9,111 results match your criteria Biopharmaceutics & Drug Disposition[Journal]


MPC1 deficiency accelerates lung adenocarcinoma progression through the STAT3 pathway.

Cell Death Dis 2019 Feb 15;10(3):148. Epub 2019 Feb 15.

Institute of Pathology and Southwest Cancer Center, Southwest Hospital, Third Military Medical University (Army Medical University), and Key Laboratory of Tumor Immunopathology, Ministry of Education of China, Chongqing, China.

Mitochondrial pyruvate carrier 1 (MPC1), a key factor that controls pyruvate transportation in the mitochondria, is known to be frequently dysregulated in tumor initiation and progression. However, the clinical relevance and potential molecular mechanisms of MPC1 in lung adenocarcinoma (LAC) progression remain to be illustrated. Herein, MPC1 was lowly expressed in LAC tissues and significantly associated with favorable survival of patients with LAC. Read More

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http://www.nature.com/articles/s41419-019-1324-8
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http://dx.doi.org/10.1038/s41419-019-1324-8DOI Listing
February 2019
1 Read
5.014 Impact Factor

Impact of uncharged and charged stabilizers on in vitro drug performances of clarithromycin nanocrystals.

Eur J Pharm Biopharm 2019 Feb 12. Epub 2019 Feb 12.

Department of Pharmacy, Faculty of Pharmacy, Mahidol University, Sri-Ayutthaya Road, Rajathavee, Bangkok, Thailand; Center of Excellence in Innovative Drug Delivery and Nanomedicine, Faculty of Pharmacy, Mahidol University, Bangkok, Thailand. Electronic address:

The purpose of this study was to evaluate the effect of charge on the in vitro drug performances of clarithromycin nanocrystals. To prepare different charges of nanocrystals, media milling was employed with the use of different stabilizing systems. The uncharged nanocrystals were prepared from poloxamer 407. Read More

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http://dx.doi.org/10.1016/j.ejpb.2019.02.004DOI Listing
February 2019

Simple and efficient genome recombineering using kil counter-selection in Escherichia coli.

J Biotechnol 2019 Feb 12. Epub 2019 Feb 12.

Beijing Institute of Biotechnology, Beijing 100850, China. Electronic address:

Seamless modification of the Escherichia coli genome using positive selection / negative selection is widely used in metabolic engineering and functional genome analysis. Some excellent negative selection systems have been reported, of which tetA-sacB and inducible toxins system are prominent. To expand the existing negative selection toolkit, we constructed a new negative selection marker system based on kil gene of lambda prophage. Read More

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http://dx.doi.org/10.1016/j.jbiotec.2019.01.024DOI Listing
February 2019

Involvement of SAPK/JNK signaling pathway in copper enhanced zinc-induced neuronal cell death.

Toxicol Sci 2019 Feb 15. Epub 2019 Feb 15.

Department of Bio-Analytical Chemistry, Faculty of Pharmacy, Musashino University, 1-1-20 Shinmachi, Nishitokyo-shi, Tokyo, Japan.

Zinc (Zn) plays an important role in many organisms in various physiological functions such as cell division, immune mechanisms and protein synthesis. However, excessive Zn release is induced in pathological situations and causes neuronal cell death. Previously, we reported that copper ions (Cu2+) markedly exacerbates Zn2+-induced neuronal cell death by potentiating oxidative stress and the ER stress response. Read More

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http://dx.doi.org/10.1093/toxsci/kfz043DOI Listing
February 2019

Xanthoceraside prevented synaptic loss and reversed learning-memory deficits in APP/PS1 transgenic mice.

J Physiol Sci 2019 Feb 14. Epub 2019 Feb 14.

Department of Pharmacology, Life Science and Biopharmaceutics School, Shenyang Pharmaceutical University, 103 Wenhua Road, Shenhe District, Shenyang, 110016, Liaoning, People's Republic of China.

Xanthoceraside, a novel triterpenoid saponin, has been found to attenuate learning and memory impairments in AD animal models. However, whether xanthoceraside has a positive effect on synaptic morphology remains unclear. Herein, we evaluated the effects of xanthoceraside on learning and memory impairments and the abnormalities of synaptic structure in APP/PS1 transgenic mice. Read More

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http://dx.doi.org/10.1007/s12576-019-00664-xDOI Listing
February 2019

Dynamic inosinome profiles reveal novel patient stratification and gender-specific differences in glioblastoma.

Genome Biol 2019 Feb 13;20(1):33. Epub 2019 Feb 13.

RNA Editing Lab., Oncohaematology Department, IRCCS Ospedale Pediatrico "Bambino Gesù", Viale San Paolo, 15 00146, Rome, Italy.

Background: Adenosine-to-inosine (A-to-I) RNA editing is an essential post-transcriptional mechanism mediated by ADAR enzymes that have been recently associated with cancer.

Results: Here, we characterize the inosinome signature in normal brain and de novo glioblastoma (GBM) using new metrics that re-stratify GBM patients according to their editing profiles and indicate this post-transcriptional event as a possible molecular mechanism for sexual dimorphism in GBM. We find that over 85% of de novo GBMs carry a deletion involving the genomic locus of ADAR3, which is specifically expressed in the brain. Read More

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https://genomebiology.biomedcentral.com/articles/10.1186/s13
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http://dx.doi.org/10.1186/s13059-019-1647-xDOI Listing
February 2019
4 Reads

Exosomes from endothelial progenitor cells improve outcomes of the lipopolysaccharide-induced acute lung injury.

Crit Care 2019 Feb 13;23(1):44. Epub 2019 Feb 13.

Department of Pathology and Laboratory Medicine, Medical University of South Carolina, 173 Ashley Ave., MSC 908, CRI Room 610, Charleston, SC, 29425, USA.

