran.

Many periodontal patients may need orthodontic treatment. Alterations in oral environment particularly the reduction of pH in periodontal patients could affect metal ion release from orthodontic appliances. However, there is no study on metal ion release in periodontal patients. Read More

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December 2018

Comparative effectiveness of Sumaq and Neem extract cream, Eniloconazole and glycerine iodine on dermatophytosis in Arabian horses: a randomized clinical trial.

Trop Anim Health Prod 2018 Dec 15. Epub 2018 Dec 15.

Department of Pharmacognosy, Faculty of Pharmacy, Mansoura University, Mansoura, 35516, Egypt.

Dermatophytosis is a contagious fungal disease among animal communities. The major concerns of dermatophytosis are cost of treatment, difficulty of control, and the public health consequences. The objective of the present study was to compare the clinical efficacy of Sumaq and Neem extract cream with that of traditional treatments, eniloconazole and glycerine iodine, on dermatophytosis in Arabian horses. Read More

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December 2018

Molecular and NLO Properties of Red Fluorescent Coumarins - DFT Computations Using Long-Range Separated and Conventional Functionals.

J Fluoresc 2018 Dec 15. Epub 2018 Dec 15.

Computational Chemistry Group, Department of Chemistry, Faculty of Science, University of Mauritius, Réduit, 80832, Mauritius.

Comparative study of nonlinear optical properties of red fluorescent coumarins was carried out with density functional theory based ab initio method using the popular global hybrid (GH) and range separated hybrid (RSH) functionals and correlated with the spectroscopic values. The GHs - M06 L, PBE1PBE, M06, BHHLYP, M062X and M06HF and RSHs - HISSbPBE, wB97, wB97X, HSEH1PBE, CAM-B3LYP and wB97XD in combination with the double zeta basis function 6-311 + G(d,p) were used. The computed polarizability (α), hyperpolarizability of the first order (β) and second order (γ) computed by the RSHs are closer to the spectroscopic values compared to GHs. Read More

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December 2018

A star-shaped molecularly imprinted polymer derived from polyhedral oligomeric silsesquioxanes with improved site accessibility and capacity for enantiomeric separation via capillary electrochromatography.

Mikrochim Acta 2018 Dec 15;186(1):22. Epub 2018 Dec 15.

Tianjin Key Laboratory on Technologies Enabling Development of Clinical Therapeutics and Diagnostics (Theranostics), School of Pharmacy, Tianjin Medical University, Tianjin, 300070, China.

A star-shaped molecularly imprinted coating was prepared starting from octavinyl-modified polyhedral oligomeric silsesquioxanes (Ov-POSS). It possesses a relatively open structure and has good site accessibility and a larger capacity even at lower cross-linking. The imprinted coating was prepared from S-amlodipine (S-AML) as the template and analyte, Ov-POSS as the cross-linker, and methacrylic acid as the functional monomer. Read More

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December 2018

Pharmacokinetics of meropenem in plasma and cerebrospinal fluid in patients with intraventricular hemorrhage after lateral ventricle drainage.

Eur J Clin Pharmacol 2018 Dec 15. Epub 2018 Dec 15.

Department of Emergency Internal Medicine, The First Affiliated Hospital of Bengbu Medical College, Bengbu, 233004, China.

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December 2018

Molecular Basis of Cystinosis: Geographic Distribution, Functional Consequences of Mutations in the CTNS Gene, and Potential for Repair.

Nephron 2018 Dec 14;141(2):1-14. Epub 2018 Dec 14.

Department of Development and Regeneration, Organ Systems Cluster, KU Leuven, Leuven,

Mutations in the CTNS gene encoding the lysosomal membrane cystine transporter cystinosin are the cause of cystinosis, an autosomal recessive lysosomal storage disease. More than 140 CTNS mutations have been reported worldwide. Recent studies have discovered that cystinosin exerts other key cellular functions beyond cystine transport such as regulation of oxidative state, lysosomal dynamics and autophagy. Read More

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December 2018

Role of TLR4 in the gut-brain axis in Parkinson's disease: a translational study from men to mice.

Gut 2018 Dec 15. Epub 2018 Dec 15.

Division of Pharmacology, Utrecht Institute for Pharmaceutical Sciences, Faculty of Science, Utrecht University, Utrecht, The Netherlands.

