Article
Pharmacology & Pharmacy
Sharareh Senemar, Benjamin A. Kuzma, Tannaz Ramezanli, Priyanka Ghosh, Sam G. Raney, Elena Rantou, Grazia Stagni
Summary: Comparative assessment of cutaneous pharmacokinetics (cPK) by dermal microdialysis (dMD) is a suitable method to evaluate the bioequivalence (BE) of topical dermatological drug products applied to the skin (TDDPs). However, previous literature studies have reported inconclusive BE assessments. In this study, we addressed methodological deficiencies and demonstrated the potential of dMD as a tool to assess BE for TDDPs.
Article
Pharmacology & Pharmacy
Benjamin A. Kuzma, Sharareh Senemar, Tannaz Ramezanli, Priyanka Ghosh, Sam G. Raney, Grazia Stagni
Summary: Dermal microdialysis (dMD) can accurately measure the availability of a topically administered active pharmaceutical ingredient (API) in the dermis. The study aimed to assess the dMD methodology in terms of sensitivity, discriminative ability, and reproducibility, showing that it is selective, sensitive, and stable over a 48-hour period.
EUROPEAN JOURNAL OF PHARMACEUTICAL SCIENCES
(2021)
Article
Pharmacology & Pharmacy
Fotis Iliopoulos, Chun Fung Tang, Ziyue Li, Annisa Rahma, Majella E. Lane
Summary: The evaluation of bioequivalence (BE) for topical dermatological drug products is challenging, and the aim of this study was to evaluate the use of Confocal Raman Spectroscopy (CRS) for BE assessment. Two commercially available formulations were found to deliver similar amounts of drug across the skin in vitro and resulted in comparable skin uptake values in vivo. This is the first study to demonstrate the capability of CRS for the evaluation of BE for topical products.
Article
Pharmacology & Pharmacy
Benjamin A. Kuzma, Sharareh Senemar, Tannaz Ramezanli, Priyanka Ghosh, Sam G. Raney, Grazia Stagni
Summary: This study investigates the effect of dose-duration on dermal exposure of metronidazole-containing drug products and characterizes metronidazole dermal elimination using a retrodialysis/microdialysis approach. The results suggest that truncating dose-duration can reduce experimental duration, but careful selection of dose-duration is necessary to discriminate between formulations.
EUROPEAN JOURNAL OF PHARMACEUTICS AND BIOPHARMACEUTICS
(2022)
Article
Infectious Diseases
Yasmeen Abouelhassan, Andrew J. Fratoni, Ashley K. Shepard, David P. Nicolau, Tomefa E. Asempa
Summary: This study assessed the pharmacokinetics of tebipenem in healthy subjects and patients with diabetic foot infection, and found that tebipenem demonstrated excellent distribution into skin and soft tissue.
JOURNAL OF ANTIMICROBIAL CHEMOTHERAPY
(2023)
Review
Pharmacology & Pharmacy
Thomas Birngruber, Katrin I. I. Tiffner, Selma I. I. Mautner, Frank M. M. Sinner
Summary: Topically applied drug products in the US have seen significant price increases due to a lack of generic options. Generic drug development is limited by high costs and risks associated with proving bioequivalence. Cutaneous PK-based studies offer a cost-effective alternative to clinical endpoint studies.
FRONTIERS IN PHARMACOLOGY
(2022)
Article
Instruments & Instrumentation
Chin-Ping Kung, Bruno C. Sil, Yanling Zhang, Jonathan Hadgraft, Majella E. Lane, Bhumik Patel, Renee McCulloch
Summary: Amitriptyline, currently used for neuropathic pain and migraine, is being explored as a potential topical analgesic. Initial studies suggest that formulations containing isopropyl myristate (IPM) and isopropyl alcohol (IPA) promote higher permeation of amitriptyline through the skin, while those containing propylene glycol (PG) also show promise for dermal delivery. Further optimization is needed for clinical investigational studies.