Background: The acute respiratory distress syndrome (ARDS) is characterized by disruption of the alveolar-capillary barrier resulting in accumulation of proteinaceous edema and increased inflammatory cells in the alveolar space. We previously found that endothelial progenitor cell (EPC) exosomes prevent endothelial dysfunction and lung injury in sepsis in part due to their encapsulation of miRNA-126. However, the effects of EPC exosomes in acute lung injury (ALI) remain unknown. Read More

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http://dx.doi.org/10.1186/s13054-019-2339-3DOI Listing
February 2019

Three new diterpenes and two new sesquiterpenoids from the endophytic fungus Trichoderma koningiopsis A729.

Bioorg Chem 2019 Feb 5;86:368-374. Epub 2019 Feb 5.

State Key Laboratory of Applied Microbiology Southern China, Guangdong Provincial Key Laboratory of Microbial Culture Collection and Application, Guangdong Open Laboratory of Applied Microbiology, Guangdong Institute of Microbiology, Guangzhou 510070, China. Electronic address:

Three new diterpenes koninginols A-C (1-3) and two new sesquiterpenoids 11-hydroxy-15-drimeneoic acid (4), koninginol D (5), together with twelve known compounds (6-17) were isolated from the endophytic fungus Trichoderma koningiopsis A729 derived from Morinda officinalis. Their structures were fully assigned with the aid of extensive spectroscopic analysis and reported data from the previous literatures. Koninginols A and B were disclosed as intriguing diterpene alkaloids, whereas the koninginol C was disclosed as one of the two examples of harziandione diterpene. Read More

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http://dx.doi.org/10.1016/j.bioorg.2019.02.005DOI Listing
February 2019

Preparation, characterization and in vitro antibacterial property of Ciprofloxacin-loaded nanostructured lipid carrier for treatment of Bacillus subtilis infection.

J Microencapsul 2019 Feb 13:1-30. Epub 2019 Feb 13.

a Drug Delivery and Nanomedicines Research Group , Department of Pharmaceutics ; Faculty of Pharmaceutical Sciences , University of Nigeria , Nsukka 410001 , Enugu State , Nigeria ;

Objective: Study of controlled ciprofloxacin (CIPRO) nanostrustructured lipid carriers of Precirol® ATO 5/Transcutol HP (batch A) and tallow fat/Transcutol HP (batch B).

Method: CIPRO concentrations C, (0.0, 0. Read More

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http://dx.doi.org/10.1080/02652048.2019.1582724DOI Listing
February 2019

Probing a dipeptide-based supramolecular assembly as an efficient camptothecin delivering carrier for cancer therapy: computational simulations and experimental validations.

Nanoscale 2019 Feb 13. Epub 2019 Feb 13.

Wuya College of Innovation, Shenyang Pharmaceutical University, Shenyang, Liaoning 110016, P. R. China.

Short peptide-based supramolecular assemblies have drawn much attention in the field of drug delivery. However, the progress still remains limited owing to the inefficient drug loading capacity of conventional short peptide-based materials. In this study, based on coordinated intramolecular π-π stacking, we customize a dipeptide-based rhein derivative (rhein-diphenylalanine peptide, RDP), which could spontaneously form spherical nanoassemblies for drug delivery. Read More

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http://dx.doi.org/10.1039/c8nr07014hDOI Listing
February 2019

Dissolution and Translational Modeling Strategies Toward Establishing an In Vitro-In Vivo Link-a Workshop Summary Report.

AAPS J 2019 Feb 11;21(2):29. Epub 2019 Feb 11.

Pharmaceutical Sciences, Merck & Co., Inc., 770 Sumneytown Pike, WP75B-210, West Point, Pennsylvania, 19486-0004, USA.

This publication summarizes the proceedings of day 2 of a 3-day workshop on "Dissolution and Translational Modeling Strategies Enabling Patient-Centric Product Development." Patient-centric drug product development from a drug product quality perspective necessitates the establishment of clinically relevant drug product specifications via an in vitro-in vivo link. Modeling and simulation offer a path to establish this link; in this regard, physiologically based modeling has been implemented successfully to support regulatory decision-making and drug product labeling. Read More

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http://dx.doi.org/10.1208/s12248-019-0298-xDOI Listing
February 2019

Characterization and anti-inflammatory effects of sulfated polysaccharide from the red seaweed Gelidium pacificum Okamura.

Int J Biol Macromol 2019 Feb 8;129:377-385. Epub 2019 Feb 8.

Heilongjiang Forest By-product and Speciality Institute, Mudanjiang 157011, China. Electronic address:

In the present study, crude polysaccharides were extracted from Gelidium pacificum Okamura, and further purified to obtain the sulfated polysaccharide with molecular weight of 28,807 Da. Its monosaccharide composition mainly consisted of xylose (7.1%), galactose (59. Read More

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http://dx.doi.org/10.1016/j.ijbiomac.2019.02.043DOI Listing
February 2019

Acute toxicity and genotoxicity evaluations of Nattokinase, a promising agent for cardiovascular diseases prevention.

Regul Toxicol Pharmacol 2019 Feb 8;103:205-209. Epub 2019 Feb 8.

Wuya College of Innovation, Shenyang Pharmaceutical University, Shenyang, Liaoning, 110016, PR China. Electronic address:

Cardiovascular diseases (CVDs) are the leading cause of death in the world; however, current agents for CVDs prevention are still limited. Owing to the serious bleeding risk of Aspirin, FDA recently recommended against it from preventing first heart attacks. Nattokinase (NK), a serine protease possessing many key beneficial effects on cardiovascular system, is being pursued as a promising alternative agent. Read More

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http://dx.doi.org/10.1016/j.yrtph.2019.02.006DOI Listing
February 2019
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RNA editing in plants: A comprehensive survey of bioinformatics tools and databases.

