10,156 results match your criteria Biopharmaceutics & drug disposition[Journal]


Small angle X-ray scattering and molecular dynamic simulations provide molecular insight for stability of recombinant human transferrin.

J Struct Biol X 2020 30;4:100017. Epub 2019 Nov 30.

Department of Chemistry, Technical University of Denmark, Kemitorvet 207, 2800 Kgs. Lyngby, Denmark.

Transferrin is an attractive candidate for drug delivery due to its ability to cross the blood brain barrier. However, in order to be able to use it for therapeutic purposes, it is important to investigate how its stability depends on different formulation conditions. Combining high-throughput thermal and chemical denaturation studies with small angle X-ray scattering (SAXS) and molecular dynamics (MD) simulations, it was possible to connect the stability of transferrin with its conformational changes. Read More

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http://dx.doi.org/10.1016/j.yjsbx.2019.100017DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC7337065PMC
November 2019

The Luminescence of 1,8-Diazafluoren-9-One/Titanium Dioxide Composite Thin Films for Optical Application.

Materials (Basel) 2020 Jul 6;13(13). Epub 2020 Jul 6.

Department of Biopharmaceutics and Pharmacodynamics, Medical University of Gdańsk, Al. Gen. Hallera 107, 80-416 Gdańsk, Poland.

The investigation of innovative label-free α-amino acids detection methods represents a crucial step for the early diagnosis of several diseases. While 1,8-diazafluoren-9-one (DFO) is known in forensic application because of the fluorescent products by reacting with the amino acids present in the papillary exudate, its application for diagnostic purposes has not been fully investigated. The stabilization of DFO over a transparent substrate allows its complexation with biomolecules for the detection of α-amino acids. Read More

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http://dx.doi.org/10.3390/ma13133014DOI Listing

Investigation of the therapeutic effect of Shaoyao Gancao decoction on CCL -induced liver injury in rats by metabolomic analysis.

Biomed Chromatogr 2020 Jul 7:e4940. Epub 2020 Jul 7.

School of Pharmacy, Shenyang Pharmaceutical University, Shenyang, Liaoning Province, China.

Shaoyao Gancao decoction (SGD) is a famous Chinese traditional prescription for treating liver injury. In this research, we investigated the liver protective effects of SGD and its metabolic mechanisms by H-NMR and UPLC-MS. Serum biochemical indicators and histopathological methods werae used to identify the status of SGD in treating liver injury. Read More

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http://dx.doi.org/10.1002/bmc.4940DOI Listing

Biopharmaceutics and Pharmacokinetics of Timosaponin A-III by a Sensitive HPLC-MS/MS Method: Low Bioavailability Resulting from Poor Permeability and Solubility.

Curr Pharm Biotechnol 2020 Jul 7. Epub 2020 Jul 7.

Department of Pharmacy, Shanghai Changhai Hospital, Second Military Medical University, Shanghai 200433. China.

Background: Timosaponin A-III is one of the most promising active saponins from Anemarrhena asphodeloides Bge. As an oral chemotherapeutic agent, there is an urgent need to clarify its biopharmaceutics and pharmacokinetics to improve its development potential.

Objective: This research explores the bioavailability of timosaponin A-III and clarifies its absorption and metabolism mechanisms by a sensitive and specific HPLC-MS/MS method. Read More

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http://dx.doi.org/10.2174/1389201021666200707134045DOI Listing

DNA density-dependent uptake of DNA origami-based two-or three-dimensional nanostructures by immune cells.

Nanoscale 2020 Jul 7. Epub 2020 Jul 7.

Department of Biopharmaceutics and Drug Metabolism, Graduate School of Pharmaceutical Sciences, Kyoto University, Sakyo-ku, Kyoto 606-8501, Japan and Laboratory of Biopharmaceutics, Faculty of Pharmaceutical Sciences, Tokyo University of Science, Noda, Chiba 278-8510, Japan.

DNA nanostructures are expected to be applied for targeted drug delivery to immune cells. However, the structural properties of DNA nanostructures required for the delivery have not fully been elucidated. In this study, we focused on the DNA density that can be important for the their recognition and uptake by immune cells. Read More

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http://dx.doi.org/10.1039/d0nr02361bDOI Listing

Gold nanoparticles phytoreduced with Cornus mas extract mitigate some of gliadin effects on Caco-2 cells.

J Physiol Pharmacol 2020 Apr 2;71(2). Epub 2020 Jul 2.

Department of Gastroenterology and Hepatology, Regional Institute of Gastroenterology and Hepatology, "Iuliu Hatieganu" University of Medicine and Pharmacy, Cluj-Napoca, Romania.

Celiac disease (CD) is an autoimmune condition that occurs in genetically predisposed people where the ingestion of gluten produces damage in the small intestine. The treatment accepted until now is a strict gluten free diet. This implies the need for novel or adjuvant treatments, in addition to the standard of care. Read More

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http://dx.doi.org/10.26402/jpp.2020.2.04DOI Listing

Population pharmacokinetics of Anidulafungin in ICU patients assessing inter- and intra-subject variability.

Br J Clin Pharmacol 2020 Jul 7. Epub 2020 Jul 7.

Laboratory of Biopharmaceutics-Pharmacokinetics, Department of Pharmacy, National and Kapodistrian University of Athens, Athens, Greece.

