Article
Pharmacology & Pharmacy
Suchiwa Pan-On, Waree Tiyaboonchai
Summary: Curcumin solid dispersion (CSD) developed using PVP as a carrier and soybean phospholipids as a co-carrier was found to have good physicochemical properties and in vitro permeability, significantly increased water solubility and enhanced curcumin absorption. The CSD showed quick and complete dissolution and stable physical and chemical properties for up to 6 months at 4 degrees C and room temperature.
JOURNAL OF DRUG DELIVERY SCIENCE AND TECHNOLOGY
(2023)
Article
Food Science & Technology
Jerome Henri, Rachelle Lanceleur, Jean-Michel Delmas, Valerie Fessard, Antoine Huguet
Summary: Microcystins are toxins produced by cyanobacteria globally, with variations in their structure affecting toxicity. Research indicates that oral absorption of Microcystin-RR may be poor, despite its common structure with more toxic variants like Microcystin-LR.
Article
Chemistry, Physical
Karen Saiswani, Aditya Narvekar, Devashree Jahagirdar, Ratnesh Jain, Prajakta Dandekar
Summary: This study investigates the enhancement in intestinal absorption of daptomycin using a new class of permeation enhancers, deep eutectic solvents (DESs), in comparison with sodium caprate. Both DESs and sodium caprate enhance the permeation of daptomycin by reducing the expression of cell junction proteins, leading to the loosening of tight junctions.
JOURNAL OF MOLECULAR LIQUIDS
(2023)
Article
Pharmacology & Pharmacy
Lena Ritters, Yuanyuan Tian, Stephan Reichl
Summary: Formulating APIs in ASDs is a promising approach to improve bioavailability of poorly soluble compounds, but challenges such as compressibility and recrystallization may arise during tablet production. The study investigated the influence of different types of PVP on the stability of ASD powders, with varying PCM contents leading to recrystallization. PVP/VA copolymer was found to be the most unstable, resulting in slow drug release from the ASD tablets.
Article
Nutrition & Dietetics
Agnes Klusoczki, Boglarka Olah, Dominik Hosszu, Ferenc Fenyvesi, Judit Remenyik, Judit Homoki, Alexandra Gyongyosi, Ildiko Bacskay, Judit Varadi
Summary: This study aimed to investigate the interaction between anthocyanins and gliadin and the impact of anthocyanins on barrier modulation in Caco-2 cells. The results showed that anthocyanins were able to reduce the release of cytokines and mitochondrial ROS levels, exhibiting anti-inflammatory, stabilizing, and restoring effects.
Article
Pharmacology & Pharmacy
Yi Cheng, Chie Watanabe, Yusuke Ando, Satoshi Kitaoka, Yuya Egawa, Tomoya Takashima, Akihiro Matsumoto, Masahiro Murakami
Summary: In this study, researchers developed a partially laminated cell culture model to simulate the mucus layer in the human intestines. Compared to traditional coculture models, this partially laminated model maintained a higher barrier function and adjustable permeability according to the cell ratio. This novel model may have potential applications in vitro for evaluating intestinal mucosal permeability and drug efficacy.
Article
Multidisciplinary Sciences
Yu Takahashi, Makoto Noguchi, Yu Inoue, Shintaro Sato, Makoto Shimizu, Hirotatsu Kojima, Takayoshi Okabe, Hiroshi Kiyono, Yoshio Yamauchi, Ryuichiro Sato
Summary: This study demonstrates that organoid-derived intestinal epithelial cells possess similar physiological properties as intestinal epithelium and can be used as tools to enhance the prediction of biological activity in humans.