Plant Physiol Biochem 2019 Feb 2;137:53-61. Epub 2019 Feb 2.

IBIOM-CNR, Institute of Biomembranes, Bioenergetics and Molecular Biotechnologies, National Research Council, Italy; Department of Biosciences, Biotechnology and Biopharmaceutics, University of Bari A. Moro, Bari, Italy. Electronic address:

RNA editing is a widespread epitranscriptomic mechanism by which primary RNAs are specifically modified through insertions/deletions or nucleotide substitutions. In plants, RNA editing occurs in organelles (plastids and mitochondria), involves the cytosine to uridine modification (rarely uridine to cytosine) within protein-coding and non-protein-coding regions of RNAs and affects organelle biogenesis, adaptation to environmental changes and signal transduction. High-throughput sequencing technologies have dramatically improved the detection of RNA editing sites at genomic scale. Read More

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http://dx.doi.org/10.1016/j.plaphy.2019.02.001DOI Listing
February 2019

Ophthalmic drug abuse: An observational study from community pharmacies.

Res Social Adm Pharm 2019 Jan 30. Epub 2019 Jan 30.

Public Health Institute, Liverpool John Moore's University, United Kingdom.

Background: There has been a trend in the past five years in Jordan for ophthalmic anticholinergic preparations to be misused or abused. This is done mainly to experience mental altering effects such as mood changes, euphoria or hallucinations. Such products are mostly obtained from community pharmacies without a prescription. Read More

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http://dx.doi.org/10.1016/j.sapharm.2019.01.016DOI Listing
January 2019

Design, synthesis and performance evaluation of mPEG-PR: A novel non-absorbable marker.

Eur J Pharm Sci 2019 Feb 6;131:50-57. Epub 2019 Feb 6.

School of Pharmacy, Shenyang Pharmaceutical University, Shenyang 110016, China. Electronic address:

The aim of the present study was to develop a new marker for correcting water flux in the in situ single-pass intestinal perfusion (SPIP) model. The new marker was designed and synthesized based on the application of both polyethylene glycol-4000 (PEG-4000) and phenol red as non-absorbable markers. The new marker mPEG-PR was obtained by combining phenol red with polyethylene glycol monomethyl ether-4000 (mPEG-4000) and verified by nuclear magnetic resonance (NMR), ultraviolet (UV) spectra, gel permeability chromatograph (GPC) and differential scanning calorimetry (DSC). Read More

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http://dx.doi.org/10.1016/j.ejps.2019.02.009DOI Listing
February 2019

A review of GI conditions critical to oral drug absorption in malnourished children.

Eur J Pharm Biopharm 2019 Feb 5. Epub 2019 Feb 5.

Department of Pharmacy, University of Greifswald, 17489 Greifswald, Germany. Electronic address:

Accurate prediction of oral absorption of drugs relies on biorelevant methodology. Current methods are based on Western healthy adult populations. Malnourished children have many differences in their gastrointestinal anatomy and physiology compared to a healthy Western adult. Read More

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http://dx.doi.org/10.1016/j.ejpb.2019.02.001DOI Listing
February 2019

Preparation and characterization of humanized nanobodies targeting the dimer interface of epidermal growth factor receptor (EGFR).

Protein Expr Purif 2019 Feb 5;157:57-62. Epub 2019 Feb 5.

Guangdong Provincial Key Laboratory for Biotechnology Candidate Drug Research, School of Biosciences and Biopharmaceutics, Guangdong Pharmaceutical University, Guangzhou, 510006, PR China. Electronic address:

Epidermal growth factor receptor (EGFR) is an effective target for the treatment of many epithelial cancers. However, EGFR inhibitors have low clinical response rates and are prone to drug resistance arising from mutations and heterodimerization of EGFR. Therefore, targeting the highly conserved dimer interface of EGFR may be an effective strategy for improving the clinical response of anti-EGFR therapies. Read More

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http://dx.doi.org/10.1016/j.pep.2019.02.003DOI Listing
February 2019

LC-HRMS-Database Screening Metrics for Rapid Prioritization of Samples to Accelerate the Discovery of Structurally New Natural Products.

J Nat Prod 2019 Feb 8. Epub 2019 Feb 8.

Marine Biodiscovery Centre, Department of Chemistry , University of Aberdeen , Aberdeen AB24 3UE , Scotland, U.K.

In order to accelerate the isolation and characterization of structurally new or novel secondary metabolites, it is crucial to develop efficient strategies that prioritize samples with greatest promise early in the workflow so that resources can be utilized in a more efficient and cost-effective manner. We have developed a metrics-based prioritization approach using exact LC-HRMS, which uses data for 24 618 marine natural products held in the PharmaSea database. Each sample was evaluated and allocated a metric score by a software algorithm based on the ratio of new masses over the total (sample novelty), ratio of known masses over the total (chemical novelty), number of peaks above a defined peak area threshold (sample complexity), and peak area (sample diversity). Read More

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http://dx.doi.org/10.1021/acs.jnatprod.8b00575DOI Listing
February 2019

Evaluation of the impact of waterpipe tobacco smoke exposure on the activity and expression of rat hepatic CYP450: a pharmacokinetic study.

Inhal Toxicol 2019 Feb 8:1-8. Epub 2019 Feb 8.

c Department of Medical Laboratory Sciences Faculty of Applied Medical Sciences , Jordan University of Science and Technology , Irbid , Jordan.

