Development of a topical treatment for tegumentary leishmaniasis using 8-hydroxyquinoline
Eur J Pharm Biopharm. 2024 Apr 26:114306. doi: 10.1016/j.ejpb.2024.114306. Online ahead of print.ABSTRACTIn the context of neglected diseases, tegumentary leishmaniasis (TL) presents an emerging and re-emerging character in the national territory and in the world. The treatment of TL has limitations, such as intravenous administration route, high toxicity, and high treatment costs. Thus, several researchers work on new therapeutic strategies to improve the effectiveness of the treatment of leishmaniasis. In this light, the present study used a topical formulation, containing 8-hydroquinoline (8-HQN), for the treatment of B...
Source: European Journal of Pharmaceutics and Biopharmaceutics - April 28, 2024 Category: Drugs & Pharmacology Authors: Naianda Rezende Ribeiro Lucas Magno Oliveira Santos Scarleth Silva Costa Carolina Kei Myasaki Daniela Pagliara Lage Vivian Tamietti Martins Rory Cristiane Fortes De Brito Larissa Chaves Freire Ana Maria Ravena Severino Carvalho Bryan Victor Serafim Brigid Source Type: research

Development of a high throughput oxidation profiling strategy for monoclonal antibody products
Eur J Pharm Biopharm. 2024 Apr 25:114301. doi: 10.1016/j.ejpb.2024.114301. Online ahead of print.ABSTRACTOxidation is one of the most common degradation pathways of biopharmaceutics, potentially leading to altered product stability, pharmacokinetics, reduced biological activity and/or an increased immunogenicity. However, it is often insufficiently assessed in early development stages, leaving potential molecule liabilities undiscovered. Aim of the present work was the development of a high throughput oxidation profiling strategy, applicable throughout various stages of biopharmaceutical development. The study demonstrates...
Source: European Journal of Pharmaceutics and Biopharmaceutics - April 27, 2024 Category: Drugs & Pharmacology Authors: Paulina Fischer Olivia M Merkel Michael Siedlar Martin Huelsmeyer Source Type: research

Development of a high throughput oxidation profiling strategy for monoclonal antibody products
Eur J Pharm Biopharm. 2024 Apr 25:114301. doi: 10.1016/j.ejpb.2024.114301. Online ahead of print.ABSTRACTOxidation is one of the most common degradation pathways of biopharmaceutics, potentially leading to altered product stability, pharmacokinetics, reduced biological activity and/or an increased immunogenicity. However, it is often insufficiently assessed in early development stages, leaving potential molecule liabilities undiscovered. Aim of the present work was the development of a high throughput oxidation profiling strategy, applicable throughout various stages of biopharmaceutical development. The study demonstrates...
Source: European Journal of Pharmaceutics and Biopharmaceutics - April 27, 2024 Category: Drugs & Pharmacology Authors: Paulina Fischer Olivia M Merkel Michael Siedlar Martin Huelsmeyer Source Type: research

Dissolvable microarray patches of levodopa and carbidopa for Parkinson's disease management
In conclusion, dissolving MAPs incorporating carbidopa and levodopa represent a promising alternative for improving the therapeutic management of Parkinson's disease.PMID:38663522 | DOI:10.1016/j.ejpb.2024.114304 (Source: European Journal of Pharmaceutics and Biopharmaceutics)
Source: European Journal of Pharmaceutics and Biopharmaceutics - April 25, 2024 Category: Drugs & Pharmacology Authors: Qonita Kurnia Anjani Natalia Moreno-Castellanos Yaocun Li Akmal Hidayat Bin Sabri Ryan F Donnelly Source Type: research

Dissolvable microarray patches of levodopa and carbidopa for Parkinson's disease management
In conclusion, dissolving MAPs incorporating carbidopa and levodopa represent a promising alternative for improving the therapeutic management of Parkinson's disease.PMID:38663522 | DOI:10.1016/j.ejpb.2024.114304 (Source: European Journal of Pharmaceutics and Biopharmaceutics)
Source: European Journal of Pharmaceutics and Biopharmaceutics - April 25, 2024 Category: Drugs & Pharmacology Authors: Qonita Kurnia Anjani Natalia Moreno-Castellanos Yaocun Li Akmal Hidayat Bin Sabri Ryan F Donnelly Source Type: research

Dissolvable microneedles in the skin: Determination the impact of barrier disruption and dry skin on dissolution
This study compares the hyaluronic acid-based DMNs penetration, formation of microchannels, dissolution, and diffusion kinetics in intact, barrier-disrupted (tape stripped), and dry (acetone-treated) porcine ear skin ex vivo. After DMNs application, comprehensive investigations including dermoscopy, stereomicroscope, skin hydration, transepidermal water loss (TEWL), optical coherence tomography (OCT), reflectance confocal laser scanning microscopy (RCLSM), confocal Raman micro-spectroscopy (CRM), two-photon tomography combined with fluorescence lifetime imaging (TPT-FLIM), histology, and scanning electron microscopy (SEM) ...
Source: European Journal of Pharmaceutics and Biopharmaceutics - April 24, 2024 Category: Drugs & Pharmacology Authors: Benchaphorn Limcharoen Supason Wanichweacharungruang Marius Kr öger Titiporn Sansureerungsikul Johannes Schleusener Anna Lena Klein Wijit Banlunara Martina C Meinke Maxim E Darvin Source Type: research