Article
Medicine, General & Internal
Katie Morgan, Steven D. Morley, Arslan K. Raja, Martin Vandeputte, Kay Samuel, Martin Waterfall, Natalie Z. M. Homer, Peter C. Hayes, Jonathan A. Fallowfield, John N. Plevris
Summary: The gut-liver axis refers to the communication between the gut, microbiome, and liver, which can be overactivated and cause liver injury. In this study, the effects of paracetamol (APAP) on intestinal and hepatic cells were investigated. The results showed that APAP did not affect the viability of intestinal cells, but increased the tightness of the intestinal epithelium. Metabolism of APAP by intestinal cells resulted in a reduced amount of intact APAP transferred to hepatic cells, which showed no loss of viability or membrane integrity when exposed to conditioned medium from intestinal cells. These findings suggest that pre-metabolism of APAP may protect hepatic tight junctions from direct exposure to APAP.
JOURNAL OF CLINICAL MEDICINE
(2023)
Article
Pharmacology & Pharmacy
Gabriela Falcon-Cano, Christophe Molina, Miguel Angel Cabrera-Perez
Summary: The study developed a QSPR approach on the KNIME platform using a structurally diverse dataset of over 4900 molecules, obtaining interpretable models with random forest algorithms. Conditional consensus models based on regional and global regression random forest were developed, showing potential applicability in predicting drug permeability and BDDCS class. An automated workflow for predicting new drugs was also created, showcasing its reliability in identifying promising compounds during early drug discovery stages.
Article
Pharmacology & Pharmacy
Lena Ritters, Stephan Reichl
Summary: Amorphous solid dispersions (ASDs) composed of paracetamol (PCM) and polyvinylpyrrolidone/vinyl acetate (PVP/VA) were evaluated for their saturation solubility, dissolution behavior, and transepithelial in vitro permeability of PCM. With increasing amounts of PVP/VA, the water solubility of ASDs containing PCM increased significantly. The phase separation of preparations with 30% PCM in water was attributed to the thermoresponsive behavior of PVP/VA. The permeation behavior of PCM from these phase-separated preparations and their effect on cell viability were also studied.
INTERNATIONAL JOURNAL OF PHARMACEUTICS
(2023)
Review
Pharmacology & Pharmacy
Marta Kus, Izabela Ibragimow, Hanna Piotrowska-Kempisty
Summary: This study aims to review the conditions for permeability studies across the Caco-2 monolayer reported in the available literature concerning validation guidelines. By summarizing the main aspects affecting the validation process, we can provide useful information for preparing the cell line and further permeability research.
Article
Nutrition & Dietetics
Ikuya Shirai, Koji Karasawa, Yusuke Kodaira, Yu Iwasaki, Yasutaka Shigemura, Hidefumi Makabe, Shigeru Katayama
Summary: This study evaluated the permeation of agaro-oligosaccharides (AOSs) in the gastrointestinal tract both in vivo and in vitro. The results showed that AOSs can be absorbed through the paracellular pathway between intestinal epithelial cells.
FRONTIERS IN NUTRITION
(2022)
Article
Pharmacology & Pharmacy
Cristiana L. Pires, Catarina Praca, Patricia A. T. Martins, Ana L. M. Batista de Carvalho, Lino Ferreira, Maria Paula M. Marques, Maria Joao Moreno
Summary: The study characterized variations in the tightness of Caco-2 cell monolayers over time and assessed their suitability for reuse in permeability assays. Results showed that manipulation during assays may affect permeability measurements, leading to P-app values dependent on sampling duration. The study also demonstrated that after incubation with culture media for two days, the cell monolayers can be reused, tripling the throughput of the assay on days 22, 25, and 28.
Article
Pharmacology & Pharmacy
Nimishraj Panse, Phillip M. Gerk
Summary: The Caco-2 cell model is widely used to assess drug permeability, providing a reliable estimation of oral drug permeability.