Objective: Recent evidence suggesting an important role of gut-derived inflammation in brain disorders has opened up new directions to explore the possible role of the gut-brain axis in neurodegenerative diseases. Given the prominence of dysbiosis and colonic dysfunction in patients with Parkinson's disease (PD), we propose that toll-like receptor 4 (TLR4)-mediated intestinal dysfunction could contribute to intestinal and central inflammation in PD-related neurodegeneration.

Design: To test this hypothesis we performed studies in both human tissue and a murine model of PD. Read More

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December 2018

A step towards development of promising trypanocidal agents: Synthesis, characterization and in vitro biological evaluation of ferrocenyl Mannich base-type derivatives.

Eur J Med Chem 2018 Dec 4;163:569-582. Epub 2018 Dec 4.

Dipartimento di Scienze e Innovazione Tecnologica, Università del Piemonte Orientale, Viale T. Michel 11, 15121, Alessandria, Italy. Electronic address:

Chagas disease is a neglected chronical parasitosis caused by the parasite Trypanosoma cruzi (T. cruzi). Nine ferrocenyl Mannich base derivatives were synthetized and characterized to explore their in vitro activity on three T. Read More

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December 2018

Synthesis, structure activity relationship and in vitro anti-influenza virus activity of novel polyphenol-pentacyclic triterpene conjugates.

Eur J Med Chem 2018 Dec 7;163:560-568. Epub 2018 Dec 7.

State Key Laboratory of Natural and Biomimetic Drugs, School of Pharmaceutical Sciences, Peking University, Beijing 100191, China; State Key Laboratory of Phytochemistry and Plant Resources in West China, Kunming Institute of Botany, Chinese Academy of Sciences, Kunming 650201, China. Electronic address:

It is urgently necessary to develop more effective anti-influenza agents due to the continuous emergence of drug-resistant strains of influenza virus. Our earlier studies have identified that certain pentacyclic triterpene derivatives are effective inhibitors of influenza virus infection. In the present study, a series of C-28 modified pentacyclic triterpene derivatives via conjugation with a series of polyphenols were synthesized, and their antiviral activities against influenza A/WSN/33 (H1N1) virus in MDCK (Madin-Darby canine kidney) cells were evaluated. Read More

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December 2018

Cabazitaxel and silibinin co-encapsulated cationic liposomes for CD44 targeted delivery: A new insight into nanomedicine based combinational chemotherapy for prostate cancer.

Biomed Pharmacother 2018 Dec 13;110:803-817. Epub 2018 Dec 13.

Department of Pharmaceutics, National Institute of Pharmaceutical Education & Research (NIPER), Hyderabad 500037, India. Electronic address:

Cancer stem cells (CSCs) are the promising targets for cancer chemotherapy that cannot be eliminated by conventional chemotherapy. In this study cationic liposomes of cabazitaxel (CBX) and silibinin (SIL) were prepared with an aim to kill cancer cells and CSCs for prostate cancer. CBX act as cancer cell inhibitor and SIL as CSC inhibitor. Read More

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December 2018

Therapeutic targeting of angiogenesis molecular pathways in angiogenesis-dependent diseases.

Biomed Pharmacother 2018 Dec 13;110:775-785. Epub 2018 Dec 13.

Biotechnology Research Center, Tabriz University of Medical Sciences, Tabriz, Iran; Department of Pharmaceutical Biotechnology, Faculty of Pharmacy, Tabriz University of Medical Sciences, Tabriz, Iran; Molecular Medicine Research Centre, Tabriz University of Medical Sciences, Tabriz, Iran. Electronic address:

Angiogenesis is a critical step in the progression of almost all human malignancies and some other life-threatening diseases. Anti-angiogenic therapy is a novel and effective approach for treatment of angiogenesis-dependent diseases such as cancer, diabetic retinopathy, and age-related macular degeneration. In this article, we will review the main strategies developed for anti-angiogenic therapies beside their clinical applications, the major challenges, and the latest advances in the development of anti-angiogenesis-based targeted therapies. Read More

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December 2018

Fiend and friend in the renin angiotensin system: An insight on acute kidney injury.

Biomed Pharmacother 2018 Dec 13;110:764-774. Epub 2018 Dec 13.

