European Journal of Pharmaceutics and Biopharmaceutics最新文献

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Platinum nanoparticles interact with epirubicin in size dependent manner and affect its biological activity 铂纳米粒子与表阿霉素的相互作用与表阿霉素的生物活性呈大小依赖性。
IF 4.3 2区 医学
European Journal of Pharmaceutics and Biopharmaceutics Pub Date : 2025-09-10 DOI: 10.1016/j.ejpb.2025.114866
Patrycja Bełdzińska , Marcin Zakrzewski , Katarzyna Grzyb , Amandine Hauer , Marzena Jamrógiewicz , Dariusz Wyrzykowski , Katarzyna Bury , Grzegorz Gołuński , Jacek Piosik
{"title":"Platinum nanoparticles interact with epirubicin in size dependent manner and affect its biological activity","authors":"Patrycja Bełdzińska ,&nbsp;Marcin Zakrzewski ,&nbsp;Katarzyna Grzyb ,&nbsp;Amandine Hauer ,&nbsp;Marzena Jamrógiewicz ,&nbsp;Dariusz Wyrzykowski ,&nbsp;Katarzyna Bury ,&nbsp;Grzegorz Gołuński ,&nbsp;Jacek Piosik","doi":"10.1016/j.ejpb.2025.114866","DOIUrl":"10.1016/j.ejpb.2025.114866","url":null,"abstract":"<div><div>In 2022, nearly 20 million new cancer cases were diagnosed worldwide. Despite undeniable improvement in cancer treatment, chemotherapy, a frequently used method, remains limited due to severe side effects. Hence, in this research we utilized platinum nanoparticles (PtNPs) of varying sizes to investigate their interactions with epirubicin (EPI), a commonly used anticancer drug, and asses their impact on its biological activity.</div><div>We employed various physicochemical methods, including Fluorescence and Infrared Spectroscopies, Differential Scanning Calorimetry, Isothermal Titration Calorimetry, Atomic Force Microscopy and Dynamic Light Scattering with Zeta Potential measurements, to investigate the interactions and aggregation patterns of PtNPs with EPI. Moreover, the biological effect of these interactions, with a particular emphasis on the differences due to nanoparticles’ sizes, was verified in Ames mutagenicity test on <em>Salmonella enterica</em> serovar Typhimurium TA98 and through cytotoxicity assays on MelJuSo (cancerous) and HaCaT (non-cancerous) cell lines.</div><div>The obtained results confirmed the presence of PtNPs-EPI interactions depending on the nanoparticles’ size. The physicochemical analyses revealed the formation of EPI-induced aggregates of nanoparticles, which may be of great importance in the context of the biological effects. Consequently, the biological part indicated that PtNPs decrease EPI mutagenicity and increase its cytotoxicity in cancerous cell line. In the contrary, nanoparticles exhibited a potential protective effect on cells and mostly increased or maintained the cells viability in non-cancerous cell line. Summing up, our research provides valuable insights into the PtNPs influence on epirubicin with special focus on the differences attributed to nanoparticles sizes.</div></div>","PeriodicalId":12024,"journal":{"name":"European Journal of Pharmaceutics and Biopharmaceutics","volume":"216 ","pages":"Article 114866"},"PeriodicalIF":4.3,"publicationDate":"2025-09-10","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145052383","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":2,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
pH-Sensitive acrylic acid grafted Abelmoschus esculentus composite for sustained release of pantoprazole sodium ph敏感丙烯酸接枝藻藻复合材料对泮托拉唑钠缓释的影响
IF 4.3 2区 医学
European Journal of Pharmaceutics and Biopharmaceutics Pub Date : 2025-09-10 DOI: 10.1016/j.ejpb.2025.114859
Maryam Basharat , Sobia Noreen , Shazia Akram Ghumman , Khadeeja Ali Alsader , Farooq Anwar , Bushra Ijaz , Tahira Batool , Fozia Batool , Afeefa Aslam , Khurram Shahzad Munawar , Samina Aslam , Nisar Ahmed