Aims: The population pharmacokinetics (PKs) of anidulafungin in critically ill patients hospitalized in ICU was explored with the scope of evaluating and optimizing dosing regimens.

Methods: A PK study has been conducted in a cohort of 13 patients treated with anidulafungin using intensive sampling during multiple periods per patient and HPLC method for drug quantification. A population PK model was developed to describe the concentration-time course of anidulafungin and the inter-individual (IIV) and inter-occasion variability (IOV) of the PK parameters. Read More

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http://dx.doi.org/10.1111/bcp.14457DOI Listing

How Does the CO in Supercritical State Affect the Properties of Drug-Polymer Systems, Dissolution Performance and Characteristics of Tablets Containing Bicalutamide?

Materials (Basel) 2020 Jun 25;13(12). Epub 2020 Jun 25.

Department of Pharmaceutical Technology and Biopharmaceutics, Faculty of Pharmacy, Jagiellonian University Medical College, Medyczna 9, 30-688 Krakow, Poland.

The increasing demand for novel drug formulations has caused the introduction of the supercritical fluid technology, CO in particular, into pharmaceutical technology as a method enabling the reduction of particle size and the formation of inclusion complexes and solid dispersions. In this paper, we describe the application of scCO in the preparation of binary systems containing poorly soluble antiandrogenic drug bicalutamide and polymeric excipients, either Macrogol 6000 or Poloxamer407. The changes in the particle size and morphology were followed using scanning electron microscopy and laser diffraction measurements. Read More

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http://dx.doi.org/10.3390/ma13122848DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC7344854PMC

Awareness, knowledge, and attitudes of health professions students toward health economics and pharmacoeconomics education in Jordan.

Curr Pharm Teach Learn 2020 Sep 30;12(9):1072-1080. Epub 2020 Apr 30.

Pathology and Microbiology, Department of Pathology and Microbiology, Jordan University of Science and Technology, Irbid 22110, Jordan. Electronic address:

Introduction: Health economics education (HEe) and pharmacoeconomics education (PEe) in the Middle East and North Africa area is growing, particularly in pharmacy education. Little is known about the awareness, knowledge, and attitudes of health professions students toward health economics (HE) and pharmacoeconomics (PE) and the extent of education they receive before joining the workforce.

Methods: A self-completed validated questionnaire was distributed to students from medical, dental, pharmacy, and nursing schools in Jordan. Read More

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http://dx.doi.org/10.1016/j.cptl.2020.04.027DOI Listing
September 2020

Protein structure analysis of the interactions between SARS-CoV-2 spike protein and the human ACE2 receptor: from conformational changes to novel neutralizing antibodies.

Cell Mol Life Sci 2020 Jul 4. Epub 2020 Jul 4.

Laboratory of Biochemistry, Molecular and Structural Biology, Department of Biosciences, Biotechnologies, Biopharmaceutics, University of Bari, Via E. Orabona, 4, 70125, Bari, Italy.

The recent severe acute respiratory syndrome, known as Coronavirus Disease 2019 (COVID-19) has spread so much rapidly and severely to induce World Health Organization (WHO) to declare a state of emergency over the new coronavirus SARS-CoV-2 pandemic. While several countries have chosen the almost complete lock-down for slowing down SARS-CoV-2 spread, the scientific community is called to respond to the devastating outbreak by identifying new tools for diagnosis and treatment of the dangerous COVID-19. With this aim, we performed an in silico comparative modeling analysis, which allows gaining new insights into the main conformational changes occurring in the SARS-CoV-2 spike protein, at the level of the receptor-binding domain (RBD), along interactions with human cells angiotensin-converting enzyme 2 (ACE2) receptor, that favor human cell invasion. Read More

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http://dx.doi.org/10.1007/s00018-020-03580-1DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC7334636PMC

Performance tuning of particle engineered mannitol in dry powder inhalation formulations.

Int J Pharm 2020 Jul 2:119592. Epub 2020 Jul 2.

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

Typically, smooth lactose particles are used as carrier in dry powder formulations for inhalation. Two classical approaches to improve their aerodynamic behaviour are the addition of fines (milled lactose) or magnesium stearate (MgSt). Mannitol (Parteck® M DPI) as an alternative carrier was used in this study. Read More

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http://dx.doi.org/10.1016/j.ijpharm.2020.119592DOI Listing

Possible utility of peptide-transporter-targeting [F]dipeptides for visualization of the biodistribution of cancers by nuclear magnetic resonance imaging.

Int J Pharm 2020 Jul 2:119575. Epub 2020 Jul 2.

Laboratory of Biopharmaceutics, Faculty of Pharmacy, Takasaki University of Health and Welfare, Takasaki, 370-0033, Japan; Laboratory of Clinical Pharmacokinetics, Graduate School of Pharmaceutical Sciences, Takasaki University of Health and Welfare, Takasaki, 370-0033, Japan.