Laboratory of Molecular Pharmacology, Department of Pharmacy, Birla Institute of Technology and Science, Pilani, Pilani Campus, Rajasthan 333 031, India. Electronic address:

Besides assisting the maintenance of blood pressure and sodium homeostasis, the renin-angiotensin system (RAS) plays a pivotal role in pathogenesis of acute kidney injury (AKI). The RAS is equipped with two arms i) the pressor arm composed of Angiotensin II (Ang II)/Angiotensin converting enzyme (ACE)/Angiotensin II type 1 receptor (AT1R) also called conventional RAS, and ii) the depressor arm consisting of Angiotensin (1-7) (Ang 1-7)/Angiotensin converting enzyme 2 (ACE2)/MasR known as non-conventional RAS. Activation of conventional RAS triggers oxidative stress, inflammatory, hypertrophic, apoptotic, and pro-fibrotic signaling cascades which promote AKI. Read More

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December 2018

N-Alkyl-1,5-dideoxy-1,5-imino-l-fucitols as fucosidase inhibitors: Synthesis, molecular modelling and activity against cancer cell lines.

Bioorg Chem 2018 Dec 4;84:418-433. Epub 2018 Dec 4.

School of Chemistry, National University of Ireland Galway, University Road, Galway H91 TK33, Ireland. Electronic address:

1,5-Dideoxy-1,5-imino-l-fucitol (1-deoxyfuconojirimycin, DFJ) is an iminosugar that inhibits fucosidases. Herein, N-alkyl DFJs have been synthesised and tested against the α-fucosidases of T. maritima (bacterial origin) and B. Read More

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December 2018

Design, synthesis and biological evaluation of novel indole derivatives as potential HDAC/BRD4 dual inhibitors and anti-leukemia agents.

Bioorg Chem 2018 Dec 10;84:410-417. Epub 2018 Dec 10.

Key Laboratory of Structure-Based Drugs Design & Discovery of Ministry of Education, Shenyang Pharmaceutical University, Shenyang 110016, China. Electronic address:

HDAC inhibitors and BRD4 inhibitors were considered to be potent anti-cancer agents. Recent studies have demonstrated that HDAC and BRD4 participate in the regulation of some signal paths like PI3K-AKT. In this work, a series of indole derivatives that combine the inhibitory activities of BRD4 and HDAC into one molecule were designed and synthesized through the structure-based design method. Read More

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December 2018

Synthesis, characterization, DNA binding, topoisomerase I inhibition and antiproliferation activities of three new functionalized terpyridine platinum(II) complexes.

J Inorg Biochem 2018 Dec 7;192:17-24. Epub 2018 Dec 7.

Jiangxi Provincial Key Laboratory of Drug Design and Evaluation, School of Pharmacy, Jiangxi Science & Technology Normal University, Nanchang 330013, PR China. Electronic address:

Three new platinum(II) complexes with pendent morpholine were synthesized, namely complex 1 ([Pt(L)Cl]CFSO), complex 2 ([Pt(L)(NH)](CFSO)) and complex 3 ([Pt(L)(PPh)](CFSO)), where L = 4'-[4-(4-morpholinobutyloxy)phenyl]-2,2':6',2″-terpyridine and PPh = triphenylphosphine. The detailed molecular structures of complex 3, L and its precursor L' (1,4'-[4-(4-bromobutyloxy)phenyl]-2,2':6',2″-terpyridine) were determined by single crystal X-ray diffraction. An evaluation of in vitro cytotoxicity for both ligand and complexes was performed by methyl thiazolyl tetrazolium (MTT) assay in three cancer cell lines and normal cells as the control, respectively. Read More

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December 2018

Gender-specific prevalence of poor sleep quality and related factors in a Chinese rural population: the Henan Rural Cohort Study.

Sleep Med 2018 Nov 22;54:134-141. Epub 2018 Nov 22.

Department of Epidemiology and Biostatistics, College of Public Health, Zhengzhou University, Zhengzhou, Henan, PR China. Electronic address:

Objective: To estimate the prevalence of poor sleep quality and identify related factors by gender in the Chinese rural population.

Methods: Overall, 27424 subjects (10881 males and 16543 females) aged 18-79 years were enrolled from the Henan Rural Cohort Study. Sleep quality was evaluated by the standard Pittsburgh Sleep Quality Index (PSQI) and global score>5 was classified as poor sleep quality. Read More

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November 2018

Association between prenatal opioid exposure, neonatal opioid withdrawal syndrome, and neurodevelopmental and behavioral outcomes at 5-8 months of age.

Early Hum Dev 2018 Dec 13;128:69-76. Epub 2018 Dec 13.

Department of Family and Community Medicine, School of Medicine, University of New Mexico, Albuquerque, NM, United States of America.