{"title":"pH-Sensitive acrylic acid grafted Abelmoschus esculentus composite for sustained release of pantoprazole sodium","authors":"Maryam Basharat ,&nbsp;Sobia Noreen ,&nbsp;Shazia Akram Ghumman ,&nbsp;Khadeeja Ali Alsader ,&nbsp;Farooq Anwar ,&nbsp;Bushra Ijaz ,&nbsp;Tahira Batool ,&nbsp;Fozia Batool ,&nbsp;Afeefa Aslam ,&nbsp;Khurram Shahzad Munawar ,&nbsp;Samina Aslam ,&nbsp;Nisar Ahmed","doi":"10.1016/j.ejpb.2025.114859","DOIUrl":"10.1016/j.ejpb.2025.114859","url":null,"abstract":"<div><div>The research presents a pH-sensitive acrylic acid-grafted hydrogel (graft composite) derived from <em>Abelmoschus esculentus</em> mucilage (AEM) to improve therapeutic outcomes in Crohn’s disease and ulcerative colitis. The FT-IR spectroscopy, scanning electron microscopy (SEM), and X-ray diffraction (XRD) confirm successful grafting with a porous structure favorable for drug loading. Drug release studies showed slower PAS release under acidic conditions and faster release under alkaline conditions, mimicking the pH variations of the gastrointestinal tract. Release kinetics confirmed the Korsmeyer-Peppas model, exhibiting non-Fickian diffusion behavior, especially in the alkaline medium, with R<sup>2</sup> value ranging from 0.9874 to 0.9989. Biocompatibility assessments, including cytotoxicity, hemocompatibility, and acute oral toxicity tests, demonstrated that the graft composite is safe for use. <em>In vivo</em> studies confirmed an increase in the half-life of PAS from 1.119 to 4.395 h. This pH-sensitive delivery system offers a promising approach for the controlled, targeted release of PAS in the colon, enhancing therapeutic efficacy for patients with inflammatory bowel diseases. The successful development of this grafted composite represents a significant advancement in biocompatible, controlled drug delivery for gastrointestinal disorders.</div></div>","PeriodicalId":12024,"journal":{"name":"European Journal of Pharmaceutics and Biopharmaceutics","volume":"216 ","pages":"Article 114859"},"PeriodicalIF":4.3,"publicationDate":"2025-09-10","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145046078","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":2,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Establishing clinically relevant dissolution specifications for prodrug bioequivalence risk assessment: Integration of a dissolution/permeation system with physiologically based biopharmaceutics modeling in abiraterone acetate 为前药生物等效性风险评估建立临床相关的溶出度规范:在醋酸阿比特龙中整合溶出/渗透系统和基于生理的生物制药模型。
IF 4.3 2区 医学
European Journal of Pharmaceutics and Biopharmaceutics Pub Date : 2025-09-07 DOI: 10.1016/j.ejpb.2025.114857
Fulin Bi , Yan Lin , Baohong Zhang , Zishan Chen , Jixia Li , Tong Yuan , Jin Yang
{"title":"Establishing clinically relevant dissolution specifications for prodrug bioequivalence risk assessment: Integration of a dissolution/permeation system with physiologically based biopharmaceutics modeling in abiraterone acetate","authors":"Fulin Bi ,&nbsp;Yan Lin ,&nbsp;Baohong Zhang ,&nbsp;Zishan Chen ,&nbsp;Jixia Li ,&nbsp;Tong Yuan ,&nbsp;Jin Yang","doi":"10.1016/j.ejpb.2025.114857","DOIUrl":"10.1016/j.ejpb.2025.114857","url":null,"abstract":"<div><div>Prodrugs with enzymatic activation requirements, such as the weakly basic biopharmaceutical classification system (BCS) class IV compound abiraterone acetate (ABA), face considerable bioequivalence (BE) risks owing to their pH-dependent solubility, food effects, and variable intestinal hydrolysis. This study established clinically relevant dissolution specifications for ABA using biorelevant dissolution and physiologically based biopharmaceutics modelling (PBBM). Two dissolution methods, two-stage (gastrointestinal transfer simulation) and single-phase (biorelevant media), were evaluated under fasted and fed conditions. Clinical BE studies revealed non-BE for formulation A (fasted, N = 39) but compliance for formulation B (fasted/fed, N = 40). Two-stage dissolution highlighted supersaturation dynamics, with fed-state