Stable-isotope-labeled probes suitable for magnetic resonance imaging (MRI) would have various potential medical applications, such as tumor imaging. Here, with the aim of developing MRI probes targeting peptide transporters, we synthesized a series of [F]dipeptides by introducing one or two fluorine atoms or a trifluoromethyl group into the benzene ring of L-phenylalanyl-ψ[CS-N]-L-alanine (Phe-ψ-Ala), which is resistant to cleavage by peptidases. The mono- and difluoro dipeptides were efficiently transported by PEPT1 and PEPT2. Read More

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http://dx.doi.org/10.1016/j.ijpharm.2020.119575DOI Listing

A simple and rapid LC-MS/MS and CE-MS/MS analytical strategy for the determination of therapeutic peptides in modern immunotherapeutics and biopharmaceutics.

J Pharm Biomed Anal 2020 Jun 25;189:113449. Epub 2020 Jun 25.

Institute of Neuroimmunology, Slovak Academy of Sciences, Dubravska cesta 9, SK-845 10 Bratislava, Slovak Republic. Electronic address:

Modern therapy of metabolic, neurodegenerative, inflammation, or cancer diseases is recently based on an immunotherapeutic approach. The peptide conjugates represent innovative and effective therapeutics that are better tolerated and are much more specific than small molecule-based medicines. The nature and manufacturing process of these therapeutics make their analysis very challenging. Read More

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http://dx.doi.org/10.1016/j.jpba.2020.113449DOI Listing

A perspective on the physicochemical and biopharmaceutic properties of marketed antiseizure drugs-From phenobarbital to cenobamate and beyond.

Epilepsia 2020 Jul 2. Epub 2020 Jul 2.

Faculty of Medicine, School of Pharmacy, Institute of Drug Research, Hebrew University of Jerusalem, Jerusalem, Israel.

The success rate from first time in man to regulatory approval of central nervous system (CNS) drugs is lower than the overall success rate across all therapeutic indications (eg, cardiovascular, infectious diseases). To understand the reasons for drug-candidate failure and to capture trends in antiseizure drug (ASD) design, we have analyzed the physicochemical and biopharmaceutical properties of marketed ASDs in comparison with new ASDs in development. Our comparative analysis included molecular weight (MW), logP, polar surface area (PSA), the "Lipinski rule of five," and the CNS Multiparameter Optimization (MPO) score. Read More

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http://dx.doi.org/10.1111/epi.16597DOI Listing

Utilization of Diluted Compendial Media as Dissolution Test Solutions with Low Buffer Capacity for the Investigation of Dissolution Rate of Highly Soluble Immediate Release Drug Products.

Chem Pharm Bull (Tokyo) 2020 ;68(7):664-670

Division of Drugs, National Institute of Health Sciences.

Research from the past decade has shown that the buffer capacities of intestinal fluids are much lower than those in the media used for dissolution test of many solid formulations. The purpose of this study was to elucidate the effect of buffer capacity on the dissolution profiles of highly soluble drug products, using metoclopramide (a biopharmaceutics classification system [BCS] class III drug) tablets as a model. The dissolution profiles of three metoclopramide products were obtained in Japanese pharmacopeia dissolution medium (pH 1. Read More

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http://dx.doi.org/10.1248/cpb.c20-00247DOI Listing
January 2020

Drug Delivery System for Refractory Cancer Therapy via an Endogenous Albumin Transport System.

Chem Pharm Bull (Tokyo) 2020 ;68(7):583-588

Department of Pharmacokinetics and Biopharmaceutics, Institute of Biomedical Sciences, Tokushima University.

A unique phenomenon in solid tumors, the enhanced permeability and retention (EPR) effect is now well known in the development of macromolecular anticancer therapy. However, cancers with low vascular permeability have posed a challenge for these EPR based therapeutic systems. An intrinsic vascular modulator, such as nitric oxide (NO), could augment the endogenous EPR effect. Read More

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http://dx.doi.org/10.1248/cpb.c20-00026DOI Listing
January 2020

Bone-Targeted Drug Delivery Systems and Strategies for Treatment of Bone Metastasis.

Chem Pharm Bull (Tokyo) 2020 ;68(7):560-566

Department of Biopharmaceutics, Kyoto Pharmaceutical University.

Bone metastases can cause high morbidity and mortality, often developing as they advance, especially in patients with prostate and breast cancers. Most drugs are rarely distributed to the bone and are hence pharmacologically ineffective in treating bone metastases. The development of drug targeting technologies is required for the efficient treatment of bone metastases. Read More

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http://dx.doi.org/10.1248/cpb.c20-00017DOI Listing
January 2020

Chiral bioanalytical methods in bioequivalence studies of intravenous vs. oral formulations of ibuprofen.

Chirality 2020 Jun 29. Epub 2020 Jun 29.

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

According to the Ibuprofen Product-Specific Bioequivalence Guidance of the European Medicines Agency, achiral bioanalytical methods are considered acceptable for demonstration of bioequivalence of ibuprofen-containing products. The aim of this investigation is to compare the bioequivalence outcomes obtained with individual R and S ibuprofen enantiomers and the sum of both enantiomers from bioequivalence studies in which new intravenous ibuprofen products were compared with oral ibuprofen products. Bioequivalence was assessed for S and R enantiomers of ibuprofen and the sum of both enantiomers, which was calculated to represent the results that would have been obtained with an achiral assay. Read More

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http://dx.doi.org/10.1002/chir.23258DOI Listing

Policy of Multisource Drug Products in Latin America: Opportunities and Challenges on the Application of Bioequivalence In Vitro Assays.

