European Journal of Pharmaceutical Sciences最新文献

{"title":"Synthesis, in vitro characterization and biopharmaceutical evaluation of a novel phosphate prodrug of sorafenib","authors":"Simon Hoang Dinh ,&nbsp;Christian Ding Fisker ,&nbsp;Juulia Järvinen ,&nbsp;Kati-Sisko Vellonen ,&nbsp;Annette Bauer-Brandl ,&nbsp;Poul Nielsen ,&nbsp;Jarkko Rautio ,&nbsp;Martin Brandl","doi":"10.1016/j.ejps.2025.107397","DOIUrl":"10.1016/j.ejps.2025.107397","url":null,"abstract":"<div><div>Sorafenib is a multi-kinase inhibitor approved for several cancers with poor aqueous solubility, resulting in low oral bioavailability (38–49 %) despite its high permeability. As a BCS Class II compound, its absorption is solubility-/dissolution-limited. Prodrug strategies, such as phosphate esterification, can improve solubility and promote oral bioavailability upon enzymatic cleavage by intestinal alkaline phosphatase (IALP), abundantly expressed at the intestinal brush border membrane and present in the intestinal lumen. This cleavage is hypothesized to lead to a transient supersaturation of the parent drug, enhancing absorption unless (premature) precipitation prevails. Besides traditional in vitro models like Caco-2 cells, recently microdialysis-sampling has been introduced to study ALP-mediated biomimetic conversion of oral phosphate prodrugs in vitro. Microdialysis enables real-time, non-destructive sampling of molecularly dissolved drug, which allows to study the complex inter-related dynamics under (simulated) human gastrointestinal conditions.</div><div>In this study, a novel and new phosphate prodrug of sorafenib (fossorafenib) was synthesized and its physico-chemical and biopharmaceutical properties were evaluated. Fossorafenib exhibited ∼600-fold higher aqueous solubility than sorafenib in HBSS pH 7.4 and was rapidly cleaved by externally added alkaline phosphatase (ALP), yielding supersaturated sorafenib. Combined cleavage &amp; permeability studies across Caco-2 cell monolayers demonstrated rapid bioconversion of fossorafenib in the apical compartment, with permeation of both the converted parent drug but, surprisingly, also the prodrug. Microdialysis enabled real-time monitoring of the biomimetic conversion of fossorafenib without the requirement for enzyme inactivation, thereby allowing for unprecedented mechanistic insights into the interplay between micellar solubilization and enzymatic cleavage. Microdialysis results suggest that micellar incorporation of fossorafenib into mixed micelles of bile salts and phospholipids can hinder enzymatic cleavage by intestinal ALP, thereby potentially limiting the extent of prodrug activation in the intestinal environment. Taken together with the unexpected ability of the prodrug to cross biological/biomimetic barriers, these findings suggest that fossorafenib may not follow the conventional behavior of classical phosphate-ester oral prodrugs in vivo, highlighting the need for further investigation into its unique biopharmaceutical profile.</div></div>","PeriodicalId":12018,"journal":{"name":"European Journal of Pharmaceutical Sciences","volume":"217 ","pages":"Article 107397"},"PeriodicalIF":4.7,"publicationDate":"2026-02-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145695903","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Individualized dosing strategies in breast cancer chemotherapy: Evidence for therapeutic drug monitoring-guided docetaxel treatment","authors":"Ya-Min Liu ,&nbsp;Wei Huang ,&nbsp;Yong-Zhe Tang ,&nbsp;Hai Zhang ,&nbsp;Sheng-Ying Qin ,&nbsp;Jin Zhang ,&nbsp;Jun-Wei Fan ,&nbsp;Rui-Zhuo Ouyang ,&nbsp;Hai-Ou Yang ,&nbsp;Xiao-Qing Zhang","doi":"10.1016/j.ejps.2025.107407","DOIUrl":"10.1016/j.ejps.2025.107407","url":null,"abstract":"<div><h3>Background</h3><div>Docetaxel is a first-line chemotherapy drug for breast cancer and is traditionally dosed based on body surface area (BSA). However, this method often leads to significant inter-patient variability and a high incidence of adverse drug reactions (ADRs). Therapeutic drug monitoring (TDM) offers a personalized dosing approach that may improve drug safety and efficacy. This study aimed to evaluate the clinical and pharmacoeconomic benefits of TDM-guided dosing compared to traditional BSA-based dosing in breast cancer patients receiving docetaxel-based chemotherapy.