Waterpipe smoke contains many toxic constituents that can alter drug pharmacokinetics. This study assessed the effect of waterpipe smoke exposure on the activity and expression of CYP450 enzymes in rats. Animals (n = 10/group) were exposed to either waterpipe smoke or side-stream cigarette smoke for 1 h/day (6 days/week) for 31 days, or fresh air (control). Read More

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https://www.tandfonline.com/doi/full/10.1080/08958378.2019.1
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http://dx.doi.org/10.1080/08958378.2019.1569182DOI Listing
February 2019
2 Reads

Delineation of proapoptotic signaling of anthracene-shelled ML metallacapsules and their synergistic activity with curcumin in cisplatin-sensitive and resistant tumor cell lines.

Invest New Drugs 2019 Feb 8. Epub 2019 Feb 8.

Department of Pharmacology, Pharmacotherapy and Toxicology, Faculty of Pharmacy, Medical University of Sofia, 2 Dunav Street, 1000, Sofia, Bulgaria.

Since the introduction of cisplatin into clinical practice a few decades ago, the topic of metal-based drugs has expanded significantly. Recent examples emphasize on metallosupramolecules as an emerging class of compounds with diverse properties. They can trigger unique cellular events in malignant cells or serve as molecular hosts for various biologically active compounds, including anticancer agents. Read More

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http://link.springer.com/10.1007/s10637-019-00738-y
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http://dx.doi.org/10.1007/s10637-019-00738-yDOI Listing
February 2019
1 Read

18β-glycyrrhetyl-3-O-sulfate would be a causative agent of licorice-induced pseudoaldosteronism.

Sci Rep 2019 Feb 7;9(1):1587. Epub 2019 Feb 7.

Department of Pharmacognosy, Graduate School of Pharmaceutical Sciences, Nagoya City University, 3-1 Tanabe-Dori, Mizuho-ku, Nagoya, Japan.

Licorice-induced pseudoaldosteronism is a common adverse effect in traditional Japanese Kampo medicine, and 3-monoglucuronyl glycyrrhetinic acid (3MGA) was considered as a causative agent of it. Previously, we found 22α-hydroxy-18β-glycyrrhetyl-3-O-sulfate-30-glucuronide (1), one of the metabolites of glycyrrhizin (GL) in the urine of Eisai hyperbilirubinuria rats (EHBRs) treated with glycyrrhetinic acid (GA), and suggested that it is also a possible causative agent of pseudoaldosteronism. The discovery of 1 also suggested that there might be other metabolites of GA as causal candidates. Read More

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http://dx.doi.org/10.1038/s41598-018-38182-2DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6367500PMC
February 2019

Sex-by-formulation interaction in bioequivalence trials with transdermal patches.

Eur J Clin Pharmacol 2019 Feb 6. Epub 2019 Feb 6.

Service on Pharmacokinetics and Generics, Division of Pharmacology and Clinical Evaluation, Department of Human Use Medicines, Spanish Agency for Medicines and Health Care Products (AEMPS), C/ Campezo 1, Edificio 8, Planta 2 A, 28022, Madrid, Spain.

Purpose: The existence of a sex-by-formulation interaction in bioequivalence studies implies that the bioequivalence results (i.e., the test/reference ratio of the pharmacokinetic parameters) obtained in one sex are not similar to those obtained in the other sex. Read More

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http://link.springer.com/10.1007/s00228-019-02632-1
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http://dx.doi.org/10.1007/s00228-019-02632-1DOI Listing
February 2019
2 Reads

Dehydroxymethylepoxyquinomicin suppresses atopic dermatitis-like lesions in a stratum corneum-removed murine model through NF-κB inhibition.

Immunopharmacol Immunotoxicol 2019 Feb 6:1-8. Epub 2019 Feb 6.

a School of Life Science and Biopharmaceutics , Shenyang Pharmaceutical University , Shenyang , China.

Background: Dehydroxymethylepoxyquinomicin (DHMEQ) is a specific and potent inhibitor of nuclear factor-kappa B (NF-κB) and has been shown to possess promising potential as an anti-inflammation including anti-atopic dermatitis (AD)-like skin lesions.

Objective: To further evaluate the activity of DHMEQ in vivo modified AD-like lesion model in BALB/c mice and in vitro AD-like lesion cell model in human keratinocytes.

Materials And Methods: In this study, in vivo modified AD-like lesion model in BALB/c mice was chronically induced by the repetitive and alternative application of 2,4-dinitrochlorobenzene (DNCB) and oxazolone (OX) on ears, and stratum corneum of the ear skin was additionally stripped off with surgical tapes before each challenge with DNCB/OX. Read More

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http://dx.doi.org/10.1080/08923973.2018.1510962DOI Listing
February 2019

Dosage Optimization Based on Population Pharmacokinetic Analysis of Tacrolimus in Chinese Patients with Nephrotic Syndrome.

Pharm Res 2019 Feb 4;36(3):45. Epub 2019 Feb 4.

Department of Pharmacy, Shengjing Hospital of China Medical University, Shenyang, 110004, China.

Purpose: The objective of this study was to merge genetic and non-genetic factors of tacrolimus pharmacokinetics to establish a more stable population pharmacokinetic model for individualized dosage regimen in Chinese nephrotic syndrome patients.

Methods: Nephrotic syndrome patients (>16 years old) treated with tacrolimus were included in the study. The population pharmacokinetic approach was analyzed using NONMEM version 7. Read More

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http://dx.doi.org/10.1007/s11095-019-2579-6DOI Listing
February 2019
1 Read

Impact of drugs on venous thromboembolism risk in surgical patients.

Eur J Clin Pharmacol 2019 Feb 5. Epub 2019 Feb 5.

Faculty of Medicine, University of Ljubljana, Vrazov trg 2, SI-1104, Ljubljana, Slovenia.

