European Journal of Pharmaceutics and Biopharmaceutics最新文献

{"title":"Hexahistidine-metal assembly encapsulated fibroblast growth factor 21 for lipopolysaccharide-induced acute lung injury.","authors":"Lanlan Song, Huihui Ye, Zhanghang Lv, Yichen Liu, Ziyi Lu, Jun Chen, Haofeng Pan, Luqiong Cai, Yuxin Chen, Shiqing Huang, Xingjie Zan, Xiaoying Huang, Chang Yu","doi":"10.1016/j.ejpb.2025.114650","DOIUrl":"https://doi.org/10.1016/j.ejpb.2025.114650","url":null,"abstract":"<p><p>Acute lung injury (ALI)/acute respiratory distress syndrome (ARDS) represents a spectrum of potentially fatal conditions that currently lack effective drug treatment. Recent researches suggest that Fibroblast Growth Factor 21 (FGF21) may protect against ALI/ARDS. However, the clinical use of FGF21 is limited by its rapid degradation, restricted targeting capabilities, and numerous adverse effects. Addressing this challenge, the study employs a pH-responsive nanoparticle delivery system known as Hexahistidine-metal Assembly (HmA) for administering FGF21. The entrapment efficiency (EE%) and loading capacity (LCwt%) of HmA exceed 90 % and 35 %, respectively, while the HmA@FGF21 nanoparticles exhibit an average size of 130 nm, a PDI value of approximately 0.28, and a zeta potential of 24 mV. In animal experiments, HmA@FGF21 administered in lipopolysaccharide (LPS)-induced lung injury significantly exceed those of standalone FGF21, including mitigating the pathological manifestations and reducing the wet/dry ratio, total protein concentration, and overall cell count in BALF of ALI, whether administered via the airway or intravenously. This therapeutic approach therefore shows promise for precise delivery of FGF21 to the lungs to treat ALI, and may offer a novel, and efficient method for delivery of potential pharmacological agents to address other lung diseases.</p>","PeriodicalId":12024,"journal":{"name":"European Journal of Pharmaceutics and Biopharmaceutics","volume":" ","pages":"114650"},"PeriodicalIF":4.4,"publicationDate":"2025-01-25","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143052094","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}

{"title":"A novel directly compressible co-processed excipient, based-on rice starch for extended-release of tablets.","authors":"Karnkamol Trisopon, Nisit Kittipongpatana, Pimjai Doungsaard, Neungreuthai Chomchoei, Ornanong Suwannapakul Kittipongpatana","doi":"10.1016/j.ejpb.2024.114623","DOIUrl":"https://doi.org/10.1016/j.ejpb.2024.114623","url":null,"abstract":"<p><p>The development of a direct compression excipient with extended-release property is crucial for improving tablet manufacturing and drug delivery. This research focuses on developing a novel co-processed excipient composed of rice starch (RS), methylcellulose (MC), and colloidal silicon dioxide (CSD) using a wet granulation technique. The ratios of RS: MC (1.66:1-1:3) and CSD concentrations (1.0 - 8.26 %) on the properties of co-processed material were evaluated. The RS co-processed with MC and CS (RMSs) formed agglomerate particles (199 - 294 μm of average particle size) with irregular shapes and rough surfaces due to the wet granulation technique. FT-IR spectroscopy confirmed that there was no change in the chemical structure during co-processing, while the amorphous characteristic of MC considerably decreased the crystallinity of the RMSs. The increase in the particle size and the bulk density of the RMSs improved material flowability (17 - 18° for angle of repose) and facilitated particle rearrangement during die filling. RS plasticity promoted material compressibility, while the brittleness of CSD contributed to the increased tablet tensile strength. The elastic recovery of RMSs relied on the ratio of RS, which facilitated permanent bonding, whereas incorporating CSD reduced the lubricant sensitivity of material. The co-processing with MC significantly improved material swellability and effectively maintained the polymer matrix for a long period in media with pH 1.2, 4.5, and 7.5. The in vitro release study confirmed the ability of RMSs to prolong drug release from the matrix tablets, where the cumulative drug release of RMS-2 tablets met the specification and conformed with Higuchi model. Among the RMSs, RMS-2 (RS co-processed with 48.7 % MC and 2.68 % CSD) exhibited the optimal ratio of co-processing, as it demonstrated more favorable compression behavior and extended-release property than other RMSs. These findings indicated that RMSs could potentially be used as a direct compression excipient with extended-release properties.</p>","PeriodicalId":12024,"journal":{"name":"European Journal of Pharmaceutics and Biopharmaceutics","volume":" ","pages":"114623"},"PeriodicalIF":4.4,"publicationDate":"2025-01-24","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143046031","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}