INTERNATIONAL JOURNAL OF PHARMACEUTICS
(2022)
Article
Pharmacology & Pharmacy
Tugba Gulsun, Nihan Izat, Selma Sahin
Summary: This study aimed to evaluate the effects of permeability enhancers on the permeability of furosemide and metformin hydrochloride. The results showed that permeability enhancers had no significant effect on the permeability of furosemide, but significantly increased the permeability of metformin. Combining chitosan and sodium lauryl sulfate, as well as other combinations, also significantly improved the permeability of metformin. Therefore, permeability enhancers could be used in the formulation development strategies of furosemide and metformin by the pharmaceutical industry.
CANADIAN JOURNAL OF PHYSIOLOGY AND PHARMACOLOGY
(2023)
Article
Immunology
Giulia Anderluzzi, Gustavo Lou, Simona Gallorini, Michela Brazzoli, Russell Johnson, Derek T. O'Hagan, Barbara C. Baudner, Yvonne Perrie
Article
Pharmacology & Pharmacy
Carla B. Roces, Emily Charlotte Port, Nikolaos N. Daskalakis, Julia A. Watts, Jonathan W. Aylott, Gavin W. Halbert, Yvonne Perrie
INTERNATIONAL JOURNAL OF PHARMACEUTICS
(2020)
Article
Chemistry, Medicinal
Thomas J. Dennison, Julian C. Smith, Raj K. S. Badhan, Afzal R. Mohammed
JOURNAL OF PHARMACEUTICAL SCIENCES
(2020)
Article
Pharmacology & Pharmacy
Swapnil Khadke, Carla B. Roces, Rachel Donaghey, Valeria Giacobbo, Yang Su, Yvonne Perrie
JOURNAL OF PHARMACY AND PHARMACOLOGY
(2020)
Review
Infectious Diseases
Muhammad Idrees, Afzal R. Mohammad, Nazira Karodia, Ayesha Rahman
Article
Pharmacology & Pharmacy
Craig Russell, Majad Hussain, David Huen, Ayesha S. Rahman, Afzal R. Mohammed
Summary: This study explores the use of DNA microarrays as a high throughput screening tool to identify markers for predicting bioavailability and formulation-driven physiological responses. Significant changes in gene expression were found as a result of formulation exposure, including genes related to drug transport and metabolism.
PHARMACEUTICAL DEVELOPMENT AND TECHNOLOGY
(2021)
Article
Pharmacology & Pharmacy
Signe Tandrup Schmidt, Dennis Christensen, Yvonne Perrie
Article
Multidisciplinary Sciences
Annsar Ahmad Warraich, Afzal Ur Rahman Mohammed, Hazel Gibson, Majad Hussain, Ayesha Sabah Rahman
Summary: Antimicrobial resistance is a global threat to public health. Amino acids may serve as antimicrobial adjuvants using alternate mechanisms to combat resistance, inhibiting bacterial growth and reducing the production of toxic pigments.
Article
Pharmacology & Pharmacy
Abdul Latif Ershad, Ali Rajabi-Siahboomi, Shahrzad Missaghi, Daniel Kirby, Afzal Rahman Mohammed
Summary: This study developed a fast, cost-effective, and repeatable swallowability ranking method to screen the in vitro swallowability of solid oral medicines, aiming to assist formulators and the pharmaceutical industry in developing easy-to-swallow formulations.
Article
Cell Biology
Habtom Ftuwi, Rheinallt Parri, Afzal R. Mohammed
Summary: This study developed a comprehensive method to fully characterize long-term cultured bovine taste bud cells, showing that these cells express taste receptor genes and can respond to taste stimuli such as denatonium and quinine. Gene expression analysis and bioinformatics research revealed that some genes in bovine taste bud cells have higher similarity to human counterparts, offering a cell-based system to study human taste transduction and potentially replace animal experimentation.
Article
Pharmacology & Pharmacy
Dilawar Khan, Daniel Kirby, Simon Bryson, Maryam Shah, Afzal Rahman Mohammed
Summary: Due to anatomical and physiological differences between pediatric subsets, it is well established that children respond differently to drugs compared to adults. Orally disintegrating mini-tablets have been considered an age-appropriate formulation option for pediatric use due to their dose flexibility and superior stability.