Purpose: This review focuses on the most common drugs administered to surgical patients during the perioperative period that affect the risk of venous thromboembolism (VTE).

Results: Among analgesics, the risk of VTE is increased in patients treated with diclofenac, ibuprofen, and rofecoxib, but not naproxen, while metamizole can confer a protective effect. The relationship between sedatives and VTE has not been sufficiently studied. Read More

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http://link.springer.com/10.1007/s00228-019-02636-x
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http://dx.doi.org/10.1007/s00228-019-02636-xDOI Listing
February 2019
4 Reads

Mannan-binding lectin suppresses growth of hepatocellular carcinoma by regulating hepatic stellate cell activation the ERK/COX-2/PGE pathway.

Oncoimmunology 2019 10;8(2):e1527650. Epub 2018 Oct 10.

Department of Immunology, School of Basic Medical Sciences, Southern Medical University, Guangzhou, Guangdong, China.

Mannan binding lectin (MBL), initially known to activate the complement lectin pathway and defend against infection, was recently shown to be potentially involved in the development of several types of cancer; however, its exact role in cancers, especially its effect on tumor microenvironment remain largely unknown. Here, using a murine hepatocellular carcinoma (HCC) model, we showed that MBL was a component of liver microenvironment and MBL-deficient (MBL) mice exhibited an enhanced tumor growth compared with wild-type (WT) mice. This phenomenon was associated with elevation of myeloid derived suppressed cells (MDSCs) in tumor tissue of MBL mice. Read More

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http://dx.doi.org/10.1080/2162402X.2018.1527650DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6343806PMC
October 2018
1 Read

Hepatic and Intrahepatic Targeting of Hydrogen Sulfide Prodrug by Bioconjugation.

Biol Pharm Bull 2019 ;42(2):273-279

Department of Biopharmaceutics, Kyoto Pharmaceutical University.

Hydrogen sulfide (HS) is an endogenous gaseous transmitter known to play an important role in biological functions. For the hepatic and intrahepatic targeting of HS prodrug at the cellular level, we developed two types of sulfo-albumins, in which five sulfide groups (source of HS) were covalently bound to succinylated (Suc) or galactosylated (Gal) bovine serum albumin (BSA). Sulfo-BSA-Suc and polyethylene glycol (PEG)-Sulfo-BSA-Gal, both released HS in the 5 mM glutathione solution, but not in the plasma. Read More

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https://www.jstage.jst.go.jp/article/bpb/42/2/42_b18-00773/_
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http://dx.doi.org/10.1248/bpb.b18-00773DOI Listing
January 2019
1 Read

Handling forces for the use of different inhaler devices.

Int J Pharm 2019 Jan 31. Epub 2019 Jan 31.

Boehringer Ingelheim Pharma GmbH & Co. KG, Ingelheim, Germany. Electronic address:

Age and comorbidities can impact on the success of handling an inhaler. In this pilot study, we assessed finger strength in 62 participants (aged 5-17 years [n = 20], 18-65 years [n = 22] and > 65 years [n = 20]) by using different types of inhalers with integrated sensors (Respimat®, Breezhaler®, Aerolizer®, Genuair®, Diskus®, Ellipta®, HandiHaler®, Turbohaler® and a pressurized metered-dose inhaler [Atrovent®]). Parameters under investigation included the spontaneous and maximum achievable force and torque required to operate devices. Read More

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https://linkinghub.elsevier.com/retrieve/pii/S03785173193009
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http://dx.doi.org/10.1016/j.ijpharm.2019.01.053DOI Listing
January 2019
1 Read
3.650 Impact Factor

Puerariae Lobatae Radix with Chuanxiong Rhizoma for treatment of cerebral ischemic stroke by remodeling gut microbiota to regulate the brain-gut barriers of dietary capsaicin against chronic low-grade inflammation.

J Nutr Biochem 2018 Dec 21;65:101-114. Epub 2018 Dec 21.

School of Pharmaceutical Sciences, Southern Medical University, Guangzhou, China; Guangdong Provincial Key Laboratory of New Drug Screening, Biopharmaceutics, School of Pharmaceutical Sciences, Southern Medical University, Guangzhou 510515, China. Electronic address:

The combination of Puerariae Lobatae Radix (PLR) and Chuanxiong Rhizoma (CXR) is commonly used to treat cerebrovascular diseases. This work aimed to clarify the mechanisms of their action in treating cerebral ischemic stroke from the perspective of gut microecology. The PLR and CXR combination effectively improved the neurological function, reduced the cerebral infarction and relieved the complications of cerebral ischemic stroke, including dyslipidemia, increased blood viscosity and thrombotic risk. Read More

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http://dx.doi.org/10.1016/j.jnutbio.2018.12.004DOI Listing
December 2018
3.794 Impact Factor

Preventative effects of metformin on glucocorticoid-induced osteoporosis in rats.

J Bone Miner Metab 2019 Jan 31. Epub 2019 Jan 31.

Department of Nephrology, The Affiliated Hospital of Inner Mongolia Medical University, Hohhot, 010050, Inner Mongolia, People's Republic of China.

This study evaluated the preventative effects of metformin (Met) on glucocorticoid (GC)-induced osteoporosis in a rat model, compared with alendronate (Aln). Twenty-eight 3-month-old female Sprague-Dawley rats were randomly assigned into four groups: normal control (Ctr), methylprednisolone (MP, 13 mg/kg/day, sc, 5 days per week), MP plus Aln orally (1 mg/kg/day), and MP plus Met orally (200 mg/kg/day). After 9 weeks, serum bone metabolic biochemistry, bone densitometry and histomorphometry were performed. Read More

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http://dx.doi.org/10.1007/s00774-019-00989-yDOI Listing
January 2019
1 Read

Characterization of the GI transit conditions in Beagle dogs with a telemetric motility capsule.

