9,849 results match your criteria BioPharm International[Journal]


Insight into Imiquimod Skin Permeation and Increased Delivery Using Microneedle Pre-treatment.

Eur J Pharm Biopharm 2019 Feb 13. Epub 2019 Feb 13.

Division of Advanced Materials and Healthcare Technologies, School of Pharmacy, The University of Nottingham, NG7 2RD, UK. Electronic address:

Basal cell carcinoma (BCC) is the most common skin cancer in humans. Topical treatment with imiquimod provides a non-invasive, self-administered treatment with relatively low treatment cost. Despite displaying excellent efficacy, imiquimod is only licensed by the FDA for superficial BCC. Read More

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http://dx.doi.org/10.1016/j.ejpb.2019.02.006DOI Listing
February 2019

Molecular simulation as a computational pharmaceutics tool to predict drug solubility, solubilization processes and partitioning.

Eur J Pharm Biopharm 2019 Feb 13. Epub 2019 Feb 13.

Department of Pharmacy, Uppsala Biomedical Center, Uppsala University, 751 23 Uppsala, Sweden; Swedish Drug Delivery Forum (SDDF), Uppsala University, Sweden. Electronic address:

In this review we will discuss how computational methods, and in particular classical molecular dynamics simulations, can be used to calculate solubility of pharmaceutically relevant molecules and systems. To the extent possible, we focus on the non-technical details of these calculations, and try to show also the added value of a more thorough and detailed understanding of the solubilization process obtained by using computational simulations. Although the main focus is on classical molecular dynamics simulations, we also provide the reader with some insights into other computational techniques, such as the COSMO-method, and also discuss Flory-Huggins theory and solubility parameters. Read More

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http://dx.doi.org/10.1016/j.ejpb.2019.02.007DOI Listing
February 2019

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

Simulation optimization for Bayesian multi-arm multi-stage clinical trial with binary endpoints.

J Biopharm Stat 2019 Feb 14:1-12. Epub 2019 Feb 14.

c Data Coordination Unit, Department of Public Health Sciences , Medical University of South Carolina , Charleston , SC , USA.

Multi-arm multi-stage designs, in which multiple active treatments are compared to a control and accumulated information from interim data are used to add or remove arms from the trial, may reduce development costs and shorten the drug development timeline. As such, this adaptive update is a natural complement to Bayesian methodology in which the prior clinical belief is sequentially updated using the observed probability of success. Simulation is often required for planning clinical trials to accommodate the complexity of the design and to optimize key design characteristics. Read More

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http://dx.doi.org/10.1080/10543406.2019.1577682DOI Listing
February 2019

Adaptation of the robust method to large distributions of reference values: program modifications and comparison of alternative computational methods.

J Biopharm Stat 2019 Feb 13:1-13. Epub 2019 Feb 13.

d Division of Neurology , Cincinnati Children's Hospital Medical Center , Cincinnati , OH , USA.

The objective of this research was to compute reference limits using reference values from patients entering pharmaceutical development clinical trials by the nonparametric method and the robust method of Horn and Pesce, with and without outlier exclusion, and compare the methods with respect to influence on the limits. Reference limits were computed for 38 analytes with over 130,000 subjects contributing reference values. Subjects were partitioned into 10 demographic strata for limit computation. Read More

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http://dx.doi.org/10.1080/10543406.2019.1579223DOI Listing
February 2019

Tag-on-Demand: exploiting amber codon suppression technology for the enrichment of high-expressing membrane protein cell lines.

Protein Eng Des Sel 2019 Feb 12. Epub 2019 Feb 12.

Antibody Discovery and Protein Engineering, MedImmune, Gaithersburg, MD, USA.

Membrane proteins play key roles in the evolution of numerous diseases and as a result have become the most dominant class of targets for therapeutic intervention. However, their poor expression and detection oftentimes prohibit drug discovery and screening efforts. Herein, we have developed an approach, named 'Tag-on-Demand' that exploits amber suppression to control the expression of 'tagged' membrane proteins for detection and selections, yet can be turned off for expression of the protein in its native form. Read More

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http://dx.doi.org/10.1093/protein/gzy032DOI Listing
February 2019

Semi-parametric Bayesian regression for subgroup analysis in clinical trials.

J Biopharm Stat 2019 Feb 12:1-19. Epub 2019 Feb 12.

b Division of Biostatistics , Center for Devices and Radiologic Health, Food and Drug Administration , Silver Spring , Maryland , USA.

Determining whether there are differential treatment effects in subgroups of trial participants remains an important topic in clinical trials as precision medicine becomes ever more relevant. Any assessment of differential treatment effect is predicated on being able to estimate the treatment response accurately while satisfying constraints of balancing the risk of overlooking an important subgroup with the potential to make a decision based on a false discovery. While regression models, such as marginal interaction model, have been widely used to improve accuracy of subgroup parameter estimates by leveraging the relationship between treatment and covariate, there is still a possibility that it can lead to excessively conservative or anti-conservative results. Read More

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http://dx.doi.org/10.1080/10543406.2019.1572613DOI Listing
February 2019
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R-TPI: rolling toxicity probability interval design to shorten the duration and maintain safety of phase I trials.