Article
Pharmacology & Pharmacy
Dilawar Khan, Daniel Kirby, Simon Bryson, Maryam Shah, Afzal Rahman Mohammed
Summary: This article discusses the factors affecting the safety, toxicity, and efficacy of pediatric drug delivery systems, as well as the anatomical and physiological differences between children and adults. It evaluates the advantages, limitations, and acceptability of current pediatric dosage forms, and explores techniques to overcome barriers associated with non-adherence to pediatric medications.
INTERNATIONAL JOURNAL OF PHARMACEUTICS
(2022)
Review
Biochemistry & Molecular Biology
Olaitan Abiona, David Wyatt, Jasdip Koner, Afzal Mohammed
Summary: This review explores the effects of particle properties on drug-carrier interactions in the preparation of a dry powder inhaler formulation. It is challenging to establish a direct cause-and-effect relationship between carrier properties and DPI formulation performance due to their interactive effects. Alpha lactose monohydrate remains the most commonly used carrier. The role of surface energetics in the optimization of dry powder inhaler formulations is discussed, along with various lactose particle modification methods.
Article
Pharmacology & Pharmacy
Dilawar Khan, Raj Badhan, Daniel J. J. Kirby, Simon Bryson, Maryam Shah, Afzal Rahman Mohammed
Summary: The rapid onset of action of nifedipine can cause a sudden decrease in blood pressure, resulting in adverse effects related to sympathetic nervous system activation. However, there are currently no approved modified release formulations of nifedipine for pediatric use, leading to a lack of pharmacokinetic data in this population. The use of pharmacokinetic modeling, particularly physiological-based pharmacokinetics (PBPK), has revolutionized the ability to predict drug pharmacokinetics in children and support drug licensing and dosing.
Review
Immunology
Kyprianos Michaelides, Maruthi Prasanna, Raj Badhan, Afzal-Ur-Rahman Mohammed, Adam Walters, M. Keith Howard, Pawan Dulal, Ali Al-Khattawi
Summary: Introduction With a limited global supply of vaccines and increasing vaccine hesitancy, improving vaccination coverage is a priority. The review focuses on the development of single administration vaccines (SAVs) and the challenges in their formulation. Case studies on hepatitis B and polio vaccines’ SAV formulations are discussed, along with their development challenges and preclinical data. Expert opinion: Although there have been efforts in SAV development, few have advanced to Phase-I trials. Overcoming commercial and technical barriers may facilitate the progress of SAVs, especially with the renewed global focus on vaccines since the COVID-19 pandemic.
EXPERT REVIEW OF VACCINES
(2023)
Article
Pharmacology & Pharmacy
Greta Camilla Magnano, Marika Quadri, Elisabetta Palazzo, Roberta Lotti, Francesca Loschi, Stefano Dall'Acqua, Michela Abrami, Francesca Larese Filon, Alessandra Marconi, Dritan Hasa
Summary: This study aimed to investigate the loading of sildenafil citrate in three commercial transdermal vehicles using 3D full-thickness skin equivalent and compare the results with permeability experiments using porcine skin. The results showed that the results obtained using the 3D skin equivalent were comparable to those obtained using porcine skin, suggesting that the 3D skin model can be a valid alternative for ex-vivo skin absorption experiments.
INTERNATIONAL JOURNAL OF PHARMACEUTICS
(2024)
Article
Pharmacology & Pharmacy
James W. Mckeage, Andrew Z. H. Tan, Andrew J. Taberner
Summary: Needle-free jet injection is a promising alternative drug delivery technique that offers rapid, non-invasive, and large-volume injections. The study presents a prototype multi-orifice nozzle and a computational fluid dynamic model to demonstrate the feasibility and effectiveness of this technology.
INTERNATIONAL JOURNAL OF PHARMACEUTICS
(2024)