Ther Innov Regul Sci 2020 Jun 29. Epub 2020 Jun 29.

Unit of Modeling and Experimental Biopharmaceutics, Centre of Chemical Bioactive, Central University of Las Villas, Villa Clara, 54830, Santa Clara, Cuba.

Background: The replacement of traditional in vivo bioequivalence studies by in vitro dissolution assays, based on the biopharmaceutical classification system (BCS), has emerged as an important tool for demonstrating the interchangeability of multisource products. This paper summarizes the current implementation of the BCS-based biowaiver for the development of multisource products in Latin America, and identifies several challenges and opportunities for greater convergence and application of BCS regulatory requirements.

Methods: Differences and similarities between the current BCS-based biowaivers' guidelines proposed by two relevant regulatory agencies for the Latin American region (FDA and WHO) and the new ICH harmonization guideline were identified and compared. Read More

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http://dx.doi.org/10.1007/s43441-020-00191-7DOI Listing

Non-stationary pharmacokinetics of caspofungin in ICU patients.

Antimicrob Agents Chemother 2020 Jun 29. Epub 2020 Jun 29.

Department of Biopharmaceutics and Pharmacodynamics, Medical University of Gdańsk, Al. Gen. Hallera 107, 80-416 Gdańsk, Poland

Standard dosing of caspofungin in critically ill patients has been reported to result in lower drug exposure, which can lead to subtherapeutic AUC/MIC ratios. The aim of the study was to investigate the population pharmacokinetics of caspofungin in a cohort of 30 ICU patients with a suspected invasive fungal infection, with a large proportion of patients requiring extracorporeal therapies including ECMO and CRRT. Caspofungin was administered as empirical antifungal therapy 70 mg i. Read More

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http://dx.doi.org/10.1128/AAC.00345-20DOI Listing

Magnetic resonance activatable thermosensitive liposomes for controlled doxorubicin delivery.

Mater Sci Eng C Mater Biol Appl 2020 Oct 25;115:111116. Epub 2020 May 25.

Department of Pharmaceutics and Biopharmaceutics, University of Marburg, 35037 Marburg, Germany. Electronic address:

To limit the massive cytotoxicity of chemotherapeutic agents, it is desirable to establish an appropriate subtle blend of formulation design based on a dual-responsive strategy. In this study, a combined therapeutic platform based on magnetic thermosensitive liposomes (Lip) was developed. The incorporation of chelated-gadolinium imparted magnetic properties to thermosensitive liposomes (Lip). Read More

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http://dx.doi.org/10.1016/j.msec.2020.111116DOI Listing
October 2020

Biocompatible indocyanine green loaded PLA nanofibers for in situ antimicrobial photodynamic therapy.

Mater Sci Eng C Mater Biol Appl 2020 Oct 11;115:111068. Epub 2020 May 11.

Department of Pharmaceutics and Biopharmaceutics, University of Marburg, Robert-Koch-Str. 4, 35037 Marburg, Germany. Electronic address:

Chronic wounds and their associated bacterial infections are major issues in modern health care systems. Therefore, antimicrobial resistance (AMR), treatment costs, and number of disability-adjusted life-years have gained more interest. Recently, photodynamic therapy emerged as an effective approach against resistant and naïve bacterial strains with a low probability of creating AMR. Read More

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http://dx.doi.org/10.1016/j.msec.2020.111068DOI Listing
October 2020

Influence of the surface tension of wet massing liquid on the functionality of microcrystalline cellulose as pelletization aid.

Eur J Pharm Biopharm 2020 Jun 26. Epub 2020 Jun 26.

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

This study designed to investigate the impact of surface tension of moistening liquid on the functionality of MCC as pelletization aid. For this purpose, sodium dodecyl sulfate (SDS), poloxamer 188 (PL), di-potassium hydrogen phosphate (KHPO) and combinations thereof were incorporated into the powder blend comprised of MCC and dicalcium phosphate (DCP) at different levels. Physical mixture (PM) and co-processed composite (Cop) of MCC and sodium carboxymethyl cellulose (SCMC) replaced MCC as pelletization aids. Read More

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http://dx.doi.org/10.1016/j.ejpb.2020.06.015DOI Listing
June 2020
3.383 Impact Factor

Assessment of tramadol pharmacokinetics in correlation with CYP2D6 and clinical symptoms.

Drug Metab Pers Ther 2020 Jun 29. Epub 2020 Jun 29.

Department of Pharmacology, School of Medicine, Tehran University of Medical Sciences, Tehran, Iran.

Objectives Due to lack of adequate data on tramadol kinetic in relevance of CYP2D6 toxicity, this study was designed to investigate the effect of CYP2D6 phenotype in tramadol poisoning. The saliva, urine and blood samples were taken at the admission time. Consequently, concentration of tramadol and its major metabolites were measured. Read More

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http://dx.doi.org/10.1515/dmdi-2019-0021DOI Listing

Evaluation of the Completeness of Information Sources Used to Prepare the Best Possible Medication Histories at a Tertiary Teaching Hospital in Jordan.

Int J Clin Pract 2020 Jun 27:e13597. Epub 2020 Jun 27.

Department of Pharmacy, Sultan Qaboos University Hospital, Sultan Qaboos University, Muscat, Oman.