media (FeSSIF-V2) enhancing solubility by &gt;10-fold compared to fasted conditions. Although this method is biopredictive, its complexity limits its practicality. Single-phase dissolution using biorelevant media balances discriminative power and operational feasibility for quality control. Permeability studies identified the active metabolite abiraterone as the absorption driver (apparent permeability coefficient: 1.55 × 10<sup>−5</sup> vs. 8.91 × 10<sup>−</sup>⁶ cm/s for ABA). PBBM integrating hydrolysis kinetics, food effects, and first-pass metabolism predicted clinical pharmacokinetics with a prediction error of &lt;20 %. Virtual BE trials defined a dissolution “safe space” for bioequivalence under both fasted/fed states. This study demonstrates that combining biorelevant dissolution with mechanistic modelling mitigates BE risks for high-variability prodrugs. This single-phase approach offers a scalable and physiologically aligned strategy for guiding the generic development of complex formulations with food-dependent absorption variability.</div></div>","PeriodicalId":12024,"journal":{"name":"European Journal of Pharmaceutics and Biopharmaceutics","volume":"216 ","pages":"Article 114857"},"PeriodicalIF":4.3,"publicationDate":"2025-09-07","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145029141","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":2,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Modeling the influence of the microbial loading level of fluidized bed granules on physical–mechanical and microbiological tablet properties 模拟流化床颗粒中微生物负荷水平对片剂物理力学和微生物学性能的影响。
IF 4.3 2区 医学
European Journal of Pharmaceutics and Biopharmaceutics Pub Date : 2025-09-07 DOI: 10.1016/j.ejpb.2025.114858
Karl Vorländer , Lukas Bahlmann , Arno Kwade , Jan Henrik Finke , Ingo Kampen
{"title":"Modeling the influence of the microbial loading level of fluidized bed granules on physical–mechanical and microbiological tablet properties","authors":"Karl Vorländer ,&nbsp;Lukas Bahlmann ,&nbsp;Arno Kwade ,&nbsp;Jan Henrik Finke ,&nbsp;Ingo Kampen","doi":"10.1016/j.ejpb.2025.114858","DOIUrl":"10.1016/j.ejpb.2025.114858","url":null,"abstract":"<div><div>In order to be able to administer efficient probiotic formulations, it is necessary to process the respective microorganisms gently into suitable dosage forms such as tablets maintaining their viability. In previous studies, the process chain consisting of fluidized bed granulation for life-sustaining drying of <em>Saccharomyces cerevisiae</em> as well as subsequent processing into tablets was investigated. Granules based on dicalcium phosphate (DCP), lactose (LAC) and microcrystalline cellulose (MCC) as carrier materials were produced and tableted, and physical–mechanical as well as microbiological tablet properties were evaluated. This revealed a carrier material-specific influence of granulation on both physical–mechanical and microbiological tablet characteristics. But the extent, to which this depends on the added cell mass, has not yet been investigated. This is addressed in the present study by examining the influence of the loading of the carriers with different amounts of yeast cells and the measurement of the resulting mechanical properties of the tablets and the survival of the microorganisms. Thereby, material-specific effects of loading on compressibility, compactibility and tabletability, but also on the survival of the yeast cells were found and related to the specific deformation mechanisms. Existing models for describing the physical–mechanical relationships are used, adapted and combined, which enables excellent correlations. In addition, empirical models are developed to describe the survival of the microorganisms during tableting the differently loaded granules.</div></div>","PeriodicalId":12024,"journal":{"name":"European Journal of Pharmaceutics and Biopharmaceutics","volume":"216 ","pages":"Article 114858"},"PeriodicalIF":4.3,"publicationDate":"2025-09-07","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145029134","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":2,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Investigating the effects of chelating agents, surfactants and magnesium cations on the size of LPS aggregates in formulations causing low endotoxin recovery in limulus amebocyte lysate assays 研究螯合剂、表面活性剂和镁离子对LPS聚集体大小的影响,这些聚集体在鲎细胞裂解液检测中引起低内毒素回收率