J Biopharm Stat 2019 Feb 11:1-14. Epub 2019 Feb 11.

c Biostatistics Department , Juno Therapeutics , Seattle , Washington , USA.

To shorten trial duration and improve safety of Phase I trials, we propose R-TPI, a rolling enrollment design that combines the features in model-based designs such as mTPI-2 and rule-based designs such as rolling six. R-TPI employs a novel rolling enrollment scheme, which allows concurrent patient enrollment that is faster than cohort-based enrollment. Bench-marking against rolling six, we find that the R-TPI design is as fast in completing clinical trials but with fewer toxicity events and higher chance of finding the maximum tolerated dose (MTD) in the single scenario laid out in the 2008 rolling six publication. Read More

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http://dx.doi.org/10.1080/10543406.2019.1577683DOI Listing
February 2019
0.716 Impact Factor

Approaches for testing noninferiority in two-arm trials for risk ratio and odds ratio.

J Biopharm Stat 2019 Feb 11:1-21. Epub 2019 Feb 11.

a Center of Molecular Medicine and Genetics , Wayne State University , Detroit , MI , USA.

For an existing established drug regimen, active control trials are defacto standard due to ethical reason as well as for clinical equipoise. However, when superiority claim of a new drug against the active control is unlikely to be successful, researchers often address the issue in terms of noninferiority (NI), provided the experimental drug demonstrates the evidence of other benefits beyond efficacy. Such trials aim to demonstrate that an experimental treatment is non-inferior to an existing comparator by not more than a pre-specified margin. Read More

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http://dx.doi.org/10.1080/10543406.2019.1572616DOI Listing
February 2019

Investigating the bioavailabilities of olerciamide A via the rat's hepatic, gastric and intestinal first-pass effect models.

Biopharm Drug Dispos 2019 Feb 10. Epub 2019 Feb 10.

School of the First Clinic, Liaoning University of Traditional Chinese Medicine, 110032, Shenyang, China.

Olerciamide A (OA), as a new alkaloid isolated from Portulaca oleracea L., has been proved to possess a low bioavailability (F) after oral administration in rats in our previous study. Hence, to clarify the reasons of its low bioavailability, the hepatic, gastric and intestinal first-pass effect models were established, and a rapid, sensitive UHPLC method were validated and applied for the determination after dosed via femoral, portal, gastric and intestinal routes. Read More

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http://dx.doi.org/10.1002/bdd.2175DOI Listing
February 2019

Ultrasound-responsive nanobubble-mediated gene transfection in the cerebroventricular region by intracerebroventricular administration in mice.

Eur J Pharm Biopharm 2019 Feb 7. Epub 2019 Feb 7.

Graduate School of Biomedical Sciences, Nagasaki University, 1-7-1 Sakamoto, Nagasaki-shi, Nagasaki 852-8588, Japan,. Electronic address:

Aim: Intracerebroventricular (ICV) administration of ultrasound-responsive bubbles and cranial ultrasound irradiation is reported as a transfection system for the cerebroventricular region. This study aimed to characterize the transfection system with respect to transfection efficiency, spatial distribution of transgene expression, and safety.

Methods: Plasmid DNA was transfected to mouse brain by ICV injection of ultrasound-responsive nanobubbles, followed by ultrasound irradiation to brain. Read More

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https://linkinghub.elsevier.com/retrieve/pii/S09396411183141
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http://dx.doi.org/10.1016/j.ejpb.2019.02.003DOI Listing
February 2019
2 Reads

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

ImmunoPET imaging to assess target engagement: Experience from Zr-anti-HER3 mAb (GSK2849330) in patients with solid tumors.

J Nucl Med 2019 Feb 7. Epub 2019 Feb 7.

Hengrui Therapeutics, Inc., United States.

Positron-emission tomography (PET) imaging with radiolabeled drug provides information on tumor uptake and dose-dependent target interaction to support selection of an optimal dose for future efficacy testing. In this immunoPET study of the anti- human epidermal growth factor receptor (HER3) mAb GSK2849330, we investigated the biodistribution and tumor uptake of 89-Zirconium (Zr)-labeled GSK2849330 and evaluated target engagement as a function of antibody mass dose. Zr-GSK2849330 distribution was monitored in 6 patients with HER3-positive tumors not amenable to standard treatment. Read More

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http://dx.doi.org/10.2967/jnumed.118.214726DOI Listing
February 2019

Vaccination with influenza hemagglutinin-loaded ceramic nanoporous microneedle arrays induces protective immune responses.

Eur J Pharm Biopharm 2019 Mar 5;136:259-266. Epub 2019 Feb 5.