Objectives: In this study we aimed to evaluate the completeness of three different medication information sources that are commonly used to collect and obtain the Best Possible Medication History (BPMH).

Methods: This is an observational study which was held at Jordan University Hospital. After identifying eligible patients, the BPMH was obtained from three different sources separately. Read More

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http://dx.doi.org/10.1111/ijcp.13597DOI Listing

The β-adrenergic receptor antagonist propranolol offsets resistance mechanisms to chemotherapeutics in diverse sarcoma subtypes: a pilot study.

Sci Rep 2020 Jun 26;10(1):10465. Epub 2020 Jun 26.

Experimental Pharmacology Laboratory, IRCCS Istituto Tumori Giovanni Paolo II, Viale O. Flacco, 65, 70124, Bari, Italy.

Standard chemotherapy for soft tissue sarcomas has shown limited efficacy. Here, we sought to evaluate whether β-adrenergic receptor (β-AR) signalling contributed to the progression of sarcomas and therapy resistance. To assess the translational potential of β-adrenergic receptors, we performed immunohistochemical detection of β1-AR, β2-AR and β3-AR in leiomyosarcoma, liposarcoma and angiosarcoma tissue specimens, reporting the results scored for the intensity. Read More

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http://dx.doi.org/10.1038/s41598-020-67342-6DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC7320177PMC

A physiologically-based nanocarrier biopharmaceutics model to reverse-engineer the in vivo drug release.

Eur J Pharm Biopharm 2020 Jun 23. Epub 2020 Jun 23.

National University of Singapore, Department of Pharmacy, Faculty of Science, Singapore. Electronic address:

Over the years, a wide variety of nanomedicines has entered global markets, providing a blueprint for the emerging generics industry. They are characterized by a unique pharmacokinetic behavior difficult to explain with conventional methods. In the present approach a physiologically-based nanocarrier biopharmaceutics model has been developed. Read More

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http://dx.doi.org/10.1016/j.ejpb.2020.06.004DOI Listing

Recommendations for Choosing the Genotyping Method and Best Practices for Quality Control in Crop Genome-Wide Association Studies.

Front Genet 2020 5;11:447. Epub 2020 Jun 5.

Department of Agricultural Sciences, University of Naples Federico II, Naples, Italy.

High-throughput genotyping boosts genome-wide association studies (GWAS) in crop species, leading to the identification of single-nucleotide polymorphisms (SNPs) associated with economically important traits. Choosing a cost-effective genotyping method for crop GWAS requires careful examination of several aspects, namely, the purpose and the scale of the study, crop-specific genomic features, and technical and economic matters associated with each genotyping option. Once genotypic data have been obtained, quality control (QC) procedures must be applied to avoid bias and false signals in genotype-phenotype association tests. Read More

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http://dx.doi.org/10.3389/fgene.2020.00447DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC7299185PMC

Enhancement of phenol biodegradation: Metabolic division of labor in co-culture of Stenotrophomonas sp. N5 and Advenella sp. B9.

J Hazard Mater 2020 Jun 18;400:123214. Epub 2020 Jun 18.

School of Environment and Energy, South China University of Technology, Guangzhou 510006, PR China.

The aim of this work is to study the synergistic effect of Stenotrophomonas sp. N5 and Advenella sp. B9 co-culture (COC) on enhancement of phenol biodegradation. Read More

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http://dx.doi.org/10.1016/j.jhazmat.2020.123214DOI Listing

Comparative investigations on key factors and print head designs for pharmaceutical inkjet printing.

Int J Pharm 2020 Jul 6;586:119561. Epub 2020 Jul 6.

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

The interest in using inkjet printing as manufacturing technology for personalized medicine has increased in recent years. The print head is the centrepiece of an inkjet printer. For pharmaceutical approaches, various types of printing equipment were tested in the past, but comparative investigations in relation to pharmaceutical use are still lacking. Read More

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http://dx.doi.org/10.1016/j.ijpharm.2020.119561DOI Listing

Molecular Dynamics and Physical Stability of Ibuprofen in Binary Mixtures with an Acetylated Derivative of Maltose.

Mol Pharm 2020 Jul 9. Epub 2020 Jul 9.

Institute of Physics, University of Silesia in Katowice, ul. 75 Pułku Piechoty 1, 41-500 Chorzów, Poland.

In this paper, we explore the strategy increasingly used to improve the bioavailability of poorly water-soluble crystalline drugs by formulating their amorphous solid dispersions. We focus on the potential application of a low molecular weight excipient octaacetyl-maltose (acMAL) to prepare physically stable amorphous solid dispersions with ibuprofen (IBU) aimed at enhancing water solubility of the drug compared to that of its crystalline counterpart. We thoroughly investigate global and local molecular dynamics, thermal properties, and physical stability of the IBU+acMAL binary systems by using broadband dielectric spectroscopy and differential scanning calorimetry as well as test their water solubility and dissolution rate. Read More

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http://dx.doi.org/10.1021/acs.molpharmaceut.0c00517DOI Listing

Influene of Pharmaceutical Excipients on the Membrane Transport of a P-glycoprotein Substrate in the Rat Small Intestine.

Eur J Drug Metab Pharmacokinet 2020 Jun 24. Epub 2020 Jun 24.