IF 4.3 2区 医学
European Journal of Pharmaceutics and Biopharmaceutics Pub Date : 2025-09-07 DOI: 10.1016/j.ejpb.2025.114861
Amy Gorman , Mark Becker , Clair Baldock , Stephanie Moore , Alexander P. Golovanov
{"title":"Investigating the effects of chelating agents, surfactants and magnesium cations on the size of LPS aggregates in formulations causing low endotoxin recovery in limulus amebocyte lysate assays","authors":"Amy Gorman ,&nbsp;Mark Becker ,&nbsp;Clair Baldock ,&nbsp;Stephanie Moore ,&nbsp;Alexander P. Golovanov","doi":"10.1016/j.ejpb.2025.114861","DOIUrl":"10.1016/j.ejpb.2025.114861","url":null,"abstract":"<div><div>To ensure safety, pharmaceuticals are rigorously tested for lipopolysaccharide (LPS) contamination, as this can trigger severe immune reactions in patients. Low Endotoxin Recovery (LER), describing the masking of spiked LPS controls in Limulus Amebocyte Lysate (LAL) assays, has been associated with the presence of chelating agents and surfactants in pharmaceutical formulations. The addition of excipients, such as Mg<sup>2+</sup>, have shown the ability to mitigate the effects of LER, however, inconsistencies in various studies regarding the influence of the excipients on LPS aggregate characteristics and LER occurrence hinder a clear understanding of the mechanisms underlying LER. In this study, dynamic light scattering (DLS) and small-angle X-ray scattering (SAXS) were employed to systematically assess the impact of chelating agents, surfactants, and divalent cations on the size and shape of LPS aggregates across various formulations. Our results indicate that surfactant-only formulations generally reduce LPS aggregate size, whereas chelating agent-only formulations do not. Notably, the smallest aggregates were observed when both chelating agents and surfactants were present, with the extent of size reduction being specific to the particular excipients used. Additionally, Mg<sup>2+</sup> generally inhibited the excipients’ capacity to decrease aggregate size, most effectively in phosphate-containing samples. Despite these variations in size, the overall aggregate shape remained largely unchanged in all formulations. These findings suggest that LPS aggregate size or shape does not distinguish formulations causing LER; instead, factors such as the characteristics of the LPS aggregate surface in different formulations should be explored in the future.</div></div>","PeriodicalId":12024,"journal":{"name":"European Journal of Pharmaceutics and Biopharmaceutics","volume":"216 ","pages":"Article 114861"},"PeriodicalIF":4.3,"publicationDate":"2025-09-07","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145027014","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":2,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Unravelling the polysorbate 20 composition: A fusion of UPLC-MS analysis and stochastic modelling 揭开聚山梨酯20组成:UPLC-MS分析和随机建模的融合。
IF 4.3 2区 医学
European Journal of Pharmaceutics and Biopharmaceutics Pub Date : 2025-09-07 DOI: 10.1016/j.ejpb.2025.114854
Dirk-Heinrich Evers , Janek Giebel , Finnya Nienau , Stefan Carle , Sascha Gorissen , Julia Buske , Michael E. Herbig , Patrick Garidel , Elina Hagelskamp