MyLife Technologies B.V., Leiden Bio Science Park, BioPartner 4, Unit 4358, Robert Boyleweg 4, 2333 CG Leiden, the Netherlands; Division of BioTherapeutics, Leiden Academic Centre for Drug Research (LACDR), Leiden University, 2300 RA Leiden, the Netherlands. Electronic address:

Microneedle arrays (MNAs) are a promising mean to administer vaccines. Without the need of highly trained personnel, MNAs can be applied to deliver vaccines into the dermis, which is well equipped to initiate potent immune responses. While vaccination using dissolving microneedle arrays has been extensively investigated, the use of solid nanoporous MNAs (npMNAs) to deliver vaccines remained largely unexplored. Read More

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http://dx.doi.org/10.1016/j.ejpb.2019.02.002DOI Listing
March 2019
1 Read

Screening of ten cytochrome P450 enzyme activities with 12 probe substrates in human liver microsomes using cocktail incubation and liquid chromatography-tandem mass spectrometry.

Biopharm Drug Dispos 2019 Feb 7. Epub 2019 Feb 7.

College of Pharmacy and Research Institute of Pharmaceutical Sciences, Kyungpook National University, Daegu, 41566, South Korea.

Testing for the potential drug interactions of new chemical entities is essential when developing a novel drug. In this study, we designed an assay to evaluate drug interactions with 10 major human cytochrome P450 (P450) enzymes incubated in liver microsomes, involving 12 probe substrates with two cocktail incubation sets used in a single liquid chromatography-tandem mass spectrometry (LC-MS/MS) run. The P450 substrate composition in each cocktail set was optimized to minimize solvent effects and mutual drug interactions among substrates as follows: cocktail A was composed of phenacetin for CYP1A2, bupropion for CYP2B6, amodiaquine for CYP2C8, diclofenac for CYP2C9, S-mephenytoin for CYP2C19, and dextromethorphan for CYP2D6; cocktail B was composed of coumarin for CYP2A6, chlorzoxazone for CYP2E1, astemizole for CYP2J2, and midazolam, nifedipine, and testosterone for CYP3A. Read More

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http://dx.doi.org/10.1002/bdd.2174DOI Listing
February 2019

A comparative study for detecting CYP3A induction by CYP3A probe drugs and endogenous markers in cynomolgus monkeys.

Biopharm Drug Dispos 2019 Feb 6. Epub 2019 Feb 6.

Translational Research Unit, Kyowa Hakko Kirin Co., Ltd., 1188 Shimotogari, Nagaizumi-cho, Sunto-gun, Shizuoka, 411-8731, Japan.

CYP3A probe drugs such as midazolam and endogenous markers, and plasma 4β-hydroxycholesterol (4β-OHC) and urinary 6β-hydroxycortisol-to-cortisol ratios (6β-OHC/C) have been used as markers of CYP3A induction in cynomolgus monkeys, as with humans. However, there is limited information on their sensitivity and ability to detect CYP3A induction, as most studies were evaluated only at a high dose of the inducer, rifampicin (RIF; 20 mg/kg). In the present study, the CYP3A induction by RIF over a range doses of 0. Read More

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https://onlinelibrary.wiley.com/doi/abs/10.1002/bdd.2173
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http://dx.doi.org/10.1002/bdd.2173DOI Listing
February 2019
1 Read

A fast and reliable test for parallelism in bioassay.

J Biopharm Stat 2019 Feb 4:1-13. Epub 2019 Feb 4.

a Department of Statistical Sciences , MedImmune LLC , Gaithersburg , Maryland , USA.

Parallelism in bioassay is a synonym of similarity between two concentration-response curves. Before the determination of relative potency in bioassays, it is necessary to test for and claim parallelism between the pair of concentration-response curves of reference standard and test sample. Methods for parallelism testing include p-value-based significance tests and interval-based equivalence tests. Read More

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http://dx.doi.org/10.1080/10543406.2019.1572615DOI Listing
February 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

Thermostable Ebola virus vaccine formulations lyophilized in the presence of aluminum hydroxide.

Eur J Pharm Biopharm 2019 Mar 28;136:213-220. Epub 2019 Jan 28.

Department of Chemical and Biological Engineering, Center for Pharmaceutical Biotechnology, University of Colorado, Boulder, CO 80309, United States. Electronic address:

No United States Food and Drug Administration-licensed vaccines protective against Ebola virus (EBOV) infections are currently available. EBOV vaccine candidates currently in development, as well as most currently licensed vaccines in general, require transport and storage under a continuous cold chain in order to prevent potential decreases in product efficacy. Cold chain requirements are particularly difficult to maintain in developing countries. Read More

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http://dx.doi.org/10.1016/j.ejpb.2019.01.019DOI Listing

Combinatorial Efficacy of Quercitin and Nanoliposomal Ceramide for Acute Myeloid Leukemia.

Int J Biopharm Sci 2018 31;1(1). Epub 2018 Jan 31.

Department of Medicine, Division of Hematology and Oncology, Penn State Hershey Cancer Institute, Penn State College of Medicine, Hershey, PA 17033 USA.