</div></div><div><h3>Methods</h3><div>A randomized controlled study was conducted at the Department of Breast Surgery, IPMCH, from October 2022 to July 2024. A total of 208 breast cancer patients were enrolled and randomly assigned to two groups: the BSA group (<em>n</em> = 104) and the TDM-guided pharmacokinetics (PK) group (<em>n</em> = 104). Adverse drug reactions—including hematological, gastrointestinal, skin, neurotoxic, and cardiotoxic events—were monitored and compared between groups. Liver function markers (ALT, AST, ALP) and pharmacoeconomic data (treatment-related costs) were also assessed. Statistical analyses included univariate and interaction models to evaluate the impact of dosing strategy on ADRs and costs.</div></div><div><h3>Results</h3><div>Patients in the TDM-guided PK group exhibited significantly lower levels of ALT, AST, and ALP, indicating reduced hepatic toxicity. Gastrointestinal ADRs—including nausea, diarrhea, and constipation—were less frequent and less severe in the PK group compared to the BSA group. Overall, the incidence and severity of ADRs were markedly reduced in the PK group. Pharmacoeconomic analysis demonstrated consistently lower treatment-related costs in the PK group. Both univariate and interaction analyses confirmed the clinical and economic benefits of TDM-guided dosing.</div></div><div><h3>Conclusion</h3><div>TDM-guided docetaxel dosing significantly reduced ADRs and improved cost efficiency in breast cancer chemotherapy. These findings support the implementation of TDM as a superior strategy to traditional BSA-based dosing, with potential to enhance both patient safety and healthcare resource utilization.</div></div>","PeriodicalId":12018,"journal":{"name":"European Journal of Pharmaceutical Sciences","volume":"217 ","pages":"Article 107407"},"PeriodicalIF":4.7,"publicationDate":"2026-02-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145741614","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Nortriptyline-targeted siRNA-loaded liposomes: Design, affinity, biodistribution, and bioactivity in a murine Herpes Simplex Virus 1 corneal infection model","authors":"Doaa Jbara-Agbaria ,&nbsp;Neethi C Thathapudi ,&nbsp;Marc Groleau ,&nbsp;Majd Agbaria ,&nbsp;Marie-Claude Robert ,&nbsp;Natalia Callai Da Silva ,&nbsp;Sebastien Talbot ,&nbsp;Janet Laganiere ,&nbsp;May Griffith ,&nbsp;Gershon Golomb","doi":"10.1016/j.ejps.2025.107388","DOIUrl":"10.1016/j.ejps.2025.107388","url":null,"abstract":"<div><div>Herpes simplex virus type 1 (HSV1) establishes latency in the trigeminal ganglia and reactivates to cause recurrent infections and severe complications, including herpes simplex keratitis (HSK), the leading cause of infectious corneal blindness in developed countries. We developed and characterized a targeted siRNA delivery system designed to suppress HSV1 by silencing the immediate-early gene ICP0, which encodes a protein essential for lytic infection and viral reactivation. To enhance neuronal accumulation, siRNA-loaded liposomes were decorated with nortriptyline (NTP), a ligand with high affinity for neuronal cells, including those in the trigeminal ganglia. The liposomes were optimized to exhibit nanoscale size, low polydispersity, neutral surface charge, high siRNA loading, spherical morphology, and long-term shelf stability. Studies in cell lines confirmed efficient internalization