{"title":"Effect of polymer architecture on the properties and in vitro cytotoxicity of drug formulation: A case study with mono- and di-gradient amphiphilic poly(2-Oxazoline)s.","authors":"Shubhashis Datta, Juraj Kronek, Zuzana Nadova, Ludmila Timulakova, Alzbeta Minarcikova, Pavol Miskovsky","doi":"10.1016/j.ejpb.2025.114635","DOIUrl":"https://doi.org/10.1016/j.ejpb.2025.114635","url":null,"abstract":"<p><p>Due to the straightforward single-step synthesis, amphiphilic gradient copoly(2-oxazoline)s are becoming more popular alternative to their block analogue for the development of next-generation drug delivery systems. Here, we investigated the influence of polymer architecture on the physiochemical and biological assessment of nanoformulations formed by the self-assembly of gradient copoly(2-oxazoline)s. Two different architectures were synthesized: hydrophilic-grad-hydrophobic (mono-gradient) and hydrophobic-grad-hydrophilic-grad-hydrophobic (di-gradient) which contained a hydrophilic monomer, 2-ethyl-2-oxazoline (EtOx) and a hydrophobic monomer, 2-phenyl-2-oxazoline (PhOx). Di-gradient copolymers self-assembled in the presence of a hydrophobic model drug, curcumin and formed monodispersed or slightly polydispersed nanoparticle solution. On the other hand, mono-gradient copolymers formed polydispersed nanoparticle solutions. Di-gradient copolymer was slightly more efficient to solubilize curcumin. Mono-gradient copolymer nanoparticle showed faster monomer chain exchange kinetics and comparatively less stability in the presence of serum albumin. At longer incubation times, faster drug release was observed from the mono-gradient copolymer nanoformulations. Cytotoxicity of free curcumin and curcumin loaded nanoparticles in cancer cell of U87 MG (human glioblastoma cell) was dose and time-dependent, whereby the significant cell death occurred after 48 h. Curcumin-loaded mono-gradient copolymer nanoparticles inhibited U87MG cancel cell growth to a large extent compared to the di-gradient copolymer nanoparticles.</p>","PeriodicalId":12024,"journal":{"name":"European Journal of Pharmaceutics and Biopharmaceutics","volume":" ","pages":"114635"},"PeriodicalIF":4.4,"publicationDate":"2025-01-22","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143037654","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}

