Application of nanofiber-based drug delivery systems in improving anxiolytic effect of new 1,2,3-triazolo-1,4-benzodiazepine derivatives
Eur J Pharm Sci. 2024 Jan 28;195:106712. doi: 10.1016/j.ejps.2024.106712. Online ahead of print.ABSTRACTAnxiety disorders are highly prevalent worldwide and can affect people of all ages, genders and backgrounds. Much efforts and resources have been directed at finding new anxiolytic agents and drug delivery systems (DDSs) especially for cancer patients to enhance targeted drug delivery, reduce drug adverse effects, and provide an analgesic effect. The aim of this study was (1) to design and develop novel nanofiber-based DDSs intended for the oral administration of new 1,2,3-triazolo-1,4-benzodiazepines derivatives, (2) to...
Source: European Journal of Pharmaceutical Sciences - January 30, 2024 Category: Drugs & Pharmacology Authors: Iryna Botsula Johannes S сhavikin Jyrki Hein ämäki Ivo Laidm äe Maryna Mazur Ain Raal Oleh Koshovyi Igor Kireyev Valentyn Chebanov Source Type: research

Silk fibroin-based dressings with antibacterial and anti-inflammatory properties
Eur J Pharm Sci. 2024 Jan 26;195:106710. doi: 10.1016/j.ejps.2024.106710. Online ahead of print.ABSTRACTSilk fibroin is a fibrillar protein obtained from arthropods such as mulberry and non-mulberry silkworms. Silk fibroin has been used as a dressing in wound treatment for its physical, chemical, mechanical, and biological properties. This systematic review analyzed studies from PubMed, Web of Science, and Scopus databases to identify the molecules preferred for functionalizing silk fibroin-based dressings and to describe their mechanisms of exhibiting anti-inflammatory and antibacterial properties. The analysis of the sel...
Source: European Journal of Pharmaceutical Sciences - January 28, 2024 Category: Drugs & Pharmacology Authors: David Gonz ález-Restrepo Augusto Zuluaga-V élez Lina M Orozco Juan C Sep úlveda-Arias Source Type: research

Modifying peptide/lipid-associated nucleic acids (PLANAs) for CRISPR/Cas9 ribonucleoprotein delivery
Eur J Pharm Sci. 2024 Jan 21;195:106708. doi: 10.1016/j.ejps.2024.106708. Online ahead of print.ABSTRACTWith the first reports on the possibility of genome editing by Clustered Regularly Interspaced Short Palindromic Repeats (CRISPR) and CRISPR-associated protein (Cas)9 surfacing in 2005, the enthusiasm for protein silencing via nucleic acid delivery experienced a resurgence following a period of diminished enthusiasm due to challenges in delivering small interfering RNAs (siRNA), especially in vivo. However, delivering the components necessary for this approach into the nucleus is challenging, maybe even more than the cyt...
Source: European Journal of Pharmaceutical Sciences - January 23, 2024 Category: Drugs & Pharmacology Authors: Abdulelah Alhazza Parvin Mahdipoor Ryley Hall Arthur Manda Sandeep Lohan Keykavous Parang Hamidreza Montazeri Aliabadi Source Type: research

Advancements in preclinical human-relevant modeling of pulmonary vasculature on-chip
Eur J Pharm Sci. 2024 Jan 19;195:106709. doi: 10.1016/j.ejps.2024.106709. Online ahead of print.ABSTRACTPreclinical human-relevant modeling of organ-specific vasculature offers a unique opportunity to recreate pathophysiological intercellular, tissue-tissue, and cell-matrix interactions for a broad range of applications. Lung vasculature is particularly important due to its involvement in genesis and progression of rare, debilitating disorders as well as common chronic pathologies. Here, we provide an overview of the latest advances in the development of pulmonary vascular (PV) models using emerging microfluidic tissue eng...
Source: European Journal of Pharmaceutical Sciences - January 21, 2024 Category: Drugs & Pharmacology Authors: Quoc Vo Kambez H Benam Source Type: research

ProtT5 and random forests-based viscosity prediction method for therapeutic mAbs
Eur J Pharm Sci. 2024 Mar 1;194:106705. doi: 10.1016/j.ejps.2024.106705. Epub 2024 Jan 19.ABSTRACTViscosity is a key characteristic of therapeutic antibodies for subcutaneous administration which requires low volume and high concentration formulations. It would be highly beneficial to accurately predict the viscosity of newly developed therapeutic antibodies in the early stages of development. In this work, a ProtT5-XL-UniRef50 (ProtT5) and Random Forests (RF)-based prediction method was proposed for accurately predicting the viscosity of monoclonal antibodies, with only corresponding sequences needed. Starting from the gi...
Source: European Journal of Pharmaceutical Sciences - January 21, 2024 Category: Drugs & Pharmacology Authors: Xiaohu Hao Long Fan Source Type: research