A novel simulated media system for in vitro evaluation of bioequivalent intestinal drug solubility
In this study we have compared literature Fa/FeHIF drug solubilities to values measured in a novel in vitro simulated nine media system for either the fasted (Fa9SIF) or fed (Fe9SIF) state. The manuscript contains 129 literature sampled human intestinal fluid equilibrium solubility values and 387 simulated intestinal fluid equilibrium solubility values. Statistical comparison does not detect a difference (Fa/Fe9SIF vs Fa/FeHIF), a novel solubility correlation window enclosed 95% of an additional literature Fa/FeHIF data set and solubility behaviour is consistent with previous physicochemical studies. The Fa/Fe9SIF system t...
Source: European Journal of Pharmaceutics and Biopharmaceutics - April 24, 2024 Category: Drugs & Pharmacology Authors: Qamar Abuhassan Maria In ês Silva Rana Abu-Rajab Tamimi Ibrahim Khadra Hannah K Batchelor Kate Pyper Gavin W Halbert Source Type: research

Dissolvable microneedles in the skin: Determination the impact of barrier disruption and dry skin on dissolution
This study compares the hyaluronic acid-based DMNs penetration, formation of microchannels, dissolution, and diffusion kinetics in intact, barrier-disrupted (tape stripped), and dry (acetone-treated) porcine ear skin ex vivo. After DMNs application, comprehensive investigations including dermoscopy, stereomicroscope, skin hydration, transepidermal water loss (TEWL), optical coherence tomography (OCT), reflectance confocal laser scanning microscopy (RCLSM), confocal Raman micro-spectroscopy (CRM), two-photon tomography combined with fluorescence lifetime imaging (TPT-FLIM), histology, and scanning electron microscopy (SEM) ...
Source: European Journal of Pharmaceutics and Biopharmaceutics - April 24, 2024 Category: Drugs & Pharmacology Authors: Benchaphorn Limcharoen Supason Wanichweacharungruang Marius Kr öger Titiporn Sansureerungsikul Johannes Schleusener Anna Lena Klein Wijit Banlunara Martina C Meinke Maxim E Darvin Source Type: research

A novel simulated media system for in vitro evaluation of bioequivalent intestinal drug solubility
In this study we have compared literature Fa/FeHIF drug solubilities to values measured in a novel in vitro simulated nine media system for either the fasted (Fa9SIF) or fed (Fe9SIF) state. The manuscript contains 129 literature sampled human intestinal fluid equilibrium solubility values and 387 simulated intestinal fluid equilibrium solubility values. Statistical comparison does not detect a difference (Fa/Fe9SIF vs Fa/FeHIF), a novel solubility correlation window enclosed 95% of an additional literature Fa/FeHIF data set and solubility behaviour is consistent with previous physicochemical studies. The Fa/Fe9SIF system t...
Source: European Journal of Pharmaceutics and Biopharmaceutics - April 24, 2024 Category: Drugs & Pharmacology Authors: Qamar Abuhassan Maria In ês Silva Rana Abu-Rajab Tamimi Ibrahim Khadra Hannah K Batchelor Kate Pyper Gavin W Halbert Source Type: research

Engineering pH-sensitive dissolution of lipid-polymer nanoparticles by Eudragit integration impacts plasmid DNA (pDNA) transfection
In this study, biocompatible Eudragit constructs E100 and RS100 were formulated as lipid-polymer nanoparticles loaded with pDNA expressing red fluorescent protein (RFP) as a model therapeutic. Using a facile nanoprecipitation technique, a core-shell structure stabilised by lipid-polyethylene glycol (PEG) surfactant was produced and displayed resistance to ultracentrifugation. Both cationic polymers E100 (pH-sensitive dissolution at 5) and RS100 (pH-insensitive dissolution) produced 150-200 nm sized particles with a small positive surface charge (+3-5 mV) and high pDNA encapsulation efficiencies (EE) of 75-90 %. The dissolu...
Source: European Journal of Pharmaceutics and Biopharmaceutics - April 21, 2024 Category: Drugs & Pharmacology Authors: Diviya Santhanes Huiming Zhang Alex Wilkins Robert John Aitken Anne-Louise Gannon Mingtao Liang Source Type: research