Eur J Pharm Biopharm 2019 Mar 28;136:221-230. Epub 2019 Jan 28.

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

In preclinical research, Beagle dogs are an important model for formulation development and for evaluation of food effects on drug absorption. In this study, the gastrointestinal transit conditions in Beagle dogs were studied with a telemetric motility capsule at different intake conditions. In a cross-over study design, the SmartPill® was given to six Beagle dogs to measure transit times, pH values, pressures and temperatures in the different parts of the canine GI tract. Read More

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http://dx.doi.org/10.1016/j.ejpb.2019.01.026DOI Listing

Broadband dielectric spectroscopy as an experimental alternative to calorimetric determination of the solubility of drugs into polymer matrix: Case of flutamide and various polymeric matrixes.

Eur J Pharm Biopharm 2019 Mar 28;136:231-239. Epub 2019 Jan 28.

Institute of Physics, University of Silesia, ul. 75 Pułku Piechoty 1a, 41-500 Chorzów, Poland; Silesian Center for Education and Interdisciplinary Research, ul. 75 Pułku Piechoty 1a, 41-500 Chorzów, Poland.

In this paper we determined the solubility limits of the amorphous flutamide within the two different polymeric matrixes - poly vinylpyrrolidone and poly vinylacetate. In order to achieve this goal, series of broadband dielectric spectroscopy measurements were performed. As a result we found that the maximal amount of the drug that can be successfully dissolved within the PVAc (maintaining the non-supersaturated conditions) is equal to 35 wt% of the amorphous solid dispersion system. Read More

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http://dx.doi.org/10.1016/j.ejpb.2019.01.025DOI Listing

Photodynamic therapy - hypericin tetraether liposome conjugates and their antitumor and antiangiogenic activity.

Drug Deliv 2019 Dec;26(1):23-33

a Department of Pharmaceutics and Biopharmaceutics , University of Marburg , Marburg , Germany.

Photodynamic therapy (PDT) is an established noninvasive tumor treatment. The hydrophobic natural occurring pigment hypericin shows a lot of attractive properties for the application in PDT. Hence, the administration to biological systems or patients requires the formulation in drug carriers enabling sufficient bioavailability. Read More

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http://dx.doi.org/10.1080/10717544.2018.1531954DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6352941PMC
December 2019

Response to 'Sex-by-formulation interaction in bioequivalence studies: the importance of formulations and experimental conditions' by Ibarra et al.

Br J Clin Pharmacol 2019 Jan 28. Epub 2019 Jan 28.

Service on Pharmacokinetics and Generics, Division of Pharmacology and Clinical Evaluation, Department of Human Use Medicines, Spanish Agency for Medicines and Health Care Products, Madrid, Spain.

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http://dx.doi.org/10.1111/bcp.13860DOI Listing
January 2019
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The nuclear receptor Shp regulates morphine withdrawal syndrome via modulation of Ugt2b expression in mice.

Biochem Pharmacol 2019 Mar 25;161:163-172. Epub 2019 Jan 25.

Research Center for Biopharmaceutics and Pharmacokinetics, College of Pharmacy, Jinan University, 601 Huangpu Avenue West, Guangzhou, China. Electronic address:

In this study, we aimed to investigate a potential role of small heterodimer partner (Shp, a nuclear receptor) in regulation of morphine withdrawal syndrome and to determine the mechanisms thereof. Somatic opiate withdrawal and pharmacokinetic experiments were performed with wild-type (WT) and Shp knockout (Shp-KO) mice. Regulatory effects of Shp on Ugt2b expression were assessed in vitro (using mouse hepatoma Hepa1-6 cells) and in vivo (using Shp-KO mice). Read More

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https://linkinghub.elsevier.com/retrieve/pii/S00062952193002
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http://dx.doi.org/10.1016/j.bcp.2019.01.019DOI Listing
March 2019
3 Reads

Hyperhydration effect on pharmacokinetic parameters and detection sensitivity of recombinant human erythropoietin in urine and serum doping control analysis of males.

J Pharm Sci 2019 Jan 23. Epub 2019 Jan 23.

Anti-Doping Lab Qatar, Sports City Road, Sports City, P.O. Box 27775, Doha, Qatar. Electronic address:

Excessive fluid intake, i.e., hyperhydration may be adopted by athletes as a masking method during anti-doping sample collection to influence the excretion patterns of doping agents and, therefore, manipulate their detection. Read More

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http://dx.doi.org/10.1016/j.xphs.2019.01.017DOI Listing
January 2019
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Folate pathway genetic polymorphisms modulate methotrexate-induced toxicity in childhood acute lymphoblastic leukemia.

Cancer Chemother Pharmacol 2019 Jan 25. Epub 2019 Jan 25.

Department of Biopharmaceutics and Clinical Pharmacy, School of Pharmacy, The University of Jordan, Queen Rania Street, Amman, 11942, Jordan.

Background: Acute lymphoblastic leukemia (ALL) is one of the major malignancies affecting children in Jordan. Methotrexate (MTX) is the cornerstone of chemotherapy for ALL, and works by targeting enzymes involved in the folate pathway. We hypothesize that genetic polymorphisms of the folate pathway are associated with MTX toxicity in children with ALL. Read More

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http://dx.doi.org/10.1007/s00280-019-03776-8DOI Listing
January 2019
3 Reads

Characterization and biological effects of Hypericum extracts on experimentally-induced - anxiety, oxidative stress and inflammation in rats.

J Physiol Pharmacol 2018 Oct 21;69(5). Epub 2019 Jan 21.

Department of Physiology, "Iuliu Hatieganu" University of Medicine and Pharmacy, Cluj-Napoca, Romania.