Background: While use of prescription opioids and medication assisted therapy (MAT) for opioid use disorder in pregnancy, as well as the incidence of neonatal opioid withdrawal syndrome (NOWS) continue to rise, little is known about outcomes for children with NOWS beyond the newborn period.

Methods: We examined 1) prenatal MAT exposure vs. unexposed healthy controls [HC]; and 2) treatment for NOWS and NOWS severity on infant neurodevelopmental and behavioral outcomes at 5-8 months of age in 78 maternal-infant pairs from the ENRICH prospective cohort study. Read More

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December 2018

Redox-responsive polymer inhibits macrophages uptake for effective intracellular gene delivery and enhanced cancer therapy.

Colloids Surf B Biointerfaces 2018 Dec 7;175:392-402. Epub 2018 Dec 7.

College of Pharmaceutical Sciences, Zhejiang University, 866 Yuhangtang Road, Hangzhou, 310058, China. Electronic address:

The development of advanced gene delivery carriers with stimuli-responsive release manner for tumor therapeutics is desirable, since they can exclusively release the therapeutic gene via their structural changes in response to the specific stimuli of the target site. Moreover, interactions between macrophages and drug delivery systems (DDSs) seriously impair the treatment efficiency of DDSs, thus macrophages uptake inhibition would to some extent improve the intracellular uptake of DDSs in tumor cells. Herein, a PEGylated redox-responsive gene delivery system was developed for effective cancer therapy. Read More

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December 2018

In-situ forming gels containing fluorometholone-loaded polymeric nanoparticles for ocular inflammatory conditions.

Colloids Surf B Biointerfaces 2018 Nov 27;175:365-374. Epub 2018 Nov 27.

Department of Pharmacy, Pharmaceutical Technology and Physical Chemistry, Faculty of Pharmacy and Food Sciences, University of Barcelona, 08028, Barcelona, Spain; Institute of Nanoscience and Nanotechnology (IN2UB), University of Barcelona, Barcelona, Spain. Electronic address:

Thermosensitive gels have been developed and optimized in such a way that they become gels at corneal temperature and with a viscosity that allows the adequate release of the Fluorometholone (FMT)-loaded PLGA nanoparticles (NPs) in order to improve ocular anti-inflammatory efficacy against a commercial formulation. It has been shown that gels avoid burst release of the drug in the first hours with a slow and increasing profile after administration. NPs have maintained their average size and spherical shape within the gels as confirmed by transmission electron microscopy (TEM). Read More

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November 2018

Understanding the kinetic mixing between liquid crystalline nanoparticles and agrochemical actives.

Colloids Surf B Biointerfaces 2018 Nov 27;175:324-332. Epub 2018 Nov 27.

Drug Delivery, Disposition and Dynamics, Monash Institute of Pharmaceutical Sciences, Monash University (Parkville Campus), 381 Royal Parade Parkville, Victoria, 3052, Australia; ARC Centre of Excellence in Convergent Bio-Nano Science and Technology, Monash Institute of Pharmaceutical Sciences, Monash University (Parkville Campus), 381 Royal Parade Parkville, Victoria, 3052, Australia. Electronic address:

The use of liquid crystalline nanoparticles as potential agrochemical delivery agents or adjuvant systems is gaining traction due to the possibility that the systems can enhance penetration of the active and increase adhesion of the formulation to the leaf, increasing overall efficacy and decreasing the harmful environmental impact. However the interaction between liquid crystalline nanoparticles and active products is not well understood. Using small angle X-ray scattering we investigated the structural changes that occur to liquid crystalline nanoparticles upon addition of three common herbicides, 2,4-D 2-ethylhexyl ester, bromoxynil octanoate and haloxyfop-p-methyl ester active agrochemicals in the form of emulsions. Read More

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November 2018

Evaluation of the protective effect of Myrtus communis in scopolamine-induced Alzheimer model through cholinergic receptors.

Gene 2018 Dec 13. Epub 2018 Dec 13.

Department of Pharmacology, Faculty of Pharmacy, Marmara University, Istanbul, Turkey.

Alzheimer's disease is a progressive neurodegenerative disorder causing common health problem with increasing age. Evidences show that the key symptoms of AD are mainly caused by cholinergic system dysfunction which has a role in cognitive disorders. Cholinergic pathways especially muscarinic receptors like M subtype also have a major role in learning, memory, cognitive functions and emotional state. Read More

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December 2018

μImpact of a nursing-driven sedation protocol with criteria for infusion initiation in the surgical intensive care unit.