Acute myeloid leukemia (AML) is an aggressive hematological malignancy with limited treatment options. Inflammation is often a contributing factor to the development and progression of AML, and related diseases, and can potentiate therapy failure. Previously, we had identified anti-inflammatory roles and anti-AML efficacy for blueberry extracts. Read More

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http://dx.doi.org/10.31021/ijbs.20181106DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6349237PMC
January 2018

TGF-β1 elevates P-gp and BCRP in hepatocellular carcinoma through HOTAIR/miR-145 axis.

Biopharm Drug Dispos 2019 Jan 30. Epub 2019 Jan 30.

Center for Drug Metabolism and Pharmacokinetics, and Department of Pharmacology, College of Pharmaceutical Sciences, Soochow University, Suzhou, 215123, China.

Multidrug resistance (MDR) is common in patients and has been linked to transforming growth factor-β1 (TGF-β1) and overexpression of drug efflux transporters P-glycoprotein (P-gp) and breast cancer resistance protein (BCRP), although molecular mechanisms remain largely unknown. Here, we aimed to investigate the mechanisms underlying TGF-β1-induced MDR in hepatocellular carcinoma (HCC) cells. We found that TGF-β1 upregulated HOX transcript antisense RNA (HOTAIR) expression in HCC cells. Read More

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http://dx.doi.org/10.1002/bdd.2172DOI Listing
January 2019
2.178 Impact Factor

Letter to the editor.

J Biopharm Stat 2019 Jan 29:1-2. Epub 2019 Jan 29.

a Institute of Cellular Medicine , Newcastle University , Newcastle upon Tyne , UK.

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http://dx.doi.org/10.1080/10543406.2019.1572618DOI Listing
January 2019

A drug refillable device for transscleral sustained drug delivery to the retina.

Eur J Pharm Biopharm 2019 Mar 25;136:184-191. Epub 2019 Jan 25.

Division of Clinical Cell Therapy, United Centers for Advanced Research and Translational Medicine (ART), Tohoku University Graduate School of Medicine, 2-1 Seiryo-machi, Aoba-ku, Sendai 980-8575, Japan. Electronic address:

Continuous drug administration with better adherence to treatment and less invasive procedures is important in treating retinal diseases such as age-related macular disease. In this study, we report a drug-refillable device consisting of a silicone reservoir and an injectable gelatin/chitosan gel (iGel). The silicone reservoir was fabricated with polydimethylsiloxane (PDMS) using a computer-aided design and manufacturing to have micropores at a releasing side for uniaxial release to the sclera. Read More

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http://dx.doi.org/10.1016/j.ejpb.2019.01.024DOI Listing

QobuR - A new in vitro human corneal epithelial model for preclinical drug screening.

Eur J Pharm Biopharm 2019 Mar 25;136:164-173. Epub 2019 Jan 25.

Instituto Universitario Fernández-Vega, Fundación de Investigación Oftalmológica, Universidad de Oviedo, Oviedo, Spain; Centro Comunitario de Sangre y Tejidos de Asturias, Centro de Investigación Biomédica en Red de Enfermedades Raras (CIBERER U714), Oviedo, Spain.

A new in vitro human corneal epithelial model (QobuR) obtained from normal limbal tissue has been developed to study ocular irritancy of different ophthalmic compounded drugs. Phenotypical characterization and trans-epithelial electrical resistance (TEER) of QobuR revealed essential similarities compared with a native human cornea, displaying functional markers and TEER values near 1500 Ωcm at day 7th of cellular differentiation. Using this model, ocular irritancy and barrier integrity alterations were evaluated using MTT reaction and variations in TEER. Read More

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https://linkinghub.elsevier.com/retrieve/pii/S09396411183120
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http://dx.doi.org/10.1016/j.ejpb.2019.01.023DOI Listing
March 2019
2 Reads

Prevention of mother-to-child transmission of hepatitis B virus in Burkina Faso: Screening, vaccination and evaluation of post-vaccination antibodies against hepatitis B surface antigen in newborns.

J Public Health Afr 2018 Dec 21;9(3):816. Epub 2018 Dec 21.

Department of Biology, Tor Vergata University of Rome, Italy.

The low rate of screening for hepatitis B virus (HBV) in pregnant women is a highrisk factor for its vertical transmission. The objectives of this study were: i) to screen pregnant women for HBV infection; ii) vaccinate all children from birth against HBV regardless their mother HBV status; and iii) evaluate after 7 months of birth the level of their AbHBs among babies who received HBV vaccine at birth. Serological markers of HBV (HBsAg, HBeAg, AbHBs, AbHBe, and AbHBc) were determined on venous blood samples from 237 pregnant women and their children using the Abon Biopharm Kit. Read More

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https://www.publichealthinafrica.org/index.php/jphia/article
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http://dx.doi.org/10.4081/jphia.2018.816DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6326159PMC
December 2018
2 Reads

A reflection on the possibility of finding a good surrogate.