{"title":"Unravelling the polysorbate 20 composition: A fusion of UPLC-MS analysis and stochastic modelling","authors":"Dirk-Heinrich Evers ,&nbsp;Janek Giebel ,&nbsp;Finnya Nienau ,&nbsp;Stefan Carle ,&nbsp;Sascha Gorissen ,&nbsp;Julia Buske ,&nbsp;Michael E. Herbig ,&nbsp;Patrick Garidel ,&nbsp;Elina Hagelskamp","doi":"10.1016/j.ejpb.2025.114854","DOIUrl":"10.1016/j.ejpb.2025.114854","url":null,"abstract":"<div><div>Polysorbate 20 (PS20) is one of the most commonly used non-ionic surfactants in cosmetics, pharmaceuticals and food products. Considered as biocompatible and non-irritating, it is further valued for its solubilising and protein stabilising properties. PS20 is manufactured through a multi-stage reaction of sorbitol with various fatty acids and ethylene oxide, resulting in a complex mixture of components with different molecular weights and polarity. Since variations in the distribution of these components can influence its performance, such as the emulsifying or solubilising efficiency, a detailed understanding of the PS20 composition is of importance.</div><div>Herein we introduce a combined approach of reversed-phase chromatography with mass detection and automated stochastic modelling that enables the quantitative characterisation of PS20 at the component level. With two straightforward sample preparations and two methods for an ultra-high performance liquid chromatography (UPLC) system coupled to a single quadrupole mass (QDa) detector, this technique ensures efficient data acquisition. Seven PS20 products of different manufacturers, age and qualities were studied using the presented approach. Molar contents and weight percentages were calculated for each of the more than 27′700 components of the PS20, which were fully characterised by i) the substance class (i.e. sorbitan, isosorbide or polyoxyethylene (POE)), ii) the number of esters, iii) the fatty acid combination and iv) the number of OE units. The obtained results allowed not only an accurate prediction of bulk parameters, such as hydroxyl and saponification values, but also a detailed product comparison.</div></div>","PeriodicalId":12024,"journal":{"name":"European Journal of Pharmaceutics and Biopharmaceutics","volume":"216 ","pages":"Article 114854"},"PeriodicalIF":4.3,"publicationDate":"2025-09-07","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145029163","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":2,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Novel development of lipid-based formulations: Improved wettability and homogeneous API solid dispersion visualised via near-infrared hyperspectral imaging 脂基配方的新发展:通过近红外高光谱成像改善润湿性和均匀的API固体分散。
IF 4.3 2区 医学
European Journal of Pharmaceutics and Biopharmaceutics Pub Date : 2025-09-06 DOI: 10.1016/j.ejpb.2025.114864
Elizabeta Atanaskova , Johannes Poms , Matthias Wolfgang , Carolina Alva , Nadia Mussner , Andreas Zimmer , Nikola Geskovski , Sharareh Salar-Behzadi
{"title":"Novel development of lipid-based formulations: Improved wettability and homogeneous API solid dispersion visualised via near-infrared hyperspectral imaging","authors":"Elizabeta Atanaskova ,&nbsp;Johannes Poms ,&nbsp;Matthias Wolfgang ,&nbsp;Carolina Alva ,&nbsp;Nadia Mussner ,&nbsp;Andreas Zimmer ,&nbsp;Nikola Geskovski ,&nbsp;Sharareh Salar-Behzadi","doi":"10.1016/j.ejpb.2025.114864","DOIUrl":"10.1016/j.ejpb.2025.114864","url":null,"abstract":"<div><div>Lipid-based formulations have been successfully applied to improve the aqueous solubility of active pharmaceutical ingredients (APIs), however, with the bottleneck of limited wettability of the system.</div><div>In this study, a lipid-based system was developed using polyglycerol ester of fatty acids (PGFA) as the main component and hexaglycerol (PG6) as a wetting agent. Felodipine, a BCS class II compound was selected as a model API. Two different temperatures (95 °C and 55 °C) were used to produce API loaded melt-casted samples, with and without PG6. Near-infrared hyperspectral imaging (NIR-HSI) was used as an advanced tool to evaluate and optimize felodipine dispersion in the lipid-based system.