DRUG DELIVERY AND TRANSLATIONAL RESEARCH
(2022)
Article
Chemistry, Medicinal
Qiuying Li, Lihui Jia, Wenli Hu, Shu Dong, Chaohong Cai
Summary: The study evaluated the bioequivalence and safety of two formulations of 25 mg tenofovir alafenamide tablets in Chinese healthy male and female subjects under fed and fasting conditions. The results showed that both formulations met the bioequivalence acceptance criteria and were well tolerated by the subjects, demonstrating bioequivalence in pharmacokinetic parameters under different feeding conditions.
DRUG DESIGN DEVELOPMENT AND THERAPY
(2021)
Article
Pharmacology & Pharmacy
Onursal Saglam, Berrak Guney, Nihal Saraner, Gamze Sevici, Emel Dogan-Kurtoglu, Merve G. Ulusoy, Gokce Demiray, Muradiye Nacak, Aydin Erenmemisoglu, Mahmut Ozbek, Peri Aytac
Summary: This study aimed to demonstrate the bioequivalence of a new favipiravir tablet formulation compared to the reference tablet formulation in healthy male subjects under fasting conditions. The results showed that the test and reference favipiravir products met the required bioequivalence criteria, and both products were well tolerated and safe.
INTERNATIONAL JOURNAL OF CLINICAL PHARMACOLOGY AND THERAPEUTICS
(2021)
Article
Chemistry, Analytical
Bianca-Maria Tuchiu, Raluca-Ioana Stefan-van Staden, Marius Badulescu, Jacobus Frederick van Staden
Summary: Three disposable stochastic sensors based on maltodextrin and nanostructures were proposed for the analysis of ibuprofen, ketoprofen, and flurbiprofen. The sensors demonstrated wide linear concentration ranges and low detection limits.
JOURNAL OF PHARMACEUTICAL AND BIOMEDICAL ANALYSIS
(2022)
Article
Pharmacology & Pharmacy
Marcelo Gomes Davanco, Jessica Meulman, Thalita Martins da Silva, Fernando Costa, Karini Bruno Bellorio, Iram Moreira Mundim, Ana Carolina Costa Sampaio, Leonardo de Souza Teixeira, Celso Francisco Pimentel Vespasiano
Summary: This study aimed to evaluate the bioequivalence between two methylphenidate extended-release tablets and found that the test formulation was considered bioequivalent to the reference formulation in both fasting and fed conditions. Both formulations were safe and well tolerated.
Article
Medicine, Research & Experimental
S. G. Pragathi, Anusha Echanur, Anusha Matadh, Srinath Rangappa, H. N. Shivakumar, Reena N. Murthy, V. S. Ranganath, Esteban E. Urena-Benavides, Howard Maibach, S. Narasimha Murthy
Summary: The objective of this study was to investigate the possibility of active pharmaceutical ingredients (APIs) to undergo sublimation after solvent evaporation from topical application. Different topical formulations containing APIs were tested for sublimation, and it was found that the extent of sublimation varied among the selected products. Salicylic acid, one of the APIs, experienced significant loss due to sublimation, which was more pronounced at skin temperature compared to room temperature. Furthermore, the formulation composition had a significant impact on the extent of sublimation, particularly for salicylic acid. The sublimation of APIs from the topical product affected the mass balance studies conducted on the salicylic acid ointment. Additionally, human studies yielded results consistent with the in vitro experiments, confirming the plausibility of API loss through sublimation at the site of application.
MOLECULAR PHARMACEUTICS
(2023)
Article
Chemistry, Multidisciplinary
Muhammad Yasir Siddique, Muhammad Faizan Nazar, Marryam Mahmood, Muhammad Atif Saleem, Norah Alwadai, Amani Saleh Almuslem, Fwzah H. Alshammari, Sajjad Haider, Muhammad Saeed Akhtar, Syed Zajif Hussain, Muhammad Safdar, Muhammad Akhlaq
Summary: Microemulsified gels (mu EGs) have unique functions and are essential for topical drug delivery systems due to their high stability and flexibility in manufacturing. New formulations using biocompatible ingredients have been developed to encapsulate and control the release of an antimycotic drug, resulting in improved transdermal therapeutic efficacy.