J Biopharm Stat 2019 Jan 26:1-10. Epub 2019 Jan 26.

a I-BioStat , KU Leuven , Leuven , Belgium.

Surrogate endpoints need to be statistically evaluated before they can be used as substitutes of true endpoints in clinical studies. However, even though several evaluation methods have been introduced over the last decades, the identification of good surrogate endpoints remains practically and conceptually challenging. In the present work, the question regarding the existence of a good surrogate is addressed using information-theoretic concepts, within a causal-inference framework. Read More

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http://dx.doi.org/10.1080/10543406.2018.1559854DOI Listing
January 2019
1 Read

Drug delivery of rifampicin by natural micelles based on inulin: Physicochemical properties, antibacterial activity and human macrophages uptake.

Eur J Pharm Biopharm 2019 Mar 24;136:250-258. Epub 2019 Jan 24.

Department of Pharmacy-Drug Science, University of Bari "Aldo Moro", Via Orabona 4, 70125 Bari, Italy. Electronic address:

This work aims at designing a drug delivery system for rifampicin (RIF) to be used for the therapy of infections from mycobacterium tuberculosis or other lung-colonizing bacteria. We are proposing, in particular, the delivery of RIF by micelles based on inulin functionalized with vitamin E (INVITE). We previously demonstrated that INVITE micelles are formed from the self-assembling sustained by the interaction, within the hydrophobic core, of aromatic groups belonging to vitamin E. Read More

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https://linkinghub.elsevier.com/retrieve/pii/S09396411183151
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http://dx.doi.org/10.1016/j.ejpb.2019.01.022DOI Listing
March 2019
6 Reads

Biophysical interaction of temozolomide and its active metabolite with biomembrane models: The relevance of drug-membrane interaction for Glioblastoma Multiforme therapy.

Eur J Pharm Biopharm 2019 Mar 22;136:156-163. Epub 2019 Jan 22.

LEPABE - Laboratory for Process Engineering, Environment, Biotechnology and Energy, R. Dr. Roberto Frias, 4200-465 Porto, Portugal. Electronic address:

Temozolomide (TMZ) is the first-line treatment for Glioblastoma Multiforme (GBM). After administration, TMZ is rapidly converted into its active metabolite (MTIC). However, its pharmacological activity is reduced due MTIC low bioavailability in the brain. Read More

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http://dx.doi.org/10.1016/j.ejpb.2019.01.015DOI Listing

The effect of chitosan on the bioaccessibility and intestinal permeability of acyclovir.

Eur J Pharm Biopharm 2019 Mar 22;136:147-155. Epub 2019 Jan 22.

Institute of Pharmacy and Biochemistry, Johannes Gutenberg University, Mainz, Germany. Electronic address:

Chitosan is object of pharmaceutical research as a candidate permeability enhancer. However, chitosan was recently shown to reduce the oral bioavailability of acyclovir in humans. The effect of chitosan on two processes determining the oral bioavailability of acyclovir, bioaccessibility and intestinal absorption, was now investigated. Read More

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https://linkinghub.elsevier.com/retrieve/pii/S09396411173148
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http://dx.doi.org/10.1016/j.ejpb.2019.01.021DOI Listing
March 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

Oral coadministration of elacridar and ritonavir enhances brain accumulation and oral availability of the novel ALK/ROS1 inhibitor lorlatinib.

Eur J Pharm Biopharm 2019 Mar 17;136:120-130. Epub 2019 Jan 17.

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

Lorlatinib, a novel generation oral anaplastic lymphoma kinase (ALK) and ROS1 inhibitor with high membrane and blood-brain barrier permeability, recently received accelerated approval for treatment of ALK-rearranged non-small-cell lung cancer (NSCLC), and its further clinical development is ongoing. We previously found that the efflux transporter P-glycoprotein (MDR1/ABCB1) restricts lorlatinib brain accumulation and that the drug-metabolizing enzyme cytochrome P450-3A (CYP3A) limits its oral availability. Using genetically modified mouse models, we investigated the impact of targeted pharmacological inhibitors on lorlatinib pharmacokinetics and bioavailability. Read More

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http://dx.doi.org/10.1016/j.ejpb.2019.01.016DOI Listing
March 2019
8 Reads

Screening a trace amount of pharmaceutical cocrystals by using an enhanced nano-spot method.

Eur J Pharm Biopharm 2019 Mar 17;136:131-137. Epub 2019 Jan 17.

Department of Molecular Pharmaceutics, Meiji Pharmaceutical University, 2-522-1 Noshio, Kiyose, Tokyo 204-8588, Japan. Electronic address:

Cocrystallization is an attractive and promising technology that can improve the physical properties of formulations of active pharmaceutical ingredients (APIs). We have developed a "nano-spot method" that can evaluate the crystalline form on the nanogram scale. In this study, the following studies were performed to obtain versatile and comprehensive improvements to the nano-spot method: modification of the sample solution, application of solvent vapor exposure to attempt the precipitation of various states of crystals, and adoption of low-frequency Raman spectroscopy. Read More

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http://dx.doi.org/10.1016/j.ejpb.2019.01.018DOI Listing
March 2019
1 Read

Efficacy of a novel LyP-1-containing self-microemulsifying drug delivery system (SMEDDS) for active targeting to breast cancer.