</div><div>The established NIR-HSI model demonstrated excellent linearity and accuracy (R<sup>2</sup>Y = 80.999, RMSEC = 0.084) and acted as a powerful tool for screening and optimizing the API dispersibility. Applying 95 °C for producing melt-casted samples enhanced the molecular distribution of felodipine, drug amorphization and uniform dispersion within the matrix. Felodipine inhibited the crystal growth of the lipid. A concentration dependent API release (first order kinetics) was observed from all lipid-based formulations. The API release rate was affected by the lipid crystalline size, the wettability of the system and the type of solid dispersion of API in the lipid-based matrix.</div><div>Deep understanding of these parameters combined with the application of the novel and robust analytical tools such as NIR-HSI is necessary to pave the way of developing advanced lipid-based formulations with tailored API release.</div></div>","PeriodicalId":12024,"journal":{"name":"European Journal of Pharmaceutics and Biopharmaceutics","volume":"216 ","pages":"Article 114864"},"PeriodicalIF":4.3,"publicationDate":"2025-09-06","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145023077","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":2,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Effect of the combination of ion-pairs strategies and permeation enhancers on iguratimod transdermal patch against rheumatoid arthritis 离子对策略联合渗透促进剂对类风湿关节炎iguratimod透皮贴剂的作用。
IF 4.3 2区 医学
European Journal of Pharmaceutics and Biopharmaceutics Pub Date : 2025-09-05 DOI: 10.1016/j.ejpb.2025.114863
Yuyi Xu , Ting Fang , Sen Mu , Ji Li , Hongwei Li , Dongkai Wang
{"title":"Effect of the combination of ion-pairs strategies and permeation enhancers on iguratimod transdermal patch against rheumatoid arthritis","authors":"Yuyi Xu ,&nbsp;Ting Fang ,&nbsp;Sen Mu ,&nbsp;Ji Li ,&nbsp;Hongwei Li ,&nbsp;Dongkai Wang","doi":"10.1016/j.ejpb.2025.114863","DOIUrl":"10.1016/j.ejpb.2025.114863","url":null,"abstract":"<div><div>Iguratimod (IGU) is a novel anti-rheumatic drug that has anti-inflammatory effects, inhibits bone destruction, and promotes bone formation. However, the gastrointestinal side effects caused by oral tablets of IGU pose a challenge. This study aimed to develop an IGU transdermal patch for Rheumatoid Arthritis (RA) through ion-pair and chemical penetrant strategies to improve the therapeutic efficacy. The IGU patch was prepared using IGU-HERP (ion-pair), POCC (permeation promoter), DT 87-4098 (pressure-sensitive adhesive (PSA)), Backings 9720 (backing layer), with component ratios optimized through BBD experiments. The resulting formulations increase the IGU loading and skin penetration of the patch. Then the mechanism of permeation promotion of POCC was investigated in terms of the drug and skin. The molecular interactions between POCC and IGU ion-pairs were investigated by <em>ex vitro</em> artificial membranes, FT-IR, <sup>13</sup>C NMR, and molecular simulation experiments. The interaction between POCC and skin stratum corneum was investigated using saturated drug solution permeation assay, exfoliation of stratum corneum assay, ATR-FTIR assay, SEM assay, and molecular simulation experiment. The results showed that hydrogen bonding between IGU-HEPR and POCC promoted drug release, while POCC would disrupt the dense structure of the stratum corneum and enhance drug penetration. When IGU-HEPR transdermal patches were applied to the rat model, IGU-HEPR transdermal patches exhibited good analgesic and anti-inflammatory effects. In conclusion, this study successfully developed an IGU patch for local administration against RA, providing a reference for improving the penetration of transdermal patches by using an ion-pair strategy.