Review
Pharmacology & Pharmacy
Ines Garcia Del Valle, Carmen Alvarez-Lorenzo
Summary: Atropine, an old-known drug, has gained increasing attention for its therapeutic effects on eye structures. When administered topically, attention should be paid to atropine ocular pharmacokinetics and its ability to access the posterior segment. There is an urgent need to design formulations that can selectively deliver atropine to the target tissue for each specific application.
EXPERT OPINION ON DRUG DELIVERY
(2021)
Article
Pharmacology & Pharmacy
Maria Natalia Calienni, Luis Manuel Martinez, Maria Cecilia Izquierdo, Silvia del Valle Alonso, Jorge Montanari
Summary: This study assessed the rheological and viscoelastic properties of hybrid formulations loaded with ultradeformable liposomes (UDL). The formulations exhibited non-Newtonian behavior with pseudoplastic traits, and the incorporation of UDL induced rheological changes. Frequency sweep tests showed predominantly elastic solid behavior at different temperatures and post-production times.
Article
Pharmacology & Pharmacy
Roger K. Verbeeck, Sophie De Niet, Sonia Lebrun, Mickael Tremege, Tim W. Rennie, Monte Coffiner, Bruno Streel, Bernard Cahay
JOURNAL OF PHARMACY AND PHARMACEUTICAL SCIENCES
(2015)
Letter
Immunology
Jan-Willem C. Alffenaar, Simon Tiberi, Roger K. Verbeeck, Scott K. Heysell, Martin P. Grobusch
CLINICAL INFECTIOUS DISEASES
(2017)
Review
Pharmacology & Pharmacy
Roger K. Verbeeck, Gunar Guenther, Dan Kibuule, Christian Hunter, Tim W. Rennie
EUROPEAN JOURNAL OF CLINICAL PHARMACOLOGY
(2016)
Editorial Material
Chemistry, Medicinal
Roger K. Verbeeck, Isadore Kanfer, Raimar Lobenberg, Bertil Abrahamsson, Rodrigo Cristofoletti, D. W. Groot, Peter Langguth, James E. Polli, Alan Parr, Vinod P. Shah, Mehul Mehta, Jennifer B. Dressman
JOURNAL OF PHARMACEUTICAL SCIENCES
(2017)
Article
Pharmacology & Pharmacy
Bonifasius S. Singu, Mwangana Mubita, Moses M. Thikukutu, Josef K. Mufenda, Shonag B. McKenzie, Roger K. Verbeeck
INTERNATIONAL JOURNAL OF CLINICAL PHARMACY
(2018)
Article
Pharmacology & Pharmacy
Klintean Wunnapuk, Fahim Mohammed, Indika Gawarammana, Xin Liu, Roger K. Verbeeck, Nicholas A. Buckley, Michael S. Roberts, Flora T. Musuamba
BRITISH JOURNAL OF CLINICAL PHARMACOLOGY
(2014)
Article
Respiratory System
Dan Kibuule, Roger K. Verbeeck, Ruswa Nunurai, Farai Mavhunga, Ette Ene, Brian Godman, Timothy W. Rennie
EXPERT REVIEW OF RESPIRATORY MEDICINE
(2018)
Article
Infectious Diseases
D. Kibuule, T. W. Rennie, N. Ruswa, F. Mavhunga, A. Thomas, R. Amutenya, M. R. Law, G. Gunther, E. Ette, B. Godman, R. K. Verbeeck
INTERNATIONAL JOURNAL OF TUBERCULOSIS AND LUNG DISEASE
(2019)
Editorial Material
Pharmacology & Pharmacy
Roger K. Verbeeck, Bonifasius S. Singu, Dan Kibuule
CLINICAL PHARMACOKINETICS
(2019)
Article
Medicine, Research & Experimental
Bonifasius S. Singu, Helen Morrison, Lydia Irengeya, Roger K. Verbeeck
Summary: This retrospective study found that monitoring unbound plasma concentrations of phenytoin and valproic acid may provide a more accurate assessment of drug levels compared to total plasma drug concentrations. The majority of patients had unbound plasma concentrations of phenytoin or valproic acid outside the therapeutic range, highlighting the limitations of using total drug concentrations for dose optimization.