Laboratory of Molecular Pharmaceutics and Technology, Faculty of Pharmacy, Takasaki University of Health and Welfare, 60 Nakaorui-machi, Takasaki, Gunma, 370-0033, Japan.

Background And Objectives: Generic drugs are generally used worldwide because of affordability compared to brand-name drugs. One of the main differences between brand-name and generic drugs is pharmaceutical excipients. We previously reported the effects of pharmaceutical excipients on the membrane permeation of drugs via the paracellular and transcellular routes, which are passive transport routes. Read More

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http://dx.doi.org/10.1007/s13318-020-00631-7DOI Listing

Enhancement of dissolution of atorvastatin through preparation of polymeric solid dispersions using supercritical fluid technology.

Res Pharm Sci 2020 Apr 11;15(2):123-136. Epub 2020 May 11.

Department of Pharmaceutical Technology, Faculty of Pharmacy, Jordan University of Science and Technology, Irbid 22110, Jordan.

Background And Purpose: This study aimed at preparation of solid dispersions in order to enhance dissolution of poorly water-soluble atorvastatin using supercritical CO2 technology. Atorvastatin has poor bioavailability of 12%, mainly due to poor water solubility and dissolution. Dispersion of drugs in various hydrophilic carriers using supercritical fluid technology has been found to be an outstanding method to prepare solid dispersion. Read More

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http://dx.doi.org/10.4103/1735-5362.283812DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC7306245PMC

Activation of the VPAC2 Receptor Impairs Axon Outgrowth and Decreases Dendritic Arborization in Mouse Cortical Neurons by a PKA-Dependent Mechanism.

Front Neurosci 2020 4;14:521. Epub 2020 Jun 4.

Laboratory of Biopharmaceutics, Graduate School of Pharmaceutical Sciences, Osaka University, Suita, Japan.

Clinical studies have shown that microduplications at 7q36.3, containing , confer significant risk for schizophrenia and autism spectrum disorder (ASD). gene encodes the VPAC2 receptor for vasoactive intestinal peptide (VIP) and pituitary adenylate cyclase-activating polypeptide (PACAP). Read More

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http://dx.doi.org/10.3389/fnins.2020.00521DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC7287155PMC

A Differential Metabarcoding Approach to Describe Taxonomy Profiles of and in the Saltern of Margherita di Savoia (Italy).

Microorganisms 2020 Jun 22;8(6). Epub 2020 Jun 22.

Institute of Biomembranes, Bioenergetics and Molecular Biotechnologies, CNR, Via Amendola 122/O, 70126 Bari, Italy.

Microorganisms inhabiting saline environments are an interesting ecological model for the study of the adaptation of organisms to extreme living conditions and constitute a precious resource of enzymes and bioproducts for biotechnological applications. We analyzed the microbial communities in nine ponds with increasing salt concentrations (salinity range 4.9-36. Read More

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http://dx.doi.org/10.3390/microorganisms8060936DOI Listing

Development of a 3D Printed Coating Shell to Control the Drug Release of Encapsulated Immediate-Release Tablets.

Polymers (Basel) 2020 Jun 22;12(6). Epub 2020 Jun 22.

Future Manufacturing Processes Research Group, Faculty of Engineering and Physical Sciences, University of Leeds, Leeds LS2 9JT, UK.

The use of 3D printing techniques to control drug release has flourished in the past decade, although there is no generic solution that can be applied to the full range of drugs or solid dosage forms. The present study provides a new concept, using the 3D printing technique to print a coating system in the form of shells with various designs to control/modify drug release in immediate-release tablets. A coating system of cellulose acetate in the form of an encapsulating shell was printed through extrusion-based 3D printing technology, where an immediate-release propranolol HCl tablet was placed inside to achieve a sustained drug release profile. Read More

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http://dx.doi.org/10.3390/polym12061395DOI Listing

Development and evaluation of a biorelevant medium simulating porcine gastrointestinal fluids.

Eur J Pharm Biopharm 2020 Jun 21. Epub 2020 Jun 21.

School of Pharmacy, University College Cork, Cork, Ireland. Electronic address:

Simulated human intestinal media, have proved to be a useful biopharmaceutics tool as a dissolution media for predicting in vivo dissolution and pharmacokinetic profile in humans. During drug product development preclinical animal models are also required to assess drug product performance, and there is a need to develop species specific intestinal media to similarly predict in vivo pharmacokinetic profiles in each preclinical model. Pigs, are increasingly being used in preclinical drug development, however to date there is a lack of quantitative information about the composition of porcine gastrointestinal (GI) fluids. Read More

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http://dx.doi.org/10.1016/j.ejpb.2020.06.009DOI Listing

Long-term profile of serological biomarkers, hepatic inflammation, and fibrosis in a mouse model of non-alcoholic fatty liver disease.

Toxicol Lett 2020 Jun 21;332:1-6. Epub 2020 Jun 21.