J Crit Care 2018 Nov 30;50:195-200. Epub 2018 Nov 30.

Department of Pharmacy, The Ohio State University Wexner Medical Center, 410 W. 10th Avenue, Columbus, OH 43210, USA. Electronic address:

Purpose: Analgesia and sedation protocols (ASPs) reduce duration of mechanical ventilation (MV) in the medical intensive care unit (ICU), but data in the surgical ICU (SICU) are limited. The objective of this study was to determine the impact of a nursing-driven ASP with criteria for infusion initiation in the SICU.

Materials And Methods: A single-center, retrospective study compared ventilator-free days at day 28 from start of MV (VFD28) before and after ASP implementation. Read More

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November 2018

Regional differences in the treatment of refractory vasodilatory shock using Angiotensin II in High Output Shock (ATHOS-3) data.

J Crit Care 2018 Dec 8;50:188-194. Epub 2018 Dec 8.

Division of Pulmonary, Critical Care, Allergy and Sleep Medicine, Emory University, Atlanta, GA, United States.

Introduction: Despite international guidelines, regional differences in treatment of vasodilatory shock remain. We characterized these differences using data from Angiotensin II in High Output Shock (ATHOS-3) trial.

Methods: The 321 patients treated in the ATHOS-3 trial were included. Read More

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December 2018

A novel in vitro co-culture model to examine contact formation between astrocytic processes and cerebral vessels.

Exp Cell Res 2018 Dec 13. Epub 2018 Dec 13.

Laboratory of Medical Pharmaceutics, Kobe Pharmaceutical University, Kobe 658-8558, Japan. Electronic address:

Here, we developed a novel in vitro co-culture model, in which process-bearing astrocytes and isolated cerebral microvessels from mice were co-cultured. Astrocytes formed contacts with microvessels from both adult and neonatal mice. However, concentrated localization of the immunofluorescence signal for aquaporin-4 (AQP4) at contact sites between perivascular endfoot processes and blood vessels was only detected with neonatal mouse microvessels. Read More

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December 2018

How changes in molecular weight and PDI of a polymer in amorphous solid dispersions impact dissolution performance.

Int J Pharm 2018 Dec 13. Epub 2018 Dec 13.

Institute of Pharmacy, Faculty I of Natural Sciences, Martin Luther University Halle-Wittenberg, Wolfgang-Langenbeck-Str. 4, 06120, Halle/Saale, Germany. Electronic address:

Polymers functionally contribute to supersaturation and precipitation inhibition of the active pharmaceutical ingredient (API) in amorphous solid dispersions (ASD). Therefore, it is necessary to monitor physicochemical changes of the polymeric carrier caused by the manufacturing process. This is especially important when the material is exposed to heat and shear stress as in case of hot-melt extrusion (HME). Read More

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December 2018

Gelatin-based Hydrogels as Potential Biomaterials for Colonic Delivery of Oxaliplatin.

Int J Pharm 2018 Dec 13. Epub 2018 Dec 13.

Faculty of Pharmacy, The University of Lahore, Pakistan; International Joint Laboratory for Nuclear Protein Regulation, Henan University, Kaifeng, China.

In present investigation, gelatin-based (AA-co-AMPS) hydrogels were prepared using N, N'-Methylenebisacrylamide (MBA) as a cross-linker and ammonium per sulfate (APS) as an initiator. The successful crosslinking and network formation was confirmed by Fourier transform infrared spectroscopy (FT IR). Differential scanning calorimetry (DSC) and thermogravimetric analysis (TGA) investigations proved the higher thermal stability and successful entrapment of oxaliplatin (OXP) in the polymeric network. Read More

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December 2018

Self-implanted tiny needles as alternative to traditional parenteral administrations for controlled transdermal drug delivery.

Int J Pharm 2018 Dec 13. Epub 2018 Dec 13.

Beijing Laboratory of Biomedical Materials, College of Materials Science and Engineering, Beijing University of Chemical Technology, Beijing, 100029, P.R. China. Electronic address:

Controlled drug-delivery systems have potential as substitutes for traditional medication systems due to the advantages in safety, efficacy, and patient compliance that these long-acting dosage forms provide. In this context, the present study focus on the development of self-implanted hyaluronicacid (HA) tiny needles that encapsulate ivermectin (IVM)-poly (lactic-co-glycolic acid) (PLGA) microparticles for controlled transdermal IVM release to treat parasitic diseases. The fabricated tiny needles involved matching portable applicator have potentially able for self-administration by patients without intense pain or complexity of current controlled-release devices. Read More

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December 2018
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Exposure to tobacco smoke during the early postnatal period modifies receptors and enzymes of the endocannabinoid system in the brainstem and striatum in mice.