AFRICAN JOURNAL OF LABORATORY MEDICINE
(2022)
Article
Pediatrics
Bonifasius Siyuka Singu, Milka Ndapandula Ndeunyema, Ene I. Ette, Clarissa Hildegard Pieper, Roger Karel Verbeeck
Summary: This study aimed to determine the maximum and minimum plasma concentrations of gentamicin and amikacin in neonates, and assess their glomerular filtration rate (eGFR). The results showed that only a minority of neonates reached the therapeutic range of these drugs, but the majority were able to clear the drugs to below the toxicity threshold within 24 hours. Although amikacin led to a decrease in eGFR, most neonates were still able to clear the drug within the dosing interval.
Article
Pharmacology & Pharmacy
Boni Singu, Roger K. Verbeeck
Summary: Codeine is widely used as an analgesic, antitussive, and antidiarrhoeal agent, but its analgesic effect varies greatly due to biotransformation to morphine by CYP2D6. Clinical trials have shown that codeine alone is the least effective in acute postoperative pain, and there is limited evidence to support its use as an antitussive. Additionally, codeine use can potentially lead to abuse and dependence, prompting the WHO to consider removing it from the list of essential medicines for adults.
JOURNAL OF PHARMACY AND PHARMACEUTICAL SCIENCES
(2021)
Article
Respiratory System
Dan Kibuule, Philomein Aiases, Nunurai Ruswa, Timothy William Rennie, Roger K. Verbeeck, Brian Godman, Mwangana Mubita
Article
Pharmacology & Pharmacy
Lauren J. Jonkman, Marvelous P. Gwanyanya, Monika N. Kakololo, Roger K. Verbeeck, Bonifasius S. Singu
DRUGS & THERAPY PERSPECTIVES
(2019)
Article
Medical Laboratory Technology
Flora T. Musuamba, Vanessa Guy-Viterbo, Raymond Reding, Roger K. Verbeeck, Pierre Wallemacq
THERAPEUTIC DRUG MONITORING
(2014)
Article
Pharmacology & Pharmacy
Xuezhi Zhuo, Vito Fodera, Per Larsson, Zarah Schaal, Christel A. S. Bergstrom, Korbinian Lobmann, Aleksei Kabedev
Summary: Our previous work demonstrated that beta-lactoglobulin-stabilized amorphous solid dispersion (ASD) loaded with 70 % indomethacin remains stable for over 12 months. We further investigated the stabilization mechanisms by testing five other drug molecules and using experimental techniques and molecular dynamics simulations. The results showed that steric confinement, hydrogen bonding, and the glass transition temperature of the drug molecule play important roles in stabilizing ASDs with high drug loadings.
EUROPEAN JOURNAL OF PHARMACEUTICAL SCIENCES
(2024)
Article
Pharmacology & Pharmacy
Sebastian Schmidt, Ulrike Holzgrabe
Summary: The binding of drugs to plasma proteins, such as human serum albumin (HSA), is crucial for determining pharmacokinetic parameters. This study investigated the enantioselective binding of S- and R-ketamine to HSA. It was found that ketamine has weak affinity to HSA, with no significant differences in binding behavior between the individual enantiomers and the racemate. The aromatic ring and N-methyl group were identified as the most strongly involved structural moieties in the binding of ketamine to HSA.
EUROPEAN JOURNAL OF PHARMACEUTICAL SCIENCES
(2024)
Article
Pharmacology & Pharmacy
Yuchen Zhao, Han Wang, Lin Jin, Ziwei Zhang, Lianghu Liu, Mengqi Zhou, Xianzheng Zhang, Lingling Zhang
Summary: Interleukins (ILs) are important for communication between immune cells and non-immune cells, but dysregulation of ILs expression is a characteristic of autoinflammatory diseases. Drugs targeting ILs have significant clinical benefits, but may also cause adverse reactions. Fusion protein technology, with its ability to enhance therapeutic efficacy, has been explored for developing anti-inflammatory drugs. This review discusses the efficacy of fusion protein drugs developed with ILs or their receptors in treating autoinflammatory diseases, highlighting the potential of this technology in future anti-inflammatory drug development.