with good tolerability, and targeted liposomes showed enhanced binding to differentiated PC‑12 neuronal cells, competitively inhibited by free NTP, supporting their targeting specificity. Following retro-orbital administration in mice, NTP-targeted siHSV1 liposomes preferentially accumulated in the trigeminal ganglia. Antiviral efficacy was further assessed by topical application of siHSV1‑loaded liposomes within a biocompatible hydrogel in a murine HSV1 corneal perforation model of HSK. In the corneal limbus, targeted liposomes produced a significant reduction in viral load, whereas in the contralateral trigeminal ganglia, they significantly reduced viral load with a pronounced trend toward decreased ICP0 expression. These results demonstrate the feasibility of using NTP-mediated targeting ligand and support the potential of this delivery platform for treating latent HSV1, warranting further optimization for improved therapeutic efficacy.</div></div>","PeriodicalId":12018,"journal":{"name":"European Journal of Pharmaceutical Sciences","volume":"217 ","pages":"Article 107388"},"PeriodicalIF":4.7,"publicationDate":"2026-02-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145631484","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Protective effects of SA-31 in a psychostimulant-induced neurotoxicity model using SH-SY5Y cells","authors":"Charles E. Amankwa ,&nbsp;Biddut DebNath ,&nbsp;Arlene Abraham ,&nbsp;Olivia Young ,&nbsp;Sudershan R Gondi ,&nbsp;Michael J Forster ,&nbsp;Ritu A. Shetty ,&nbsp;Suchismita Acharya","doi":"10.1016/j.ejps.2025.107399","DOIUrl":"10.1016/j.ejps.2025.107399","url":null,"abstract":"<div><h3>Background</h3><div>Cocaine- and methamphetamine (METH)-induced mitochondrial dysfunction and oxidative stress are key contributors to the neuropathology of psychostimulant addiction. These effects are often accompanied by epigenetic alterations, mitochondrial damage, and the accumulation of reactive oxygen species (ROS). Methionine synthase (MS) plays a critical role in epigenetic regulation and neuronal survival and may offer neuroprotection against psychostimulant-induced toxicity. We hypothesize that SA-31, a novel thiourea-based analog of TEMPOL, will attenuate cocaine or METH induced decrease in antioxidant, anti-inflammatory, and MS activities in neuronal cells.</div></div><div><h3>Methods</h3><div>SA-31 was synthesized and characterized via ¹H NMR and mass spectrometry. Human SH-SY5Y dopaminergic neural cells were exposed to tert‑butyl hydrogen peroxide (TBHP), cocaine hydrochloride, or methamphetamine (METH), with or without co-treatment with SA-31 for 24 h. Cell viability was measured using MTT assays. MS activity, IL-1β, superoxide dismutase (SOD), glutathione peroxidase (GPx), and catalase levels were assessed via ELISA. Mitochondrial function was evaluated using Seahorse-based oxygen consumption rate (OCR) and extracellular acidification rate (ECAR) assays.</div></div><div><h3>Results</h3><div>SA-31 (10–100 µM) significantly protected cells from TBHP-, cocaine-, and METH-induced cytotoxicity. TBHP and METH reduced MS activity, which was significantly restored by SA-31. The compound also reversed cocaine-induced reductions in SOD, GPx, and catalase and lowered pro-inflammatory IL-1β levels. Additionally, SA-31 (1–100 µM) enhanced mitochondrial respiration and glycolytic activity.</div></div><div><h3>Conclusion</h3><div>These findings suggest that SA-31 confers neuroprotection by enhancing MS activity, upregulating antioxidant defenses, and improving mitochondrial function. Further studies in rodent models of addiction are planned to evaluate its therapeutic potential for psychostimulant use disorders and related neurodegenerative conditions.