Article
Pharmacology & Pharmacy
Chiara Migone, Letizia Mattii, Martina Giannasi, Stefania Moscato, Andrea Cesari, Ylenia Zambito, Anna Maria Piras
Summary: The study aimed to develop a new vehicle for promoting the oral absorption of the neuropeptide DAL, which can cross both the intestinal mucosal barrier and blood-brain barrier. Results suggest the potential of DAL-NP in transporting a fraction of DAL dose administered orally to the brain, but further in vivo experiments are needed for confirmation.
Article
Pharmacology & Pharmacy
Fiona McCartney, Diego R. Perinelli, Mattia Tiboni, Robert Cavanagh, Simone Lucarini, Giovanni Filippo Palmieri, Luca Casettari, David J. Brayden
Summary: The study compared the performance of three monoesters with varying sugar moieties as intestinal permeation enhancers. Results showed that all three esters enhanced permeability in rat intestinal tissue likely via tight junction modulation, while C12-trehalose was slightly less efficacious but also less damaging to the tissue. All three esters have potential for oral formulations as permeation enhancers.
INTERNATIONAL JOURNAL OF PHARMACEUTICS
(2021)
Article
Pharmacology & Pharmacy
Nikhil Suthar, Jagruti Desai, Hetal Paresh Thakkar
Summary: In this study, Risedronate sodium-loaded chitosan nanoparticles were developed to enhance oral bioavailability and evaluated for various parameters. The nanoparticles showed good flow property, compatibility with excipients, and high in vitro release efficiency. Overall, the developed nanoparticles appear to be a promising approach to improve oral bioavailability and avoid upper GI tract side effects.
Article
Engineering, Electrical & Electronic
Priyanshu Banerjee, Eunhwa Jang, Jiyuan Huang, Rudolph Holley, Sudharshan Vadnala, Adnan Sheikh, Arjun Trivedi, Kendall Jackson, Vincent Kai Homman, Deepa Madan
Summary: This study implemented an environmentally friendly and cost-effective method to enhance the thermoelectric performance of printable thermoelectric composite films. By utilizing specific techniques and materials, the electrical conductivity and power factor of the composite films were improved, resulting in higher thermoelectric performance. The successful demonstration of this approach suggests new possibilities for the fabrication of thermoelectric composite films.
JOURNAL OF ELECTRONIC MATERIALS
(2021)
Article
Engineering, Biomedical
Richard Wibel, Patrick Knoll, Bao Le-Vinh, Gergely Kali, Andreas Bernkop-Schnurch
Summary: The study synthesized docusate analogues with different alkyl residues to investigate the most favorable hydrophobic tail for hydrophobic ion pairing. The lead counterions dioleyl sulfosuccinate and bis(isotridecyl) sulfosuccinate significantly increased the hydrophobicity of the resulting complexes.
ACTA BIOMATERIALIA
(2022)
Article
Chemistry, Physical
Zeynep Burcu Akkus-Dagdeviren, Andrea Fuerst, Julian David Friedl, Martina Tribus, Andreas Bernkop-Schnuerch
Summary: This study investigates the combined usage of Layer-by-Layer coating and alkaline phosphatase-responsive charge reversal strategies in colloidal drug delivery systems. The findings show that this combination improves cellular internalisation and decreases cytotoxic effects.
JOURNAL OF COLLOID AND INTERFACE SCIENCE
(2023)
Article
Biochemistry & Molecular Biology
Ahmad Saleh, Zeynep Burcu Akkus-Dagdeviren, Soheil Haddadzadegan, Richard Wibel, Andreas Bernkop-Schnuerch
Summary: The study developed peptide antibiotic-polyphosphatenanoparticles for targeted drug release on the intestinal epithelium. These nanoparticles showed protection against enzymatic degradation, superior mucus permeating properties, and the ability to release drug when triggered by intestinal alkaline phosphatase. The findings suggest that the PMB-PP NPs are promising delivery systems for protecting cationic peptide antibiotics, overcoming the mucus barrier, and providing direct drug release.
Article
Pharmacology & Pharmacy
Victor Claus, Helen Spleis, Christoph Federer, Katrin Zoeller, Richard Wibel, Flavia Laffleur, Camille Dumont, Philippe Caisse, Andreas Bernkop-Schnuerch
Summary: In this study, the lipophilicity of insulin glargine was increased through hydrophobic ion pairing with sodium octadecyl sulfate, enabling its incorporation into self-emulsifying drug delivery systems (SEDDS). Two SEDDS formulations were developed and loaded with the insulin glargine-HIP complex. The results showed that the bioavailability of the complexed insulin glargine in the SEDDS formulations was significantly increased after oral administration in rats.
INTERNATIONAL JOURNAL OF PHARMACEUTICS
(2023)
Article
Nanoscience & Nanotechnology
Bao Le-Vinh, Christian Steinbring, Nguyet-Minh Nguyen Le, Barbara Matuszczak, Andreas Bernkop-Schnurch
Summary: Chitosan and its derivatives with high cell adhesion properties were designed and tested for their suitability as scaffold materials in tissue engineering. The attachment of a thiol group to chitosan significantly improved cell adhesion, with higher modification levels leading to better results. The resulting chitosan-based cryogels showed promise for 3D cell culture and tissue engineering.
ACS APPLIED MATERIALS & INTERFACES
(2023)
Review
Chemistry, Multidisciplinary
Sobia Noreen, Andreas Bernkop-Schnuerch
Summary: Thiolation of poly- and oligosaccharides introduces various favorable properties for tissue engineering and wound healing, including stable 3D networks, enhanced cell adhesion and signaling, and controlled release of active ingredients.