Eur J Pharm Biopharm 2019 Mar 22;136:138-146. Epub 2019 Jan 22.

Department of Pharmaceutical Technology, Faculty of Pharmacy, Hacettepe University, Ankara, Turkey. Electronic address:

An ideal cancer therapy targets the tumor cells selectively without damaging healthy tissues. Even though the tumor-specific markers are limited, these molecules can be used for the delivery of anti-cancer drugs as an active targeting strategy. Since the lymphatic system plays a critical role in the dissemination of cancer cells, the drugs directed through lymphatics can feasibly reach to the sites of metastasis. Read More

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http://dx.doi.org/10.1016/j.ejpb.2019.01.017DOI Listing
March 2019
2 Reads

Development of electrospun nanofibers that enable high loading and long-term viability of probiotics.

Eur J Pharm Biopharm 2019 Mar 17;136:108-119. Epub 2019 Jan 17.

Department of Biotechnology, Jožef Stefan Institute, Jamova 39, SI-1000 Ljubljana, Slovenia; Faculty of Pharmacy, University of Ljubljana, Aškerčeva 7, SI-1000 Ljubljana, Slovenia. Electronic address:

The interest in probiotics has grown in recent years due to increased awareness of the importance of microbiota for human health. We present the development of monolithic poly(ethylene oxide) and composite poly(ethylene oxide)/lyoprotectant nanofibers loaded with the probiotic Lactobacillus plantarum ATCC 8014. High loading was achieved for L. Read More

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http://dx.doi.org/10.1016/j.ejpb.2019.01.013DOI Listing
March 2019
2 Reads

Formulation development of a continuously manufactured orodispersible film containing warfarin sodium for individualized dosing.

Eur J Pharm Biopharm 2019 Mar 17;136:93-101. Epub 2019 Jan 17.

Heinrich Heine University Düsseldorf, Institute of Pharmaceutics and Biopharmaceutics, Universitätsstr. 1, 40225 Düsseldorf, Germany. Electronic address:

Continuously manufactured orodispersible films (ODFs) offer a promising approach for individualized therapy with an easy to administer solid dosage form. The aim of this study was to develop a long ODF containing warfarin sodium to enable safe and more flexible dosing. Formulation development was conducted systematically for the continuous film coating process. Read More

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http://dx.doi.org/10.1016/j.ejpb.2019.01.011DOI Listing
March 2019
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Ultrasound-responsive nanobubbles for enhanced intravitreal drug migration: An ex vivo evaluation.

Eur J Pharm Biopharm 2019 Mar 17;136:102-107. Epub 2019 Jan 17.

The University of Queensland, School of Pharmacy, Pharmacy Australia Centre of Excellence, 20 Cornwall Street, Woolloongabba, Brisbane, QLD 4102, Australia. Electronic address:

The intravitreal route faces many challenges in rapidly and effectively reaching posterior eye pathology, with administered therapeutics experiencing non-specific distribution around and premature clearance from ocular tissues. Nanobubbles and ultrasound may improve outcomes of intravitreally administered drugs by influencing the directionality of drug-containing particle migration. In this study, we assessed the impact of trans-scleral or corneal ultrasound application on the distribution of intravitreally-injected nanobubbles. Read More

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http://dx.doi.org/10.1016/j.ejpb.2019.01.014DOI Listing
March 2019
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A novel technique for intraduodenal administration of drug suspensions/solutions with concurrent pH monitoring applied to ibuprofen formulations.

Eur J Pharm Biopharm 2019 Mar 16;136:192-202. Epub 2019 Jan 16.

Johannes Gutenberg-Universität, Staudingerweg 5, 55099 Mainz, Germany. Electronic address:

Characterization of dissolution of solid suspended drug particles in vivo is important for developing biopredictive in vitro tests. Therefore, methods to gain deeper insights into particle dissolution in vivo are needed. The soft Bioperm intubation method, a well established tool for investigation of permeability, absorption, metabolism, and drug interactions at predefined locations in the gastroinstinal tract, was modified. Read More

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https://linkinghub.elsevier.com/retrieve/pii/S09396411183149
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http://dx.doi.org/10.1016/j.ejpb.2019.01.010DOI Listing
March 2019
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Potential therapeutic effect of curcumin loaded hyalurosomes against inflammatory and oxidative processes involved in the pathogenesis of rheumatoid arthritis: The use of fibroblast-like synovial cells cultured in synovial fluid.

Eur J Pharm Biopharm 2019 Mar 17;136:84-92. Epub 2019 Jan 17.

Department of Scienze della Vita e dell'Ambiente, CNBS, University of Cagliari, Cagliari, Italy.