Toxicol Lett 2018 Dec 13. Epub 2018 Dec 13.

Department of Clinical and Toxicological Analysis, School of Pharmaceutical Sciences, University of São Paulo, Av. Prof. Lineu Prestes, 580, bloco 13B, 05508-000, São Paulo, SP, Brazil. Electronic address:

Environmental tobacco smoke (ETS) exposure during brain development has been associated with several disorders, such as depression, anxiety, sudden infant death syndrome, and the predisposition to addiction. The endocannabinoid system plays an essential role in neuronal development. We investigated the effects of early postnatal ETS exposure on the endocannabinoid system in different brain regions. Read More

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December 2018

The concentration of dissolved organic matter impacts the metabolic response in Daphnia magna exposed to 17α-ethynylestradiol and perfluorooctane sulfonate.

Ecotoxicol Environ Saf 2018 Dec 13;170:468-478. Epub 2018 Dec 13.

Department of Chemistry, University of Toronto, 80 St. George Street, Toronto, ON, Canada M5S 3H6; Environmental NMR Centre and Department of Physical and Environmental Sciences, University of Toronto Scarborough, 1265 Military Trail, Toronto, ON, Canada M1C 1A4. Electronic address:

The pharmaceutical 17α-ethynylestradiol (EE2) and the industrial chemical perfluorooctane sulfonate (PFOS) are organic contaminants frequently detected in freshwater environments. It is hypothesized that hydrophobic organic contaminants can sorb to dissolved organic matter (DOM) and this may reduce the toxicity of these contaminants by reducing the contaminants' bioavailability. To investigate this hypothesis, H nuclear magnetic resonance (NMR)-based metabolomics was used to determine how the metabolome of Daphnia magna changes when a range of DOM concentrations are added during EE2 and PFOS exposure experiments. Read More

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December 2018

Betulinic acid inhibits the migration and invasion of fibroblast-like synoviocytes from patients with rheumatoid arthritis.

Int Immunopharmacol 2018 Dec 13;67:186-193. Epub 2018 Dec 13.

Formula-pattern Research Center, School of Traditional Chinese Medicine, Jinan University, Guangzhou, Guangdong, China. Electronic address:

The aggressive phenotype displayed by fibroblast-like synoviocytes (FLSs) contributes to cartilage and bone destruction in rheumatoid arthritis (RA). Betulinic acid has been demonstrated to have a positive therapeutic effect on tumor, inflammation and immune disorder, however, the effects of betulinic acid on RA FLSs have not been verified. Therefore, in the present study, we observed the effect of betulinic acid on the migration and invasion of RA FLSs and explored its underlying signal mechanisms. Read More

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December 2018

Human α-casein induces IL-8 secretion by binding to the ecto-domain of the TLR4/MD2 receptor complex.

Biochim Biophys Acta Gen Subj 2018 Dec 13. Epub 2018 Dec 13.

Institute of Pharmaceutical and Medicinal Chemistry, PharmaCampus, Westphalian Wilhelms-University, Corrensstr. 48, 48149 Münster, Germany. Electronic address:

Background: The milk protein α-casein was recently reported to induce secretion of proinflammatory cytokines via Toll-like receptor 4 (TLR4). In this study, α-casein was identified as binder of theTLR4 ecto domain.

Methods: IL-8 secretion after stimulation of TLR4/MD2 (myeloid differentiation factor 2)/CD14 (cluster of differentiation 14)-transfected HEK293 cells (TLR4) and Mono Mac 6 cells (MM6) with recombinant α-casein, or LPS as control was monitored. Read More

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December 2018

Structural alteration of glycosaminoglycan side chains and spatial disorganization of collagen networks in the skin of patients with mcEDS-CHST14.

Biochim Biophys Acta Gen Subj 2018 Dec 13. Epub 2018 Dec 13.