Engineering pH-sensitive dissolution of lipid-polymer nanoparticles by Eudragit integration impacts plasmid DNA (pDNA) transfection
In this study, biocompatible Eudragit constructs E100 and RS100 were formulated as lipid-polymer nanoparticles loaded with pDNA expressing red fluorescent protein (RFP) as a model therapeutic. Using a facile nanoprecipitation technique, a core-shell structure stabilised by lipid-polyethylene glycol (PEG) surfactant was produced and displayed resistance to ultracentrifugation. Both cationic polymers E100 (pH-sensitive dissolution at 5) and RS100 (pH-insensitive dissolution) produced 150-200 nm sized particles with a small positive surface charge (+3-5 mV) and high pDNA encapsulation efficiencies (EE) of 75-90 %. The dissolu...
Source: European Journal of Pharmaceutics and Biopharmaceutics - April 21, 2024 Category: Drugs & Pharmacology Authors: Diviya Santhanes Huiming Zhang Alex Wilkins Robert John Aitken Anne-Louise Gannon Mingtao Liang Source Type: research

Exosome-Based Macromolecular neurotherapeutic drug delivery approaches in overcoming the Blood-Brain barrier for treating brain disorders
Eur J Pharm Biopharm. 2024 Apr 18:114298. doi: 10.1016/j.ejpb.2024.114298. Online ahead of print.ABSTRACTDelivering drugs to the brain is a complex challenge in medical research, particularly for disorders like Alzheimer's and Parkinson's. The blood-brain barrier restricts the entry of many therapeutic molecules, hindering their effectiveness. Nanoparticles, a potential solution, face issues like toxicity and limited approvals. A new avenue explores the use of small extracellular vesicles (sEVs), i.e., exosomes, as natural carriers for drug delivery. sEVs, tiny structures below 150 nm, show promise due to their minimal imm...
Source: European Journal of Pharmaceutics and Biopharmaceutics - April 20, 2024 Category: Drugs & Pharmacology Authors: Krishna Yadav R Vijayalakshmi Kantrol Kumar Sahu Pavani Sure Kavita Chahal Renu Yadav None Sucheta Akhilesh Dubey Megha Jha Madhulika Pradhan Source Type: research

Spray-drying of PEI-/PPI-based nanoparticles for DNA or siRNA delivery
In this study, we identify optimal spray-drying conditions for PEI-based nanoparticles containing large plasmid DNA or small siRNAs, and further explore the spray-drying of nanoparticles containing chemically modified polymers. Poly(vinyl alcohol) (PVA), but not trehalose or lactose, is particularly well-suited as excipient, retaining or even enhancing transfection efficacies compared to fresh complexes. A big mesh size is critically important as well, while the variation of the spray-drying temperature plays a minor role. Upon spray-drying, microparticles in a ∼ 3.3 - 8.5 µm size range (laser granulometry) are obtained...
Source: European Journal of Pharmaceutics and Biopharmaceutics - April 19, 2024 Category: Drugs & Pharmacology Authors: Sandra Noske Michael Karimov Martin Kr üger Bettina Lilli Alexander Ewe Achim Aigner Source Type: research

Bioequivalence risk assessment of oral formulations containing racemic ibuprofen through a chiral physiologically based pharmacokinetic model of ibuprofen enantiomers
Eur J Pharm Biopharm. 2024 Apr 17:114293. doi: 10.1016/j.ejpb.2024.114293. Online ahead of print.ABSTRACTThe characterization of the time course of ibuprofen enantiomers can be useful in the selection of the most sensitive analyte in bioequivalence studies. Physiologically based pharmacokinetic (PBPK) modelling and simulation represents the most efficient methodology to virtually assess bioequivalence outcomes. In this work, we aim to develop and verify a PBPK model for ibuprofen enantiomers administered as a racemic mixture with different immediate release dosage forms to anticipate bioequivalence outcomes based on differ...
Source: European Journal of Pharmaceutics and Biopharmaceutics - April 19, 2024 Category: Drugs & Pharmacology Authors: Javier Reig-L ópez Marina Cuquerella-Gilabert Enrique Band ín-Vilar Matilde Merino-Sanju án V íctor Mangas-Sanjuán Alfredo Garc ía-Arieta Source Type: research

Transcriptomic and western blot characterisation of the human CLEFF4 clone, a new rapid cell line replacement for the Caco2 model
Eur J Pharm Biopharm. 2024 Apr 17:114291. doi: 10.1016/j.ejpb.2024.114291. Online ahead of print.ABSTRACTThe CLEFF4 sub clone from stock late passage Caco2 cells has a unique property of being able to develop polarised cell monolayers with high P-gp expression and tight junctions much quicker than the original cell line. Instead of being useful for transport studies 21-24 days after initiating culture, the CLEFF4 cell line matures in 5-6 days with tight junctions surpassing that of 3 week old Caco2 cells in that time frame [1]. This has enabled the CLEFF4 cell line to provide measures of apparent permeability for potential...
Source: European Journal of Pharmaceutics and Biopharmaceutics - April 19, 2024 Category: Drugs & Pharmacology Authors: Andrew Crowe Source Type: research