In the present work curcumin loaded hyalurosomes were proposed as innovative systems for the treatment of rheumatoid arthritis. Vesicles were prepared using a one-step and environmentally friendly method. Aiming at finding the most suitable formulation in terms of size, surface charge and stability on storage, an extensive pre-formulation study was performed using different type and amount of phospholipids. Read More

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https://linkinghub.elsevier.com/retrieve/pii/S09396411183145
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http://dx.doi.org/10.1016/j.ejpb.2019.01.012DOI Listing
March 2019
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Covalently crosslinked organophosphorous derivatives-chitosan hydrogel as a drug delivery system for oral administration of camptothecin.

Eur J Pharm Biopharm 2019 Mar 14;136:174-183. Epub 2019 Jan 14.

Instituto Interuniversitario de Investigación de Reconocimiento Molecular y Desarrollo Tecnológico (IDM), Universitat Politècnica de València, Universitat de València, Dpto. de Farmacia y Tecnología Farmacéutica y Parasitología, Vicente Andrés Estelles s/n, Burjassot, Valencia, Spain.

Hydrogels are widely studied as drug delivery system. In this work we propose the employment of tetrakis(hydroxymethyl)phosphonium chloride as crosslinking agent to obtain covalent hydrogels based on chitosan. These hydrogels are obtained by Mannich reaction between the amino groups of chitosan with the hydroxymethyl groups of the crosslinker molecule. Read More

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http://dx.doi.org/10.1016/j.ejpb.2019.01.009DOI Listing
March 2019
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Functional characterization for polymorphic organic anion transporting polypeptides (OATP/SLCO1B1, 1B3, 2B1) of monkeys recombinantly expressed with various OATP probes.

Biopharm Drug Dispos 2019 Jan 16. Epub 2019 Jan 16.

Mitsubishi Tanabe Pharma Corporation, Toda, Saitama, 335-8505, Japan.

The hepatic uptake of clinical drugs mediated by human hepatic organic anion transporting polypeptides (OATP/SLCO) has been reported extensively. In this study, hepatic uptake by recombinantly expressed monkey OATP1B1, OATP1B3 and OATP2B1 was investigated using three human OATP1B1 and OATP1B3 substrates (pitavastatin, pravastatin and rosuvastatin) and one OATP1B3 substrate (telmisartan), as the governmental drug interaction guidelines recommend, and seven reported clinical drugs. The uptake of known human probes into recombinant OATP-expressing cells was significantly greater than that of mock cells. Read More

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http://dx.doi.org/10.1002/bdd.2171DOI Listing
January 2019
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Self-assembled mPEG-hexPLA polymeric nanocarriers for the targeted cutaneous delivery of imiquimod.

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

School of Pharmaceutical Sciences, University of Geneva & University of Lausanne, Geneva, Switzerland. Electronic address:

mPEG-hexPLA micelles have shown their ability to improve delivery and cutaneous bioavailability of a wide range of poorly water soluble and lipophilic molecules. Although poorly water soluble, imiquimod (IMQ) is only moderately lipophilic and it was decided to investigate whether mPEG-hexPLA polymeric micelles could be used as a drug delivery system for this "less than ideal" candidate for encapsulation. Nanosized IMQ micelles (d = 27 nm) were formulated and characterized. Read More

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http://dx.doi.org/10.1016/j.ejpb.2019.01.008DOI Listing
January 2019
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Tumor recognition of peanut agglutinin-immobilized fluorescent nanospheres in biopsied human tissues.

Eur J Pharm Biopharm 2019 Mar 9;136:29-37. Epub 2019 Jan 9.

Faculty of Pharmaceutical Sciences, Setsunan University, Hirakata 573-0101, Japan. Electronic address:

We are investigating an imaging agent for early detection of colorectal cancer. The agent, named the nanobeacon, is coumarin 6-encapsulated polystyrene nanospheres whose surfaces are covered with poly(N-vinylacetamide) and peanut agglutinin that reduces non-specific interactions with the normal mucosa and exhibits high affinity for terminal sugars of the Thomsen-Friedenreich antigen, which is expressed cancer-specifically on the mucosa, respectively. We expect that cancer can be diagnosed by detecting illumination of intracolonically administered nanobeacon on the mucosal surface. Read More

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http://dx.doi.org/10.1016/j.ejpb.2019.01.007DOI Listing
March 2019
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Epigenetics and Sphingolipid Metabolism in Health and Disease.

Int J Biopharm Sci 2018 Oct 22;1(2). Epub 2018 Jan 22.

Department of Molecular, Cellular and Biomedical Sciences, University of New Hampshire, Durham, NH 03824 USA.

Sphingolipids represent one of the major classes of bioactive lipids. Studies of sphingolipids have intensified in the past several years, revealing their roles in nearly all cell biological processes. In addition, epigenetic regulation has gained substantial interest due to its role in controlling gene expression and activity without changing the genetic code. Read More

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http://dx.doi.org/10.31021/ijbs.20181105DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6326171PMC
October 2018
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Identification of specific UGT1A9-mediated glucuronidation of licoricidin in human liver microsomes.