</div></div>","PeriodicalId":12018,"journal":{"name":"European Journal of Pharmaceutical Sciences","volume":"217 ","pages":"Article 107399"},"PeriodicalIF":4.7,"publicationDate":"2026-02-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145713845","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Recent developments of novel nanotechnology-based drug delivery systems for dermal and transdermal applications","authors":"Nazlı Erdoğar ,&nbsp;Betül Gür ,&nbsp;Dilara Örgül","doi":"10.1016/j.ejps.2025.107413","DOIUrl":"10.1016/j.ejps.2025.107413","url":null,"abstract":"<div><div>Topical and transdermal drug delivery faces continuous challenges, primarily due to the formidable barrier function of the stratum corneum (SC), which limits the bioavailability of therapeutics. Nanotechnology-based drug delivery systems (NDDS) have emerged as powerful strategies to overcome these limitations, offering improved drug permeation, sustained release, and enhanced solubility for hydrophobic compounds. This review provides a critical and concise analysis of the latest advancements in NDDS, specifically those employed for both dermal (localized) and transdermal (systemic) delivery. Key nanosystems, including lipid-based, polymeric nanoparticles, vesicular structures, nanoemulsions, nanofibers, dendrimers and micelles are explored, highlighting how their unique physicochemical properties facilitate optimized drug performance. Crucially, the design strategies that selectively target the dermis versus those engineered for transdermal penetration are compared and contrasted. Furthermore, the often-overlooked clinical aspects, including the current understanding of the in vivo fate, biocompatibility, and safety profile of these nanocarriers within the skin layers, are addressed. This comprehensive evaluation provides a foundation for future development of safer and more effective nanomedicines for cutaneous applications.</div></div>","PeriodicalId":12018,"journal":{"name":"European Journal of Pharmaceutical Sciences","volume":"217 ","pages":"Article 107413"},"PeriodicalIF":4.7,"publicationDate":"2026-02-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145751765","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Uncertainties in drug dissolution tests - identification and CFD evaluation of factors limiting the accuracy of the USP2 test","authors":"Normunds Jekabsons ,&nbsp;Sabīne Upnere ,&nbsp;Artūrs Lācis ,&nbsp;Ance Bārzdiņa ,&nbsp;Daniela Paula Prudņikova ,&nbsp;Una Lote Vītoliņa ,&nbsp;Baiba Mauriņa ,&nbsp;Agnese Brangule","doi":"10.1016/j.ejps.2025.107387","DOIUrl":"10.1016/j.ejps.2025.107387","url":null,"abstract":"<div><div>Accurate USP2 paddle dissolution testing is crucial for the quality characterisation, development, and research of solid‑dosage forms, but measurement uncertainties, particularly during the initial flow‑build‑up phase, can mask batch‑to‑batch differences. This work focuses on Computational Fluid Dynamics (CFD) using high-resolution simulations to identify and quantify the main factors contributing to uncertainty in the dissolution of single-component paracetamol tablets. CFD simulations were performed using the OpenFOAM toolkit using a custom solver that simultaneously resolves Navier–Stokes flow and the convective‑diffusive transport of paracetamol. The dissolution process was modelled using the Direct Numerical Simulation and the Smagorinsky-Lilly LES formulation with Van Driest wall damping. Targeted dissolution experiments were used to validate the numerical predictions. Laboratory-prepared tablets (500 ± 1.6 mg) were tested under three configurations: (i) free floating, (ii) magnetically fixed, and (iii) fixed with the tablet bottom coated to suppress rear‑face dissolution. Tests were conducted in a USP2 apparatus at paddle speeds of 25, 50, and 75 RPM, with sampling from 0.5 min to 40 min to capture the time dynamics. The simulated concentration and integral mass fluxes matched experimental dissolution rates.