EUROPEAN JOURNAL OF PHARMACEUTICAL SCIENCES
(2024)
Article
Pharmacology & Pharmacy
Serena Bertoni, Elena Simone, Stefano Sangiorgi, Beatrice Albertini, Nadia Passerini
Summary: This study investigated the correlation between the structure and release properties of solid lipid microparticles (MPs) with different liquid additives. The additives accelerated the conversion of the unstable alpha-form of tristearin to the stable beta-polymorph and caused structural modifications in the MPs. The presence of additives prolonged the drug release in water and resulted in higher release profiles in biorelevant media. The findings suggest that the release behavior can be influenced by the polymorphism and supramolecular-level structural modification of lipid formulations containing crystal modifiers.
EUROPEAN JOURNAL OF PHARMACEUTICAL SCIENCES
(2024)
Article
Pharmacology & Pharmacy
Juulia Jarvinen, Ahmed B. Montaser, Santosh Kumar Adla, Jukka Leppanen, Marko Lehtonen, Kati-Sisko Vellonen, Tuomo Laitinen, Aaro Jalkanen, William F. Elmquist, Juri Timonen, Kristiina M. Huttunen, Jarkko Rautio
Summary: This study attempted to alter the brain distribution pattern of Palbociclib by creating and assessing two novel prodrugs. Although the prodrug design did not significantly improve Palbociclib brain delivery, the study provides valuable insights for future prodrug development and drug delivery strategies targeting specific transporters.
EUROPEAN JOURNAL OF PHARMACEUTICAL SCIENCES
(2024)
Review
Pharmacology & Pharmacy
Miao Wang, Xinyu Ma, Shiyu Zong, Yaqiong Su, Rui Su, Hong Zhang, Yang Liu, Chunliu Wang, Ye Li
Summary: This article discusses the potential and limitations of nasal administration in central nervous system drug delivery. Nasal gel viscosity can alleviate the impact of nasal mucociliary clearance on drug delivery, and materials such as gellan gum, chitosan, carbomer, cellulose, and poloxamer can be used to prepare nasal gels.
EUROPEAN JOURNAL OF PHARMACEUTICAL SCIENCES
(2024)
Article
Pharmacology & Pharmacy
Bjarke Strom Larsen, Eric Kissi, Liebert Parreiras Nogueira, Natalja Genina, Ingunn Tho
Summary: This study investigates the influence of drug load and polymer molecular weight on the structure of 3D printed tablets. The results show that drug load and polymer molecular weight have a significant impact on the porosity and size of the tablets, while the effect of drug load on the total porosity of the tablets is minimal.
EUROPEAN JOURNAL OF PHARMACEUTICAL SCIENCES
(2024)
Article
Pharmacology & Pharmacy
Zhentao Qiao, Fuhang Wang, Dongjian Han, Yuansong Zhuang, Qingjiao Jiang, Yi Zhang, Miaomiao Liu, Quanxu An, Zhiwei Wang, Deliang Shen
Summary: In this study, it was demonstrated that periadventitial delivery of rapamycin-fibrin glue (RPM-FG) can inhibit intimal hyperplasia (IH) in a rat carotid artery injury model without compromising re-endothelialization. This provides a promising direction for the future development of a safe, effective, and minimally invasive perivascular drug delivery method to treat vascular disease.
EUROPEAN JOURNAL OF PHARMACEUTICAL SCIENCES
(2024)
Article
Pharmacology & Pharmacy
Neele Puhlmann, Rodrigo Vidaurre, Klaus Kuemmerer
Summary: Active pharmaceutical ingredients and their metabolites and transformation products are pollutants that can harm human and environmental health. Designing greener APIs is an effective strategy to address this issue. The drug discovery and development process can incorporate environmental parameters to achieve this design, and this process is highly flexible.
EUROPEAN JOURNAL OF PHARMACEUTICAL SCIENCES
(2024)