Division of Biopharmaceutics and Pharmacokinetics, National Cerebral and Cardiovascular Center Research Institute, 6-1 Shinmachi, Kishibe, Suita, Osaka, 564-8565, Japan. Electronic address:

Non-alcoholic fatty liver disease (NAFLD) can be typically classified into two subgroups: non-alcoholic fatty liver and non-alcoholic steatohepatitis. Mouse models of NAFLD are useful tools for understanding the pathogenesis and progression of NAFLD and for developing drugs for its treatment. Here, we investigated the time-dependent changes in serum lipids and biochemical markers of hepatic function, hepatic inflammation, and fibrosis in mice fed a normal diet (ND) or a NAFLD diet (choline deficient, L-amino acid-defined, high-fat diet; CDAHFD) for 12 weeks. Read More

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http://dx.doi.org/10.1016/j.toxlet.2020.06.020DOI Listing

Engineered Capsids for Efficient Gene Delivery to the Retina and Cornea.

Hum Gene Ther 2020 Jun 24. Epub 2020 Jun 24.

Sanofi Genzyme, 2194, Gene Therapy, Cambridge, Massachusetts, United States;

Adeno-associated viral (AAV) vectors represent an ideal vehicle for human gene transfer. One advantage to the AAV vector system is the availability of multiple naturally occurring serotypes that provide selective tropisms for various target cells. Strategies to enhance the properties of the natural AAV isolates have been developed and can be divided into two approaches, rational design or directed evolution. Read More

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http://dx.doi.org/10.1089/hum.2020.070DOI Listing

Design of substrates and inhibitors of G protein-coupled receptor kinase 2 (GRK2) based on its phosphorylation reaction.

Amino Acids 2020 Jun 23. Epub 2020 Jun 23.

Department of Microbiology, St. Marianna University School of Medicine, 2-16-1 Sugao, Miyamae, Kawasaki, 216-8511, Japan.

The G protein-coupled receptor kinase (GRK) family consists of seven cytosolic serine/threonine (Ser/Thr) protein kinases, and among them, GRK2 is involved in the regulation of an enormous range of both G protein-coupled receptors (GPCRs) and non-GPCR substrates that participate in or regulate many critical cellular processes. GRK2 dysfunction is associated with multiple diseases, including cancers, brain diseases, cardiovascular and metabolic diseases, and therefore GRK2-specific substrates/inhibitors are needed not only for studies of GRK2-mediated cellular functions but also for GRK2-targeted drug development. Here, we first review the structure, regulation and functions of GRK2, and its synthetic substrates and inhibitors. Read More

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http://dx.doi.org/10.1007/s00726-020-02864-xDOI Listing

Antibody-Drug Conjugates and Targeted Treatment Strategies for Hepatocellular Carcinoma: A Drug-Delivery Perspective.

Molecules 2020 Jun 21;25(12). Epub 2020 Jun 21.

Department of Pharmacy, Division of Biopharmaceutics, Uppsala University, 752 36 Uppsala, Sweden.

Increased understanding of cancer biology, pharmacology and drug delivery has provided a new framework for drug discovery and product development that relies on the unique expression of specific macromolecules (i.e., antigens) on the surface of tumour cells. Read More

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http://dx.doi.org/10.3390/molecules25122861DOI Listing

Application of the Gastrointestinal Simulator (GIS) Coupled with In Silico Modeling to Measure the Impact of Coca-Cola on the Luminal and Systemic Behavior of Loratadine (BCS Class 2b).

Pharmaceutics 2020 Jun 18;12(6). Epub 2020 Jun 18.

Department of Pharmaceutical Sciences, College of Pharmacy, University of Michigan, Ann Arbor, MI 48109-1065, USA.

In the present work, we explored if Coca-Cola had a beneficial impact on the systemic outcome of the weakly basic drug loratadine (Wal-itin, immediate-release formulation, 10 mg, generic drug product). To map the contribution of underlying physiological variables that may positively impact the intestinal absorption of loratadine, a multi-compartmental and dynamic dissolution device was built, namely the Gastrointestinal Simulator (GIS). The luminal behavior of one immediate-release (IR) tablet of 10 mg of loratadine was tested under four different fasted state test conditions in the GIS: (i) with 250 mL of water and applying a predetermined gastric half-life (t) of 15 min; (ii) with 250 mL of water and applying a t of 30 min; (iii) with 250 mL of Coca-Cola and a t of 15 min; (iv) with 250 mL of Coca-Cola and a t of 30 min. Read More

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http://dx.doi.org/10.3390/pharmaceutics12060566DOI Listing

Genotype as a Potential Pharmacodynamic Biomarker for Tacrolimus Therapy in Ulcerative Colitis in Japanese Patients.

Int J Mol Sci 2020 Jun 18;21(12). Epub 2020 Jun 18.

Department of Clinical Pharmacology and Therapeutics, Kyoto University Hospital, 54 Kawaharacho, Shogoin, Sakyo-ku, Kyoto 606-8507, Japan.

Tacrolimus has been used to induce remission in patients with steroid-refractory ulcerative colitis. It poses a problem of large individual differences in dosage necessary to attain target blood concentration and, often, this leads to drug inefficacy. We examined the difference in mRNA expression levels of ATP binding cassette transporter B1 (ABCB1) between inflamed and non-inflamed tissues, and the influence of genotype on tacrolimus therapy. Read More

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http://dx.doi.org/10.3390/ijms21124347DOI Listing

Enantioselective LC-MS/MS method for the determination of cloperastine enantiomers in rat plasma and its pharmacokinetic application.