</div></div>","PeriodicalId":12018,"journal":{"name":"European Journal of Pharmaceutical Sciences","volume":"217 ","pages":"Article 107387"},"PeriodicalIF":4.7,"publicationDate":"2026-02-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145596231","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Diphenyl carbonate crosslinked β-cyclodextrin nanosponge-based topically applied gel for co-delivery of baricitinib and tenoxicam in rheumatoid arthritis","authors":"Manxiang Wang ,&nbsp;Umara Arif ,&nbsp;Tayyaba Kaleem ,&nbsp;Humaira Majeed Khan ,&nbsp;Abid Mehmood Yousaf ,&nbsp;Nadeem Ahmad ,&nbsp;Imran Nazir ,&nbsp;Yasser Shahzad","doi":"10.1016/j.ejps.2025.107418","DOIUrl":"10.1016/j.ejps.2025.107418","url":null,"abstract":"<div><div>The present study is aimed at developing baricitinib (BAR) and tenoxicam (TNX) loaded nanosponge (NS) gel for potential topical treatment of rheumatoid arthritis (RA). DPC crosslinked β-CD NS were synthesized at various molar ratios (1:2–1:20), with the 1:8 ratio showing the highest drug loading efficiency (67.0 ± 6.9% for BAR; 82.1 ± 6.8% for TNX). XRD and DSC analysis confirmed amorphization of drugs, SEM revealed porous morphology, DLS revealed particle sizes of 545.5 ± 16.4 nm (BAR-NS) and 585.2 ± 57.7 nm (TNX-NS) with zeta potentials of −11.1 ± 4.4 and −14.6 ± 3.9 mV, respectively. The optimized NS were formulated into topical gels, demonstrating sustained release (BAR: 77–90%; TNX: 96% within 12 h). In vivo evaluation using a CFA-induced RA rat model revealed that combined BAR-NS and TNX-NS gel (0.05/0.25% w/w) inhibited paw edema by &gt;90% at day 25, significantly downregulated pro-inflammatory cytokines (IL-6, IL-1β, TNF-α), restored IL-10, and normalized liver enzymes (ALT, AST, ALP). Histopathological analysis confirmed preservation of cartilage and bone with minimal synovial infiltration. In conclusion, combination of BAR-NS and TNX-NS gel showed synergistic anti-arthritic and anti-inflammatory effects, thus offering a potential topical alternative to conventional therapies for the management of RA.</div></div>","PeriodicalId":12018,"journal":{"name":"European Journal of Pharmaceutical Sciences","volume":"217 ","pages":"Article 107418"},"PeriodicalIF":4.7,"publicationDate":"2026-02-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145793517","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"The relationship between PDE4 and AQP5 in lung tissue under inflammatory conditions: An experimental study","authors":"Ayse Bozkurt ,&nbsp;Zafer Bayraktutan ,&nbsp;Erdem Toktay ,&nbsp;Adem Kara ,&nbsp;Zekai Halici ,&nbsp;Elif Cadirci","doi":"10.1016/j.ejps.2025.107400","DOIUrl":"10.1016/j.ejps.2025.107400","url":null,"abstract":"<div><h3>Objective</h3><div>This study aimed to examine the relationship between Phosphodiesterase 4 (PDE4) and Aquaporin-5 (AQP5) under Lipopolysaccharide (LPS) induced-inflammatory condition.</div></div><div><h3>Methods</h3><div>Inflammatory Acute lung injury (ALI) was induced by intratracheal LPS (5 mg/kg) administration. Rolipram (intraperitoneal) was used as PDE4 inhibiting agent at three different doses (1, 3 and 5 mg/kg) in rat groups. 24 h after LPS administration lung tissues obtained and following analyses performed. AQP5, Phosphodiesterase 4D (PDE4D), Cyclic adenosine monophosphate (cAMP) levels were evaluated for determination of the relationship between these parameters. Also Interleukin-6 (IL-6), Tumor necrosis factor-α (TNF-α), Nuclear factor kappa B (NF-κB), Mitogen-activated protein kinase (MAPK) levels were evaluated as ALI markers.</div></div><div><h3>Results</h3><div>LPS-induced ALI resulted in increased PDE4 enzyme and inflammatory marker levels (IL-6, TNF-α, NF-κB and MAPK) and decreased AQP5 and cAMP levels. Inhibition of PDE4 enzyme to increase cAMP levels by Rolipram resulted in increased AQP5 expression and decreased inflammatory condition and in lung tissues. These results were supported by histopathological and immunhistochemical results.