Trifluoromethyl quinoline derivative targets inhibiting HDAC1 for promoting the acetylation of histone in cervical cancer cells
In conclusion, our study suggested that FKL117 might be used as a novel candidate for targeting the inhibition of HDAC1 against cervical cancer.PMID:38244809 | DOI:10.1016/j.ejps.2024.106706 (Source: European Journal of Pharmaceutical Sciences)
Source: European Journal of Pharmaceutical Sciences - January 20, 2024 Category: Drugs & Pharmacology Authors: Ting Zhang Changhua Zhou Mengfan Lv Jia Yu Sha Cheng Xudong Cui Xinwei Wan Mashaal Ahmad Bixue Xu Juan Qin Xueling Meng Heng Luo Source Type: research

Physiologically based pharmacokinetic modeling to predict maternal pharmacokinetics and fetal carbamazepine exposure during pregnancy
In conclusion, this study established and validated a pregnancy PBPK model of carbamazepine and carbamazepine-10,11-epoxide to assess exposure in pregnant women and fetuses, which provided a reference for the dosage adjustment of carbamazepine during pregnancy.PMID:38244810 | DOI:10.1016/j.ejps.2024.106707 (Source: European Journal of Pharmaceutical Sciences)
Source: European Journal of Pharmaceutical Sciences - January 20, 2024 Category: Drugs & Pharmacology Authors: Yuying Chen Meng Ke Weipeng Fang Yaojie Jiang Rongfang Lin Wanhong Wu Pinfang Huang Cuihong Lin Source Type: research

Erratum to "Sodium glycodeoxycholate and sodium deoxycholate as epithelial permeation enhancers: in vitro and ex vivo intestinal and buccal bioassays" [European Journal of Pharmaceutical Sciences 159 (2021) 105737]
Eur J Pharm Sci. 2024 Mar 1;194:106698. doi: 10.1016/j.ejps.2024.106698. Epub 2024 Jan 18.NO ABSTRACTPMID:38242807 | DOI:10.1016/j.ejps.2024.106698 (Source: European Journal of Pharmaceutical Sciences)
Source: European Journal of Pharmaceutical Sciences - January 19, 2024 Category: Drugs & Pharmacology Authors: David J Brayden Vivien Stuettgen Source Type: research

Pitfalls in evaluating permeability experiments with Caco-2/MDCK cell monolayers
Eur J Pharm Sci. 2024 Mar 1;194:106699. doi: 10.1016/j.ejps.2024.106699. Epub 2024 Jan 16.ABSTRACTWhen studying the transport of molecules across biological membranes, intrinsic membrane permeability (P0) is more informative than apparent permeability (Papp), because it eliminates external (setup-specific) factors, provides consistency across experiments and mechanistic insight. It is thus an important building block for modeling the total permeability in any given scenario. However, extracting P0 is often difficult, if not impossible, when the membrane is not the dominant transport resistance. In this work, we set out to ...
Source: European Journal of Pharmaceutical Sciences - January 17, 2024 Category: Drugs & Pharmacology Authors: Andrea Ebert Carolin Dahley Kai-Uwe Goss Source Type: research

Microparticles and multi-unit systems for advanced drug delivery
Eur J Pharm Sci. 2024 Mar 1;194:106704. doi: 10.1016/j.ejps.2024.106704. Epub 2024 Jan 14.ABSTRACTMicroparticles have unique benefits in the formulation of multiparticulate and multi-unit type pharmaceutical dosage forms allowing improved drug safety and efficacy with favorable pharmacokinetics and patient centricity. On the other hand, the above advantages are served by high and well reproducible quality attributes of the medicinal product where even flexible design and controlled processability offer success as well as possible longer product life-cycle for the manufacturers. Moreover, the specific demands of patients ca...
Source: European Journal of Pharmaceutical Sciences - January 16, 2024 Category: Drugs & Pharmacology Authors: Nikolett K állai-Szabó D óra Farkas Mil éna Lengyel B álint Basa Christian Fleck Istv án Antal Source Type: research