Laboratory of Anatomy, School of Veterinary Medicine, Rakuno Gakuen University, Ebetsu, Hokkaido, Japan. Electronic address:

Musculocontractural Ehlers-Danlos syndrome (mcEDS) due to CHST14/D4ST1 deficiency (mcEDS-CHST14) is a recently delineated type of EDS caused by biallelic loss-of-function mutations in CHST14, which results in the depletion of dermatan sulfate (DS). Clinical characteristics of mcEDS-CHST14 consist of multiple malformations and progressive fragility-related manifestations, including skin hyperextensibility and fragility. Skin fragility is suspected to result from the impaired assembly of collagen fibrils caused by alteration of the glycosaminoglycan (GAG) chain of decorin-proteoglycan (PG) from DS to chondroitin sulfate (CS). Read More

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December 2018
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Effect of polymer concentration and solution pH on viscosity affecting integrity of a polysaccharide coat of compression coated tablets.

Int J Biol Macromol 2018 Dec 13. Epub 2018 Dec 13.

Division of Pharmaceutics, Department of Pharmaceutical Technology, Jadavpur University, Kolkata 700032, West Bengal, India.

Tablets, compression coated with certain polysaccharides and intended for colon delivery, retain the integrity of the coat for an initial period of about 6 h (lag period) beyond which (post-lag period) the coat is degraded by colonic enzymes to induce drug release. This work was undertaken to investigate the factors which influence the integrity of the coat during the lag period. Core tablets containing two model drugs were compression coated with various amounts of carboxymethyl locust bean gum (CMLBG). Read More

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December 2018

Characterizations and immunostimulatory activities of a polysaccharide from Arnebia euchroma (Royle) Johnst. roots.

Int J Biol Macromol 2018 Dec 13. Epub 2018 Dec 13.

College of Pharmacy, Inner Mongolia Medical University, Hohhot, Inner Mongolia Jinshan Development Zone, 010110, China. Electronic address:

A polysaccharide from Arnebia euchroma (Royle) Johnst. named ARP, was obtained and purified by the hot water extraction, ethanol precipitation and deproteinization of TCA. The molecular weight of the polysaccharide fraction of ARP was calculated to be 1. Read More

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December 2018

Grafted hyaluronic acid N-acetyl-l-methionine for targeting of LAT1 receptor: In-silico, synthesis and microscale thermophoresis studies.

Int J Biol Macromol 2018 Dec 13. Epub 2018 Dec 13.

Discipline of Pharmaceutical Sciences, College of Health Sciences, University of KwaZulu-Natal, Private Bag X54001, Durban, South Africa. Electronic address:

Neutral amino acids can be delivered into cells through the l-type amino acid transporter-1 (LAT1), which is a sodium independent transporter. The LAT1 protein is expressed in different tissues, including kidney, blood brain barrier and intestinal wall hence LAT1 can be used as a target in diseases associated with its overexpression. In-silico interactions between different ligands, including methionine (Met), N-acetyl-l-methionine (AcMet), hyaluronic acid (HA), grafted hyaluronic-acid l-methionine (HA-ADH-Met) and a novel grafted hyaluronic acid-N-acetyl-l-methionine (HA-ADH-AcMet), which are at the active site of the LAT1 transporter, was studied and the binding energies calculated. Read More

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December 2018

Current state of the polymeric delivery systems of fluoroquinolones - A review.

J Control Release 2018 Dec 13. Epub 2018 Dec 13.

Department of Biomaterials Chemistry, Chair of Analytical Chemistry and Biomaterials, Faculty of Pharmacy With the Laboratory Medicine Division, Medical University of Warsaw, 1 Banacha St., Warsaw 02-097, Poland. Electronic address:

Recently, growing interest in polymers (natural and synthetic) as drug carriers in controlled release formulations and drug targeting systems that may improve the efficacy of treatment and reduce the side effects of a drug therapy, has been observed. Special attention has been paid to improving the effectiveness of antibiotics, which constitute a very important, often life-saving group of drugs. In this paper, we review polymers as macromolecular carriers of fluoroquinolones, a group of antibiotics with a broad spectrum of activity. Read More

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December 2018

Rational combination immunotherapeutic approaches for effective cancer treatment.

J Control Release 2018 Dec 13. Epub 2018 Dec 13.

College of Pharmacy, Yeungnam University, 280 Deahak-ro, Gyeongsan 38541, Republic of Korea. Electronic address:

Immunotherapy is an important mode of cancer treatment. Over the past decades, immunotherapy has improved the clinical outcome for cancer patients. However, in many cases, mutations in cancer cells, lack of selectivity, insufficiency of tumor-reactive T cells, and host immunosuppression limit the clinical benefit of immunotherapy. Read More

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December 2018

Mesenchymal stem cell-based drug delivery strategy: from cells to biomimetic.