Anxiety disorders can associate with oxidative stress and immune system alterations. Our study aimed to chemically analyze Hypericum maculatum (HM) and Hypericum perforatum (HP) dry extracts and to evaluate their effects along with quercetin (Q), on brain oxidative stress biomarkers: malondialdehyde (MDA), catalase (CAT) and superoxide dismutase (SOD), inflammatory cytokines: interleukin-1α, (IL-1α), IL-1β, regulated on activation normal T cell expressed and secreted (RANTES), interferon (IFN), monocyte chemoattractant protein-1 (MCP1), macrophage inflammatory protein (MIP) and serum corticosterone levels. Nuclear transcription factor κB (NFκB) signaling pathway in the hippocampus and frontal lobe in rats with N-methyl-9H-pyrido[5,4-b]indole-3-carboxamide (FG-7142) experimental-induced anxiety were also investigated. Read More

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http://dx.doi.org/10.26402/jpp.2018.5.13DOI Listing
October 2018

Oral probiotic administration during pregnancy prevents autism-related behaviors in offspring induced by maternal immune activation via anti-inflammation in mice.

Autism Res 2019 Jan 25. Epub 2019 Jan 25.

Department of Anatomy and Neurobiology, Zhongshan School of Medicine, Sun Yat-sen University, Guangzhou, Guangdong, P. R. China.

Maternal immune activation (MIA) is associated with an increased risk for autism spectrum disorders (ASD) in offspring. Animal experiments have found that interleukin 6 (IL-6) and IL-17a are key cytokines in the induction of ASD by MIA. Moreover, probiotics were verified to inhibit the production of proinflammatory cytokines. Read More

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http://doi.wiley.com/10.1002/aur.2079
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http://dx.doi.org/10.1002/aur.2079DOI Listing
January 2019
3 Reads

Molecular structure and function of myelin protein P0 in membrane stacking.

Sci Rep 2019 Jan 24;9(1):642. Epub 2019 Jan 24.

Department of Biomedicine, University of Bergen, Bergen, Norway.

Compact myelin forms the basis of nerve insulation essential for higher vertebrates. Dozens of myelin membrane bilayers undergo tight stacking, and in the peripheral nervous system, this is partially enabled by myelin protein zero (P0). Consisting of an immunoglobulin (Ig)-like extracellular domain, a single transmembrane helix, and a cytoplasmic extension (P0ct), P0 harbours an important task in ensuring the integrity of compact myelin in the extracellular compartment, referred to as the intraperiod line. Read More

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http://www.nature.com/articles/s41598-018-37009-4
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http://dx.doi.org/10.1038/s41598-018-37009-4DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6345808PMC
January 2019
3 Reads

Sortagged anti-EGFR immunoliposomes exhibit increased cytotoxicity on target cells.

Eur J Pharm Biopharm 2019 Mar 21;136:203-212. Epub 2019 Jan 21.

Department of Pharmaceutics and Biopharmaceutics, Kiel University, Grasweg 9a, 24118 Kiel, Germany.

Purpose: Conventional chemotherapy is associated with therapy-limiting side effects, which might be alleviated by targeted chemotherapeutics such as immunoliposomes. The targeting ligands of immunoliposomes are commonly attached by unspecific chemical conjugation, bearing risk of structural heterogeneity and therewith related biological consequences. Chemoenzymatic methods may mitigate such risks through site-specific conjugation. Read More

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https://linkinghub.elsevier.com/retrieve/pii/S09396411183139
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http://dx.doi.org/10.1016/j.ejpb.2019.01.020DOI Listing
March 2019
6 Reads

Orthogonal redundant monitoring of a new continuous fluid-bed dryer for pharmaceutical processing by means of mass and energy balance calculations and spectroscopic techniques.

J Pharm Sci 2019 Jan 21. Epub 2019 Jan 21.

Novartis AG, 4002 Basel, Switzerland. Electronic address:

In line with the ongoing shift from batch- to continuous pharmaceutical production of solid oral dosage forms, a novel continuous fluid-bed dryer was developed. The forced-feed nature of the Glatt GPCG2 CM fluid-bed dryer allows continuous, first-in-first-out drying of wet granulate materials based on its compartmentalized, rotating fluidizing chamber. The presented work aims to introduce the dryer's functionalities in detail, and to demonstrate that the rotating fluid-bed chambers facilitates a stable drying behavior, which ensures robust and repeatable residual moisture contents (loss-on-drying; LOD) of the discharged granules. Read More

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http://dx.doi.org/10.1016/j.xphs.2018.12.028DOI Listing
January 2019
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The Role of the Middle East in ZIKA Virus Circulation: Implications of a Cross-Sectional Study in Jordan.

Am J Trop Med Hyg 2019 Jan 21. Epub 2019 Jan 21.

Department of Biopharmaceutics and Clinical Pharmacy, School of Pharmacy, The University of Jordan, Amman, Jordan.

ZIKA virus (ZIKAV) outbreak in Latin America was associated with international concerns of ZIKAV circulation. The lack of vaccine and FDA-approved drugs against this virus rendered prevention as the single most effective method to control its spread. Hence, this study aimed to assess Jordanian population knowledge, attitude, and practices toward ZIKAV and its prevention. Read More

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http://dx.doi.org/10.4269/ajtmh.18-0715DOI Listing
January 2019
2 Reads
2.699 Impact Factor

LOCAL PULMONARY DRUG DELIVERY IN THE PRETERM RABBIT: FEASIBILITY AND EFFICACY OF DAILY INTRATRACHEAL INJECTIONS.

Am J Physiol Lung Cell Mol Physiol 2019 Jan 24. Epub 2019 Jan 24.