{"title":"Hot-melt extruded-FDM 3D-printed polyethylene oxide tablets: Dissolution imaging analysis of swelling and drug release.","authors":"Haja Muhamad, Abdul Basit Bashir, James Charlton-Harrison, Rand Abdulhussain, Nihad Mawla, Krishan Patel, James Williamson, Liam Blunt, Karl Walton, Barbara Conway, Kofi Asare-Addo","doi":"10.1016/j.ejpb.2025.114636","DOIUrl":"https://doi.org/10.1016/j.ejpb.2025.114636","url":null,"abstract":"<p><p>Recent developments in pharmacogenetics have emphasised the importance of customised medication, driving interest in technologies like FDM 3D-printing for tailored drug delivery. FDM 3D-printing is a promising technique for the on-demand manufacturing of customised oral dosage forms, providing flexibility in terms of shape and size, dose and drug release profiles. This study investigates the fabrication and characterisation of 3D-printed oral dosage forms using PEO as the primary polymer and PEG 6 K as a plasticiser. Firstly, the printability of the PEO filaments with different propranolol hydrochloride concentrations was explored using the hot-melt extrusion technology. The influence of the propranolol hydrochloride concentrations on the mechanical properties of the filaments was examined was then examined after which surface characteristics, including roughness and wettability, were evaluated. Dissolution imaging was used to visualise the effects of drug content on the swelling and dissolution characteristics of the PEO-based 3D-printed tablets. Results showed a reduction in the flexural stress of the filaments with increasing drug load. It was also observed that increasing the drug load led to higher surface roughness and lower contact angles of the 3D-printed PEO tablets, implying increased surface hydrophilicity. The swelling behaviour of the tablets increased with higher drug concentrations, resulting in a larger gel layer formation. When comparing the drug release percentages, the release rate was higher in the 10 mg propranolol tablets, suggesting that a lower drug content led to a faster release. The greater gel layer of the 40 mg PPN tablets hindered the drug release by acting as a diffusion barrier, while the 10 mg PPN tablets, with less swelling and gel formation, experienced a faster drug release. These findings show the importance of drug content in modifying the surface properties, swelling behaviour, and drug release profiles of 3D-printed PEO tablets. The study also demonstrates the novel use of dissolution imaging for 3D-printed dosage forms, providing valuable quantitative and qualitative insights into swelling dynamics and channel formation to optimise 3D-printed tablets for drug delivery systems.</p>","PeriodicalId":12024,"journal":{"name":"European Journal of Pharmaceutics and Biopharmaceutics","volume":" ","pages":"114636"},"PeriodicalIF":4.4,"publicationDate":"2025-01-22","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143037667","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}

{"title":"Glow in the dark tumor: Enhanced near-IR visualization and destruction of cancer with a self-quenched theranostic.","authors":"S İrem Güler, Cem Levent Altan, E Esma Demircioglu, Nihan Verimli, Beyza Abisoglu, Cigdem Bayraktaroglu, Mustafa Caglar Beker, S Sibel Erdem","doi":"10.1016/j.ejpb.2025.114632","DOIUrl":"https://doi.org/10.1016/j.ejpb.2025.114632","url":null,"abstract":"<p><p>Late diagnosis is one of the major obstacles for the treatment of breast cancer which can be overcome with a system offering sensitive imaging and selective therapeutic effect. In this study, we developed a \"dark-bright\" multifunctional drug delivery system bringing real-time imaging and non-invasive therapy together. Theranostic ability of the system was delivered by Verteporfin (VP), serving as a fluorescence probe and a photosensitizer. To create a \"dark state\" system via self-quenching ability of VP, it was immobilized onto the superparamagnetic iron oxide nanoparticle (SPION) surface. Upon cellular uptake of the \"dark state\" system, release of VP led to fluorescence regain, switching the system to \"bright state\" after which photodynamic therapy (PDT) was initiated to lead to cell death. Theranostic feature of the system was evaluated in MCF-7 and MDA-MB-231 cell lines. Following internalization, fluorescence signal was increased up to ∼56-fold in MCF-7 cells. The IC₅₀ value decreased ∼20-fold and ∼117-fold in MCF-7 and MDA-MB-231 cell lines, respectively. Moreover, the system significantly inhibited migration in the highly aggressive MDA-MB-231 cell line and induced apoptosis by caspase-3 activation. The developed \"dark-bright\" system is a promising multifunctional drug delivery vehicle with extraordinary theranostic features for the detection and destruction of micro tumors.</p>","PeriodicalId":12024,"journal":{"name":"European Journal of Pharmaceutics and Biopharmaceutics","volume":" ","pages":"114632"},"PeriodicalIF":4.4,"publicationDate":"2025-01-19","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143002680","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}