Biopharm Drug Dispos 2019 Jan 12. Epub 2019 Jan 12.

BK21 Plus KNU Multi-Omics Based Creative Drug Research Team, College of Pharmacy, Research Institute of Pharmaceutical Sciences, Kyungpook National University, Daegu, 41566, Republic of Korea.

Licoricidin is a major prenylated isoflavone of Glycyrrhiza uralensis Fisch. (Leguminosae), and its pharmacological effects have been reported frequently. Typically, flavonoids having multiple hydroxyl groups are unambiguous substrates for glucuronyl conjugation by UDP-glucuronosyltransferases (UGTs). Read More

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http://doi.wiley.com/10.1002/bdd.2169
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http://dx.doi.org/10.1002/bdd.2169DOI Listing
January 2019
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Application of data mining approach to identify drug subclasses based on solubility and permeability.

Biopharm Drug Dispos 2019 Jan 11. Epub 2019 Jan 11.

Department of Pharmaceutical Technology and Cosmetology, University of Belgrade - Faculty of Pharmacy, Vojvode Stepe 450, 11221, Belgrade, Serbia.

Solubility and permeability are recognized as key parameters governing drug intestinal absorption and represent the basis for biopharmaceutics drug classification. The Biopharmaceutics Classification System (BCS) is widely accepted and adopted by regulatory agencies. However, currently established low/high permeability and solubility boundaries are the subject of the ongoing scientific discussion. Read More

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http://doi.wiley.com/10.1002/bdd.2170
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http://dx.doi.org/10.1002/bdd.2170DOI Listing
January 2019
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Polyamidoamine dendrimers-based nanomedicine for combination therapy with siRNA and chemotherapeutics to overcome multidrug resistance.

Eur J Pharm Biopharm 2019 Mar 8;136:18-28. Epub 2019 Jan 8.

Center for Pharmaceutical Biotechnology and Nanomedicine, Northeastern University, Boston, MA 02115, USA. Electronic address:

Multidrug resistance (MDR) significantly decreases the therapeutic efficiency of anti-cancer drugs. Its reversal could serve as a potential method to restore the chemotherapeutic efficiency. Downregulation of MDR-related proteins with a small interfering RNA (siRNA) is a promising way to reverse the MDR effect. Read More

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https://linkinghub.elsevier.com/retrieve/pii/S09396411183121
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http://dx.doi.org/10.1016/j.ejpb.2019.01.006DOI Listing
March 2019
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Recent advances in microneedle-based drug delivery: Special emphasis on its use in paediatric population.

Eur J Pharm Biopharm 2019 Mar 8;136:48-69. Epub 2019 Jan 8.

School of Pharmacy, Faculty of Medical and Health Sciences, University of Auckland, New Zealand. Electronic address:

Transdermal drug delivery offers several attractive advantages over the traditional oral and parenteral routes. Particularly, in case of paediatric patients, it helps to overcome the issues specific to this population, such as difficulty in swallowing and palatability of oral medicines as well as fear and pain associated with needles. However, due to the formidable barrier characteristic of the stratum corneum, it fails in the effective systemic delivery of broad range of therapeutic molecules, especially macromolecules and genetic material. Read More

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http://dx.doi.org/10.1016/j.ejpb.2019.01.005DOI Listing
March 2019
2 Reads

Stability of lysozyme incorporated into electrospun fibrous mats for wound healing.

Eur J Pharm Biopharm 2019 Mar 7;136:240-249. Epub 2019 Jan 7.

Department of Pharmacy, University of Copenhagen, Universitetsparken 2, DK-2100 Copenhagen, Denmark; Wuya College of Innovation, Shenyang Pharmaceutical University, Wenhua Road No. 103, 110016 Shenyang, China. Electronic address:

In this study, we investigated the feasibility of incorporating protein drugs into electrospun fibrous mats (EFMs) for wound healing using lysozyme as a model drug. Lysozyme nanoparticles (Lyso- NPs) were first obtained by electrospray. Lysozyme solutions were prepared with a binary solvent mixture of ethanol (EtOH)-water (HO) at varied volume ratios. Read More

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https://linkinghub.elsevier.com/retrieve/pii/S09396411183070
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http://dx.doi.org/10.1016/j.ejpb.2019.01.003DOI Listing
March 2019
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Edible solid foams as porous substrates for inkjet-printable pharmaceuticals.

Eur J Pharm Biopharm 2019 Mar 8;136:38-47. Epub 2019 Jan 8.

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

The aim of this study was to investigate new porous flexible substrates, i.e., solid foams that would serve as a carrier with a high ink absorption potential for inkjet printable pharmaceuticals. Read More

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http://dx.doi.org/10.1016/j.ejpb.2019.01.004DOI Listing
March 2019
1 Read