Development and Regeneration, KU Leuven.

Recent clinical trials in newborns have successfully used surfactant as a drug carrier for an active compound, in order to minimize systemic exposure. To investigate the translational potential of surfactant-compound mixtures and other local therapeutics, a relevant animal model is required where intratracheal (IT) administration for maximal local deposition is technically possible and well tolerated. Preterm rabbit pups (born at 28 days of gestation) were exposed to either hyperoxia or normoxia and randomized to receive daily IT surfactant, daily IT saline or no injections for 7 days. Read More

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http://dx.doi.org/10.1152/ajplung.00255.2018DOI Listing
January 2019
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PBPK Absorption Modeling: Establishing the In Vitro-In Vivo Link-Industry Perspective.

AAPS J 2019 Jan 23;21(2):19. Epub 2019 Jan 23.

Biopharmaceutics and Specialty Dosage Forms, Pharmaceutical Sciences, Merck & Co., Inc., 770 Sumneytown Pike, WP75B-210, West Point, Pennsylvania, 19486-0004, USA.

The establishment of an in vitro-in vivo correlation (IVIVC) is considered the gold standard to establish in vivo relevance of a dissolution method and to utilize dissolution data in the context of regulatory bioequivalence questions, including the development of dissolution specifications. However, several recent publications, including industry surveys and reviews from regulatory agencies, have indicated a low success rate for IVIVCs, especially for immediate-release formulations. In recent years, the use of physiologically based pharmacokinetics (PBPK) and absorption modeling, as a tool to facilitate formulation development, has been attracting increased attention. Read More

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http://dx.doi.org/10.1208/s12248-019-0292-3DOI Listing
January 2019
3 Reads

Dynamic changes of MMP-9 plasma levels correlate with JCV reactivation and immune activation in natalizumab-treated multiple sclerosis patients.

Sci Rep 2019 Jan 22;9(1):311. Epub 2019 Jan 22.

Department of Public Health and Infectious Diseases, Sapienza University, Rome, Italy.

The aim of the study was to investigate the changes of matrix metalloproteinase (MMP)-2 and MMP-9 plasma levels during natalizumab treatment and their correlation with JC virus (JCV) reactivation and T-lymphocyte phenotypic modifications in peripheral blood samples from 34 relapsing-remitting multiple sclerosis (RRMS) patients. MMP-9 levels were assessed by zymography in plasma samples. JCV-DNA was detected through quantitative real time PCR in plasma samples. Read More

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http://dx.doi.org/10.1038/s41598-018-36535-5DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6342994PMC
January 2019

Identification of the metabolic fingerprints in women with polycystic ovary syndrome using the multiplatform metabolomics technique.

J Steroid Biochem Mol Biol 2019 Feb 27;186:176-184. Epub 2018 Oct 27.

Department of Biopharmaceutics and Pharmacodynamics, Medical University of Gdańsk, Hallera 107, 80-416 Gdańsk, Poland. Electronic address:

In addition to chronic anovulation and clinical signs of hyperandrogenism women with polycystic ovary syndrome (PCOS) are insulin resistant and therefore, develop central obesity with its long term consequences such as dyslipidaemia, hypertension, atherosclerosis and type 2 diabetes mellitus (T2DM), which all lead to the development of cardiovascular disease (CVD). Due to the polysymptomatic nature of this syndrome and lack of consensus on its diagnostic criteria there is a strong need of finding a reliable biochemical or molecular marker, which would facilitate making the accurate diagnosis of PCOS. Therefore, the aim of our study was to perform a metabolomics analysis with the use of two complementary techniques: gas chromatography and liquid chromatography coupled with mass spectrometry, of the serum samples from women with PCOS (n = 30) and to compare them with healthy age and BMI matched controls (n = 30). Read More

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https://linkinghub.elsevier.com/retrieve/pii/S09600760183031
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http://dx.doi.org/10.1016/j.jsbmb.2018.10.012DOI Listing
February 2019
3 Reads

Stability Assessment of Topical Amitriptyline Extemporaneously Compounded with Lipoderm Base, PLO Gel Mediflo 30, and Emollient Cream.

Int J Pharm Compd 2019 Jan-Feb;23(1):82-87

Biopharmaceutics and Drug Delivery Lab, College of Pharmacy, Dalhousie University, Halifax, Nova Scotia, Canada.

Extemporaneous topical compounds for neuropathic pain offers an alternative or adjunct approach to existing therapies for patients. Assigning evidence-based beyond-use dating prior to dispensing topical medications is a legal requirement by pharmacy governing bodies. The purpose of this study was to utilize a validated stability-indicating high-performance liquid chromatography assay to determine beyond-use dating of topical amitriptyline in three different bases (Lipoderm Base, PLO Gel Mediflo 30, Emollient Cream) at three different temperatures [room temperature (25°C), refrigeration (4°C), and high temperature (40°C)]. Read More

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January 2019

Test models for the evaluation of immunogenicity of protein aggregates.

Int J Pharm 2019 Jan 18;559:192-200. Epub 2019 Jan 18.

Department of Pharmacy, Pharmaceutical Technology & Biopharmaceutics, Ludwig-Maximilians-Universität München, Butenandtstr. 5, D-81377 Munich, Germany.

Protein aggregates have been discussed for a long time as a potential risk factor for immunogenicity in patients. Meanwhile, many research groups have investigated the immunogenicity of differently produced aggregates using in vitro or in vivo models. Despite all knowledge gained in these studies still little is known about the mechanisms of immunogenicity and the kind of protein aggregates bearing the greatest risk for immunogenicity. Read More

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http://dx.doi.org/10.1016/j.ijpharm.2019.01.015DOI Listing
January 2019
1 Read