</div></div><div><h3>Conclusion</h3><div>The fact that this study observed a decreases PDE4 expression and increases in AQP5 expression upon Rolipram administration might indicate a close relationship of these two parameters in inflammatory lung disease.</div></div>","PeriodicalId":12018,"journal":{"name":"European Journal of Pharmaceutical Sciences","volume":"217 ","pages":"Article 107400"},"PeriodicalIF":4.7,"publicationDate":"2026-02-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145721652","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"High-throughput screening of amorphous solid dispersions: a systematic approach to enhance bioaccessibility of a poorly soluble drug","authors":"Malte Bøgh Senniksen ,&nbsp;Justus Johann Lange ,&nbsp;Wiebke Saal ,&nbsp;Patrick O’Dwyer ,&nbsp;Martin Kuentz ,&nbsp;Brendan T. Griffin ,&nbsp;Susanne Page ,&nbsp;Jennifer Dressman ,&nbsp;Nicole Wyttenbach","doi":"10.1016/j.ejps.2025.107401","DOIUrl":"10.1016/j.ejps.2025.107401","url":null,"abstract":"<div><div>Poor aqueous solubility and thereby poor and/or variable bioavailability of drug candidates is frequently overcome by developing enabling formulations such as amorphous solid dispersions (ASDs). This study proposes a systematic, miniaturized approach to evaluate the ASD developability of an active pharmaceutical ingredient (API) based on i) assessment of glass forming ability ii) assessment of the supersaturation potential of the neat API by supersaturation/permeation testing, iii) selection of an appropriate ASD carrier system using high-throughput dissolution screening of ASD films and iv) performing high-throughput dissolution/permeation testing of ASD films. The model drug candidate, RO6897779, exhibited good glass forming ability. Eight pharmaceutical polymers (CAP, Eudragit® E, Eudragit® L100, HPMC 100LV, HPMCAS-M, PVP K25, PVP VA64, and Soluplus®) were screened as ASD carriers by high-throughput dissolution testing at drug loads of 20, 30 and 40 % [w/w]. Due to poor performance of the binary systems, ternary ASDs containing Soluplus® were prepared at surfactant loads of 4, 6 and 8 % [w/w] and subsequently, high-throughput dissolution/permeation studies were conducted on selected compositions. The composition containing RO6897779 at a drug load of 20 % in Soluplus®[w/w] with the addition of 6 % [w/w] SDS yielded the best performance, but was inferior to the permeation of supersaturated neat RO6897779. Further studies should be conducted to assess the ability of this four-step, miniaturized approach to predict optimal ASD formulations over a broad range of API physicochemical properties.</div></div>","PeriodicalId":12018,"journal":{"name":"European Journal of Pharmaceutical Sciences","volume":"217 ","pages":"Article 107401"},"PeriodicalIF":4.7,"publicationDate":"2026-02-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145707092","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Corrigendum to “Physiologically-based pharmacokinetic modeling of natalizumab for multiple sclerosis patients to predict the withdrawal time in pregnancy and vaccine time in infants” [European Journal of Pharmaceutical Sciences, 215 (2025), 107301]","authors":"Peilin Zhou ,&nbsp;Chenming Zhong ,&nbsp;Wanhong Wu ,&nbsp;Meng Ke ,&nbsp;Jianwen Xu ,&nbsp;Rongfang Lin ,&nbsp;Pinfang Huang ,&nbsp;Cuihong Lin","doi":"10.1016/j.ejps.2025.107420","DOIUrl":"10.1016/j.ejps.2025.107420","url":null,"abstract":"","PeriodicalId":12018,"journal":{"name":"European Journal of Pharmaceutical Sciences","volume":"217 ","pages":"Article 107420"},"PeriodicalIF":4.7,"publicationDate":"2026-02-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145921395","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}