</div></div>","PeriodicalId":12024,"journal":{"name":"European Journal of Pharmaceutics and Biopharmaceutics","volume":"216 ","pages":"Article 114863"},"PeriodicalIF":4.3,"publicationDate":"2025-09-05","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145014189","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":2,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Biomass-derived lignin nanoparticles for the sustained delivery of vascular endothelial growth factor-C 用于血管内皮生长因子- c持续递送的生物质衍生木质素纳米颗粒。
IF 4.3 2区 医学
European Journal of Pharmaceutics and Biopharmaceutics Pub Date : 2025-09-04 DOI: 10.1016/j.ejpb.2025.114860
Ahmad Mavali Zadeh , Emanuela Gatto , Raffaella Lettieri , Honey Bokharaie , Alice Caravella , Cadia D’Ottavi , Elisabetta di Bartolomeo , Fabio Domenici , Setareh Sima , Alexandra Correia , Khushbu Rauniyar , Anna Klose , Zahra Gounani , Timo Laaksonen , Jaana Künnapuu , Michael Jeltsch
{"title":"Biomass-derived lignin nanoparticles for the sustained delivery of vascular endothelial growth factor-C","authors":"Ahmad Mavali Zadeh ,&nbsp;Emanuela Gatto ,&nbsp;Raffaella Lettieri ,&nbsp;Honey Bokharaie ,&nbsp;Alice Caravella ,&nbsp;Cadia D’Ottavi ,&nbsp;Elisabetta di Bartolomeo ,&nbsp;Fabio Domenici ,&nbsp;Setareh Sima ,&nbsp;Alexandra Correia ,&nbsp;Khushbu Rauniyar ,&nbsp;Anna Klose ,&nbsp;Zahra Gounani ,&nbsp;Timo Laaksonen ,&nbsp;Jaana Künnapuu ,&nbsp;Michael Jeltsch","doi":"10.1016/j.ejpb.2025.114860","DOIUrl":"10.1016/j.ejpb.2025.114860","url":null,"abstract":"<div><div>Vascular Endothelial Growth Factor C (VEGFC) is a promising biological drug, with preclinical studies indicating its potential for treating myocardial infarction, neurodegenerative diseases, and lymphedema, a condition that currently lacks curative treatment. While adenoviral VEGFC gene therapy has progressed to phase II studies, its clinical efficacy is limited by rapid immune inactivation. This study explores lignin nanoparticles (LNPs) as an alternative VEGFC delivery system.</div><div>Lignin was extracted from grape shoot-derived wood biomass via the organosolv method and used to synthesize LNPs. The resulting particles, with a Z-Average of 143.6 nm, a PDI of 0.126 and a zeta potential of –41 ± 8 mV, were thoroughly characterized using dynamic light scattering and microscopic techniques to evaluate their structural and morphological features.</div><div>VEGFC loading and release profiles were assessed, showing efficient loading and controlled release capabilities. Stability in plasma and cell viability were evaluated using the 3-[4,5-dimethylthiazol-2-yl]-2,5-diphenyltetrazolium bromide (MTT) assay to assess biocompatibility and therapeutic potential. Our data indicate that VEGFC is relatively stable on its own, suggesting that the key advantage of LNPs lies in their ability to modulate the release profile rather than protect the protein from degradation/inactivation.</div></div>","PeriodicalId":12024,"journal":{"name":"European Journal of Pharmaceutics and Biopharmaceutics","volume":"216 ","pages":"Article 114860"},"PeriodicalIF":4.3,"publicationDate":"2025-09-04","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145008203","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":2,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Best practices to reduce microbial contamination during media-fill testing process in hospital pharmacies: a scoping review of literature 减少医院药房培养基填充测试过程中微生物污染的最佳实践:文献综述。
IF 4.3 2区 医学
European Journal of Pharmaceutics and Biopharmaceutics Pub Date : 2025-09-04 DOI: 10.1016/j.ejpb.2025.114840
S. Bruno , MC. Nurchis , F. Pattavina , E. Campo , G. Santoli , D. Tarantino , R. Campopiano , M. Pani , P. Laurenti , G. Damiani
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