{"title":"Excipients in drug delivery systems: A comprehensive review of approved inactive ingredients for human ophthalmic formulations.","authors":"Raquel Arribada, Daniela Rodrigues-Braz, Armando Silva-Cunha, Francine Behar-Cohen","doi":"10.1016/j.ejpb.2025.114637","DOIUrl":"https://doi.org/10.1016/j.ejpb.2025.114637","url":null,"abstract":"<p><p>Pharmaceutical excipients, commonly known as inactive ingredients, encompass any substance aside from the active ingredient that fulfills a distinct and vital role in a formulation. Their purpose is to enhance specific characteristics, whether associated with the performance of the formulation or aspects related to patient comfort, safety, and acceptability. Because of the limited toxicity studies provided, and the several allergic and toxic side effects that have been reported throughout the years, it is not trivial for the regulatory agencies to approve inactive ingredients for human use. In general, excipients are approved within good manufacturing practices (GMPs) when they undergo analysis of the formulation as a whole, not the standalone substance. However, there is a lack of updated information regarding this subject, given that only the American Food and Drug Administration (FDA) provides a complete list describing the inactive ingredients that are currently approved in drug products for human use. Here, we aimed to provide an overview of key excipients approved by the FDA for ophthalmic use in humans, focusing on their functional roles in ophthalmic formulations, particularly eye drops, and the regulatory requirements involved in these ingredients approval.</p>","PeriodicalId":12024,"journal":{"name":"European Journal of Pharmaceutics and Biopharmaceutics","volume":" ","pages":"114637"},"PeriodicalIF":4.4,"publicationDate":"2025-01-19","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143002655","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}

{"title":"Advances in soft nanoparticle-based platforms for human and veterinary trichomoniasis therapy: A scoping review.","authors":"Raul Edison Luna Lazo, Fernando Miguel Stelmach Alves, Eric Luiz Domingos, Alexandre de Fatima Cobre, Paulo Vitor Farago, Letícia Cruz, Tiana Tasca, Roberto Pontarolo, Luana Mota Ferreira","doi":"10.1016/j.ejpb.2025.114638","DOIUrl":"https://doi.org/10.1016/j.ejpb.2025.114638","url":null,"abstract":"<p><p>This scoping review focuses on drug delivery systems based on soft materials designed for the administration of drugs with anti-Trichomonas vaginalis activity. It primarily examines their use in addressing human trichomoniasis, exploring their physicochemical characteristics, in vitro and in vivo evaluation and identifying existing challenges and gaps. Given the economic burden and the One Health approach, formulations developed aiming at treating animal infections - cattle and poultry - were also discussed. The review involved searching electronic databases, such as PubMed, Scopus, and Web of Science, to find studies published until May 2024; out of the 103 articles retrieved, 18 fulfilled the eligibility criteria. This study investigated soft-nanoparticle formulations, including polymericand lipid-based systems, and their incorporation into suitable formulations for topical application, including hydrogels and polymeric films. Additionally, the discussion covered toxicology and highlighted the knowledge gaps related to the potential use of these formulations in humans. Anti-trichomonas soft nano-based formulations emerge as promising candidates for treating gynecological and animal infections. In conclusion, further preclinical testing is necessary, as none of the formulations have progressed to human clinical trials and have only been evaluated in animal models.</p>","PeriodicalId":12024,"journal":{"name":"European Journal of Pharmaceutics and Biopharmaceutics","volume":" ","pages":"114638"},"PeriodicalIF":4.4,"publicationDate":"2025-01-18","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143002645","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}