Using molecularly dissolved drug concentrations in PBBMs improves the prediction of oral absorption from supersaturating formulations
Eur J Pharm Sci. 2024 Mar 1;194:106703. doi: 10.1016/j.ejps.2024.106703. Epub 2024 Jan 14.ABSTRACTPredicting the absorption of drugs from enabling formulations is still challenging due to the limited capabilities of standard physiologically based biopharmaceutics models (PBBMs) to capture complex absorption processes. Amongst others, it is often assumed that both, molecularly and apparently dissolved drug in the gastrointestinal lumen are prone to absorption. A recently introduced method for measuring concentrations of molecularly dissolved drug in a dynamic in vitro dissolution setup using microdialysis has opened new opp...
Source: European Journal of Pharmaceutical Sciences - January 15, 2024 Category: Drugs & Pharmacology Authors: Florentin Lukas Holzem Jeannine Petrig Schaffland Martin Brandl Annette Bauer-Brandl Cordula Stillhart Source Type: research

Development of a canine artificial colonic mucus model for drug diffusion studies
In conclusion, the canine artificial colonic mucus can be used to study drug permeation across the mucus and its flexibility allows its use in various set ups depending on the nature of the compound under investigation and equipment availability.PMID:38218203 | DOI:10.1016/j.ejps.2024.106702 (Source: European Journal of Pharmaceutical Sciences)
Source: European Journal of Pharmaceutical Sciences - January 13, 2024 Category: Drugs & Pharmacology Authors: V Barmpatsalou M Tjakra L Li I R Dubbelboer E Karlsson B Pedersen Lomstein C A S Bergstr öm Source Type: research

J24335 exerts neuroprotective effects against 6-hydroxydopamine-induced lesions in PC12 cells and mice
Eur J Pharm Sci. 2024 Mar 1;194:106696. doi: 10.1016/j.ejps.2024.106696. Epub 2024 Jan 9.ABSTRACTParkinson's disease is the second most prevalent age-related neurodegenerative disease and disrupts the lives of people aged >60 years. Meanwhile, single-target drugs becoming inapplicable as PD pathogenesis diversifies. Mitochondrial dysfunction and neurotoxicity have been shown to be relevant to the pathogenesis of PD. The novel synthetic compound J24335 (11-Hydroxy-1-(8-methoxy-5-(trifluoromethyl)quinolin-2-yl)undecan-1-one oxime), which has been researched similarly to J2326, has the potential to be a multi-targeted drug...
Source: European Journal of Pharmaceutical Sciences - January 10, 2024 Category: Drugs & Pharmacology Authors: Zhijian Pan Min Shao Chen Zhao Xuanjun Yang Haitao Li Guozhen Cui Xiaonan Liang Chao-Wu Yu Qingqing Ye Cheng Gao Lijun Di Ji-Wang Chern Hefeng Zhou Simon Ming-Yuen Lee Source Type: research

Physiologically based pharmacokinetic modeling of ritonavir-oxycodone drug interactions and its implication for dosing strategy
This study was aimed to simulate DDI between ritonavir and oxycodone, a widely used opioid, and to formulate dosing protocols for oxycodone by using physiologically based pharmacokinetic (PBPK) modeling. We developed a ritonavir PBPK model incorporating induction and competitive and time-dependent inhibition of CYP3A4 and competitive inhibition of CYP2D6. The ritonavir model was evaluated with observed clinical pharmacokinetic data and validated for its CYP3A4 inhibition potency. We then used the model to simulate drug interactions between oxycodone and ritonavir under various dosing scenarios. The developed model captured...
Source: European Journal of Pharmaceutical Sciences - January 10, 2024 Category: Drugs & Pharmacology Authors: Liang Zheng Wei Zhang Klaus T Olkkola Andr é Dallmann Liang Ni Yingjie Zhao Ling Wang Qian Zhang Wei Hu Source Type: research

Pharmacokinetics, biodistribution, and in vivo toxicity of 7-nitroindazole loaded in pegylated and non-pegylated nanoemulsions in rats
This study evaluates the pharmacokinetic profiles and toxicological properties of 7-NI loaded into the nanoemulsions. After a single intravenous administration of the free drug and the nanoemulsions at a dose of 10 mg.kg-1 in Wistar rats, 7-NI was widely distributed in the organs. The pharmacokinetic parameters of Cmax, t1/2, and AUC0-t were significantly increased after administration of the NEPEG7NI, compared to both free 7-NI and NENPEG7NI (p < 0.05). No observable adverse effects were observed after administering the free 7-NI, NEPEG7NI, or NENPEG7NI in the animals after a single dose of up to 3.0 mg.kg-1. The resul...
Source: European Journal of Pharmaceutical Sciences - January 8, 2024 Category: Drugs & Pharmacology Authors: Angela Patricia Fran ça Thais Alves Silva Daniela Schulz Leonardo Gomes-Pereira Livia Melo Arruda Cunha Merita Pereira Gon çalves Jo ão Victor Soares Vieira Mariele Paludetto Sanches Natalia Koehler Sharbel Maluf Anicleto Poli Jos é Eduardo da Silva-S Source Type: research