Chirality 2020 Aug 22;32(8):1129-1138. Epub 2020 Jun 22.

Department School of Pharmacy, Institution Shenyang Pharmaceutical University, Shenyang, China.

Cloperastine is a central antitussive used to reduce the frequency and intensity of coughing on a short-term basis. In this study, a reliable chiral LC-MS/MS technology has been developed for the quantification of cloperastine enantiomers in the rat plasma. Carbinoxamine was selected as the internal standard. Read More

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http://dx.doi.org/10.1002/chir.23257DOI Listing

Isolation, structure elucidation and neuroprotective effects of caffeoylquinic acid derivatives from the roots of Arctium lappa L.

Phytochemistry 2020 Jun 17;177:112432. Epub 2020 Jun 17.

Department of Pharmacy, General Hospital of Northern Theater Command, Shenyang, 110840, People's Republic of China. Electronic address:

Five undescribed caffeoylquinic acid derivatives (CQAs), along with fifteen known CQAs, were isolated from the roots of Arctium lappa L.(burdock). The chemical structures of compounds were determined using extensive spectroscopic analyses, including UV, IR, NMR and MS. Read More

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http://dx.doi.org/10.1016/j.phytochem.2020.112432DOI Listing

Cross-linking of poly (vinyl alcohol) films under acidic and thermal stress.

Eur J Pharm Sci 2020 Jun 17;152:105429. Epub 2020 Jun 17.

Analytical Research and Development, Biocon Bristol Myers Squibb R&D Centre (BBRC), Bristol-Myers Squibb India Pvt Ltd., Bangalore 560099, India. Electronic address:

Poly (vinyl alcohol), PVA, a commonly used excipient to coat tablets, forms insoluble films in the presence of acids and thermal stress. This may lead to drug products failing to meet dissolution specifications over time. Studies were conducted to understand the effect of acid strength, processing conditions, and storage stress on the mechanism of insoluble film formation using PVA and Opadry II as model systems. Read More

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http://dx.doi.org/10.1016/j.ejps.2020.105429DOI Listing

Blood retention and antigenicity of polycarboxybetaine-modified liposomes.

Int J Pharm 2020 Jun 17;586:119521. Epub 2020 Jun 17.

Graduate School of Systems Life Sciences, Kyushu University, 744 Motooka, Nishi-ku, Fukuoka 819-0395, Japan; Department of Applied Chemistry, Faculty of Engineering, Kyushu University, 744 Motooka, Nishi-ku, Fukuoka 819-0395, Japan; Center for Future Chemistry, Kyushu University, 744 Motooka, Nishi-ku, Fukuoka 819-0395, Japan; International Research Center for Molecular Systems, Kyushu University, 744 Motooka, Nishi-ku, Fukuoka 819-0395, Japan; Centre for Advanced Medicine Innovation, Kyushu University, 3-1-1 Maidashi, Higashi-ku, Fukuoka 812-8582, Japan; Department of Biomedical Engineering, Chung Yuan Christian University, 200 Chung Pei Rd, Chung Li 32023, Taiwan, ROC. Electronic address:

Zwitterionic polycarboxybetaines (PCBs) have gained attention as alternative stealth polymers whose liposomal formulation and protein conjugates were reported not to elicit anti-polymer antibodies. Here, we studied the blood retention and antigenicity of liposomes modified with PCBs focusing on their chemical structures and doses. We compared PCBs with either 1 or 3 (PCB1 or PCB3) spacer carbons between the carboxylate and ammonium groups. Read More

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http://dx.doi.org/10.1016/j.ijpharm.2020.119521DOI Listing

Tumor Suppressors-HTRA Proteases and Interleukin-12-in Pediatric Asthma and Allergic Rhinitis Patients.

Medicina (Kaunas) 2020 Jun 17;56(6). Epub 2020 Jun 17.

Department of General and Medical Biochemistry, University of Gdańsk, Wita Stwosza 59 80-308 Gdańsk, Poland.

: Allergy belongs to a group of mast cell-related disorders and is one of the most common diseases of childhood. It was shown that asthma and allergic rhinitis diminish the risk of various cancers, including colon cancer and acute lymphoblastic leukemia. On the other hand, asthma augments the risk of lung cancer and an increased risk of breast cancer in patients with allergy has been observed. Read More

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http://dx.doi.org/10.3390/medicina56060298DOI Listing

Oral Microbiota and Immune System Crosstalk: A Translational Research.

Biology (Basel) 2020 Jun 16;9(6). Epub 2020 Jun 16.

Department of Interdisciplinary Medicine, University of Bari "Aldo Moro", 70121 Bari, Italy.

Background: Oral pathogens may exert the ability to trigger differently the activation of local macrophage immune responses, for instance and induce predominantly pro-inflammatory (M1-like phenotypes) responses, while oral commensal microbiota primarily elicits macrophage functions consistent with the anti-inflammatory (M2-like phenotypes).

Methods: In healthy individuals vs. periodontal disease patients' blood samples, the differentiation process from monocyte to M1 and M2 was conducted using two typical growth factors, the granulocyte/macrophage colony stimulating factor (GM-CSF) and the macrophage colony stimulating factor (M-CSF). Read More

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http://dx.doi.org/10.3390/biology9060131DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC7344575PMC