{"title":"Control of biomedical nanoparticle distribution and drug release in vivo by complex particle design strategies.","authors":"Melanie Bresinskya, Achim Goepfericha","doi":"10.1016/j.ejpb.2025.114634","DOIUrl":"https://doi.org/10.1016/j.ejpb.2025.114634","url":null,"abstract":"<p><p>The utilization of targeted nanoparticles as a selective drug delivery system is a powerful tool to increase the amount of active substance reaching the target site. This can increase therapeutic efficacy while reducing adverse drug effects. However, nanoparticles face several challenges: upon injection, the immediate adhesion of plasma proteins may mask targeting ligands, thereby diminishing the target cell selectivity. In addition, opsonization can lead to premature clearance and the widespread presence of receptors or enzymes limits the accuracy of target cell recognition. Nanoparticles may also suffer from endosomal entrapment, and controlled drug release can be hindered by premature burst release or insufficient particle retention at the target site. Various strategies have been developed to address these adverse events, such as the implementation of switchable particle properties, regulating the composition of the formed protein corona, or using click-chemistry based targeting approaches. This has resulted in increasingly complex particle designs, raising the question of whether this development actually improves the therapeutic efficacy in vivo. This review provides an overview of the challenges in targeted drug delivery and explores potential solutions described in the literature. Subsequently, appropriate strategies for the development of nanoparticular drug delivery concepts are discussed.</p>","PeriodicalId":12024,"journal":{"name":"European Journal of Pharmaceutics and Biopharmaceutics","volume":" ","pages":"114634"},"PeriodicalIF":4.4,"publicationDate":"2025-01-16","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143002646","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}

{"title":"Corrigendum to \"pH-Sensitive Tacrolimus loaded nanostructured lipid carriers for the treatment of inflammatory bowel disease\" [Eur. J. Pharm. Biopharm. 204 (2024) 114461].","authors":"Sidra Altaf, Mahira Zeeshan, Hussain Ali, Ahmed Zeb, Iqra Afzal, Ayesha Imran, Danish Mazhar, Salman Khan, Fawad Ali Shah","doi":"10.1016/j.ejpb.2024.114573","DOIUrl":"10.1016/j.ejpb.2024.114573","url":null,"abstract":"","PeriodicalId":12024,"journal":{"name":"European Journal of Pharmaceutics and Biopharmaceutics","volume":" ","pages":"114573"},"PeriodicalIF":4.4,"publicationDate":"2025-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142603736","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}

{"title":"Optimization and evaluation of gastroresistant microparticles designed for siRNA oral delivery.","authors":"Thomas Stalder, Nathan Koenig, Raphaël Cornu, Gautier Laurent, Yann Pellequer, Florian Jurin, Brice Moulari, Hélène Martin, Arnaud Beduneau","doi":"10.1016/j.ejpb.2024.114588","DOIUrl":"10.1016/j.ejpb.2024.114588","url":null,"abstract":"<p><p>Oral administration of siRNA is a challenging strategy for the local treatment of intestinal diseases, including cancer and inflammatory bowel disease. Both nucleic acids and delivery systems, especially lipid nanoparticles (LNPs), are sensitive to the acidic pH of the stomach, bile salts and digestive enzymes. The present work focuses on the design and evaluation of gastroresistant alginate microparticles (MPs) prepared with an original process for oral delivery of siRNA. MPs with a mean diameter of less than 200 µm were obtained without extrusion and emulsification methods. Onpattro® marketed pharmaceutical product and TNF-α siRNA-loaded LNPs were successfully microencapsulated with an efficiency of at least 80 %. Gastroresistance properties and intestinal release were demonstrated in simulated gastric and intestinal fluids. After exposure to simulated gastric fluid, MPs in contact with hepatocyte and LPS-activated monocyte-derived macrophage cell lines reduced the expression of transthyretin and TNF-α, demonstrating the preservation of the siRNA activity.</p>","PeriodicalId":12024,"journal":{"name":"European Journal of Pharmaceutics and Biopharmaceutics","volume":" ","pages":"114588"},"PeriodicalIF":4.4,"publicationDate":"2025-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142754915","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}