ADVANCED FUNCTIONAL MATERIALS
(2023)
Article
Biochemistry & Molecular Biology
Gergely Kali, Bengi Ozkahraman, Flavia Laffleur, Patrick Knoll, Richard Wibel, Katrin Zoller, Andreas Bernkop-Schnurch
Summary: This study aimed to design and evaluate an anionic, thiolated cellulose derivative for its mucoadhesive and permeation-enhancing properties using enoxaparin as a model drug. The thiolated cellulose exhibited enhanced mucoadhesion on porcine intestinal mucosa and improved permeation in Caco-2 cell monolayer. In vivo studies in rats showed significantly higher oral bioavailability compared to the aqueous solution of the drug.
Article
Pharmacology & Pharmacy
Richard Wibel, Florina Veider, Barbara Hoyer, Joseph Chamieh, Andreas Bernkop-Schnuerch
Summary: Organic solvents have a substantial impact on the solubility and precipitation rate of drugs in self-emulsifying drug delivery systems. This impact is particularly significant for moderately lipophilic drugs.
INTERNATIONAL JOURNAL OF PHARMACEUTICS
(2023)
Article
Pharmacology & Pharmacy
Victor Claus, Matthias Sandmeier, Nathalie Hock, Helen Spleis, Sera Lindner, Monika Kalb, Andreas Bernkop-Schnuerch
Summary: In this study, the lipophilicity of model proteins was increased by combining various surfactants with insulin, bovine serum albumin, and horseradish peroxidase. The key factors responsible for complex formation were identified. The formed complexes were stable in simulated gastrointestinal fluids and could be incorporated into self-emulsifying drug delivery systems.
INTERNATIONAL JOURNAL OF PHARMACEUTICS
(2023)
Article
Pharmacology & Pharmacy
Zeynep Burcu Akkus-Dagdeviren, Sema Arisoy, Julian David Friedl, Andrea Fuerst, Ahmad Saleh, Andreas Bernkop-Schnuerch
Summary: The aim of this study was to develop enzyme-activated charge-reversal lipid nanoparticles (LNPs) as novel gene delivery systems. The researchers successfully anchored a transfection promoter on the surfaces of LNPs to achieve high encapsulation and efficient gene delivery. The experiment results showed that the enzyme-triggered charge reversal of LNPs resulted in significantly increased transfection efficiency in human alveolar epithelial cells.
INTERNATIONAL JOURNAL OF PHARMACEUTICS
(2023)
Article
Pharmacology & Pharmacy
Nathalie Hock, Dennis To, Eva Sanchez Armengol, Simona Summonte, Anna Seybold, Christoph Federer, Andreas Bernkop-Schnuerch
Summary: The aim of this study was to develop biodegradable polyphosphate nanoparticles as long-acting drug delivery systems by utilizing ubiquitarian alkaline phosphatase. The nanoparticles were prepared and characterized, showing good stability and release characteristics. The results also demonstrated their biocompatibility and lack of toxicity. These findings open up new opportunities in parenteral drug delivery.
JOURNAL OF DRUG DELIVERY SCIENCE AND TECHNOLOGY
(2023)
Review
Chemistry, Multidisciplinary
Florina Veider, Eva Sanchez Armengol, Andreas Bernkop-Schnuerch
Summary: The past two decades have seen significant progress in the development of surface charge-reversible nanoparticles for drug delivery and diagnosis. These nanoparticles can change their surface charge from negative to positive at the target site, thereby improving drug delivery and diagnostic agent sensitivity. They have also shown potential in overcoming biofilms and delivering antibiotics directly to cell membranes of microorganisms. This review highlights the latest design and emerging applications of charge-reversible nanoparticles in drug delivery and diagnosis.
Article
Engineering, Biomedical
Arne Matteo Joergensen, Christian Steinbring, Daniel Stengel, Dennis To, Pascal Schmid, Andreas Bernkop-Schnuerch
Summary: This study developed self-emulsifying drug delivery systems containing dry reverse micelles (SEDDS-dRMsPMB) loaded with the model peptide drug polymyxin B (PMB) using anionic (AOT), cationic (DODAB), amphoteric (SL), or non-ionic (P85) surfactants. These systems showed high payload, efficient cellular uptake, and maintained antimicrobial activity, suggesting a potential game-changing strategy for oral peptide drug delivery.
ADVANCED HEALTHCARE MATERIALS
(2023)
Article
Materials Science, Biomaterials
Dennis To, Gergely Kali, Soheil Haddadzadegan, Arne Matteo Joergensen, Katharina Nigl, Fabrizio Ricci, Andreas Bernkop-Schnuerch
Summary: Nanoemulsions with enhanced gastro-intestinal retention time can be achieved by incorporating thiolated surfactants into their surface. Two generations of thiolated surfactants were synthesized and characterized, and their incorporation into nanoemulsions improved the mucoadhesiveness. S-protected thiol derivatives showed the highest mucoadhesive properties among all tested surfactants.
ACS BIOMATERIALS SCIENCE & ENGINEERING
(2023)
Article
Chemistry, Physical
Katrin Zoeller, Anna Karlegger, Martyna Truszkowska, Daniel Stengel, Andreas Bernkop-Schnuerch
Summary: This study investigates the cellular uptake of hydrophobic complexes via nanocarriers using hydrophobic ion pairs (HIPs) formed between two fluorescent components. The results show that HIPs increase the lipophilicity of the model drugs and incorporating HIPs into nanoemulsions (NE) further enhances cellular uptake. HIPs serve as a powerful tool to visualize the cellular distribution of hydrophobic complexes and study their cellular uptake.
JOURNAL OF COLLOID AND INTERFACE SCIENCE
(2024)
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)