J Control Release 2018 Dec 13. Epub 2018 Dec 13.

Institute of Pharmaceutics, College of Pharmaceutical Sciences, Zhejiang University, PR China; Dr. Li Dak Sum & Yip Yio Chin Center for Stem Cell and Regenerative Medicine, Zhejiang University, Hangzhou, Zhejiang, PR China. Electronic address:

Owing to the diversity and ease of preparation of nanomaterials, the rational nanocarriers with a rational design have become increasingly popular in medical researches. Although nanoparticle-based drug delivery exhibits great potential, there are some challenges facing like rapid plasma clearance, triggering or aggravation of immune response, etc. Herein, cell-based targeted drug delivery systems have drawn more and more attention owing to low immunogenicity and intrinsic mutation rate, and innate ability to allow targeted delivery. Read More

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December 2018

A comprehensive analysis of the protein-ligand interactions in crystal structures of Mycobacterium tuberculosis EthR.

Biochim Biophys Acta Proteins Proteom 2018 Dec 13. Epub 2018 Dec 13.

Unité Microbiologie, Bioorganique et Macromoléculaire (CP206/04), département R3D, Faculté de Pharmacie, Université Libre de Bruxelles, B-1050 Brussels, Belgium. Electronic address:

The Mycobacterium tuberculosis EthR is a member of the TetR family of repressors, controlling the expression of EthA, a mono-oxygenase responsible for the bioactivation of the prodrug ethionamide. This protein was established as a promising therapeutic target against tuberculosis, allowing, when inhibited by a drug-like molecule, to boost the action of ethionamide. Dozens of EthR crystal structures have been solved in complex with ligands. Read More

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December 2018

The critical role of microRNAs in stress response: therapeutic prospect and limitation.

Pharmacol Res 2018 Dec 13. Epub 2018 Dec 13.

Department of Pharmacy, Xiangya Hospital, Central South University, Changsha, 410008, China; National Clinical Research Center for Geriatric Disorders (XIANGYA), Xiangya Hospital, Central South University, Changsha, 410008, Hunan, China. Electronic address:

Stress response refers to the systemic nonspecific response upon exposure to strong stimulation or chronic stress, such as severe trauma, shock, infection, burn, major surgery or improper environment, which disturb organisms and damage their physical and psychological health. However, the pathogenesis of stress induced disorder remains complicated and diverse under different stress exposure. Recently, studies have revealed a specific role of microRNAs (miRNAs) in regulating cellular function under different types of stress, suggesting a significant role in the treatment and prevention of stress-related diseases, such as stress ulcer, posttraumatic stress disorder, stress-induced cardiomyopathy and so on. Read More

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December 2018

Alzheimer's disease: understanding homeostasis deregulation to foster development of effective therapies.

Pharmacol Res 2018 Dec 13. Epub 2018 Dec 13.

GRAP UMR1247, INSERM, Centre Universitaire de Recherche en Santé, Université de Picardie Jules Verne, Amiens, France. Electronic address:

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December 2018

Full thickness intraoral mucosa barrier models for in vitro drug permeation studies employing microneedles.

J Pharm Sci 2018 Dec 13. Epub 2018 Dec 13.

Department of Physiological Sciences, Piracicaba Dental School, University of Campinas, Piracicaba, São Paulo, Brazil. Electronic address:

The use of permeation enhancers such as microneedles (MNs) to increase drug penetration across intraoral mucosa has increased in recent years. Permeation studies, commonly performed using vertical diffusion cells, are a well-established way to preview formulations and enhance their performance during the development stage. However, to our knowledge, the existing intraoral mucosa barrier models do not permit permeation using MNs-pretreated mucosa, due to their insufficient thickness. Read More

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December 2018

Corneal-PAMPA: A novel, non-cell-based assay for prediction of corneal drug permeability.

Eur J Pharm Sci 2018 Dec 13. Epub 2018 Dec 13.

Chemistry Department, Gedeon Richter Plc, Gyömrői út 19-21, 1107 Budapest, Hungary. Electronic address:

The present study was aimed to develop an in vitro non-cell-based method, for the measurement of corneal permeability. To this avail, the parallel artificial membrane permeability assay (PAMPA) was used for studying the effects of composition of the artificial lipid membrane, the DMSO cosolvent content of the donor phase as well as different buffer solutions in the model. Based on experimental corneal permeability values of 25 active pharmaceutical ingredients (APIs), a final model with good predictive ability (R = 0. Read More

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December 2018
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