European Journal of Pharmaceutical Sciences最新文献

{"title":"Development, characterization and evaluation of antibacterial efficacy of actively targeted gold-polydopamine nanoparticle formulations for tuberculosis treatment.","authors":"Eda Turan-Ayhan, Merve Çalımcı, Yasin Turanlı, Funda Şahin, Gülnur Tarhan, Ugur Tamer, Sibel Ilbasmis-Tamer","doi":"10.1016/j.ejps.2025.107219","DOIUrl":"https://doi.org/10.1016/j.ejps.2025.107219","url":null,"abstract":"<p><p>Tuberculosis (TB) is one of the oldest known diseases in the world and it remains a significant public health challenge. The increasing resistance of microorganisms to antibiotics underlines the necessity of appropriate use of antibiotics and correct dosage in treatment. In some cases, frequent and high-dose drug therapy is required, which can lead to serious organ damage in the liver and kidneys in long-term treatment. However, this problem can be overcome by using appropriate drug delivery systems that allow more effective treatments at lower doses. Here, we developed a drug delivery system specifically targeting tuberculosis using gold (Au)-polydopamine (PDA) nanoparticles and modified with polyethylene glycol (PEG), a targeting agent (antibody), and the antibiotic linezolid, resulting in Au-PDA-PEG-Antibody-Linezolid nanoparticles. We successfully developed and characterized these active targeted nanoparticles using UV-Vis absorbance spectroscopy, Fourier-transform infrared spectroscopy (FT-IR), dynamic light scattering (DLS), zeta potential measurements, and surface-enhanced Raman spectroscopy (SERS) measurements. Additionally, the developed formulations were compared with the commercial product through in vitro release studies, and antibacterial efficacy studies were conducted on multidrug-resistant tuberculosis (MDR-TB) strains. The targeted drug delivery system might be able to reduce side effects by increasing treatment effectiveness at lower doses. Additionally, our study is the one of the first example to feature actively targeted nanoparticle formulations using the active ingredient linezolid and PEGs with different chemical structures.</p>","PeriodicalId":12018,"journal":{"name":"European Journal of Pharmaceutical Sciences","volume":" ","pages":"107219"},"PeriodicalIF":4.7,"publicationDate":"2025-08-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144774969","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":"Trehalose-Stabilized Micelle-in-Microparticles of Icariin Targeting IL-4 Pathway in Chronic Obstructive Pulmonary Disease.","authors":"Chengwei Jiang, Satyanarayana Somavarapu","doi":"10.1016/j.ejps.2025.107223","DOIUrl":"https://doi.org/10.1016/j.ejps.2025.107223","url":null,"abstract":"<p><p>Chronic obstructive pulmonary disease (COPD) is a progressive inflammatory airway disorder with limited therapeutic strategies capable of addressing its underlying immunopathology. Icariin (ICA), a flavonoid with documented anti-inflammatory and antioxidant activity, exhibits mechanistic relevance to COPD pathology but is limited in clinical utility due to poor aqueous solubility and low systemic bioavailability. This study reports the development of a dry powder inhalation system comprising DSPE-PEG2000/DPPC micelle-in-microparticles stabilized with trehalose for targeted pulmonary delivery of ICA. Spray-drying produced respirable microparticles with a mass median aerodynamic diameter of 2.36 ± 0.3 µm, an emitted dose of 93%, and a fine particle fraction of 44%, consistent with efficient deposition in the lower respiratory tract. Physicochemical characterization confirmed ICA encapsulation in an amorphous state, with preservation of micellar structure upon rehydration, supporting formulation stability. In vitro studies demonstrated enhanced uptake of ICA-loaded micelles by RAW 264.7 macrophages and a 73% reduction in IL-4-induced CD206 expression, indicative of inhibition of M2 macrophage polarization. These findings support the potential applicability of this inhalable system for modulating macrophage-mediated inflammation in COPD. In vivo studies are required to evaluate pharmacokinetic behaviour, pulmonary distribution, and therapeutic efficacy in validated models of chronic obstructive pulmonary disease.</p>","PeriodicalId":12018,"journal":{"name":"European Journal of Pharmaceutical Sciences","volume":" ","pages":"107223"},"PeriodicalIF":4.7,"publicationDate":"2025-08-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144774970","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":"Engineered carbon dots for mucosal gene delivery.","authors":"Samuel Arca, Françoise Pons, Luc Lebeau","doi":"10.1016/j.ejps.2025.107222","DOIUrl":"https://doi.org/10.1016/j.ejps.2025.107222","url":null,"abstract":"<p><p>Although lung gene therapy holds promise for treating various life-threatening lung diseases, its efficacy is hindered by the mucus layer covering the airways, whose role is to protect the lung epithelium from airborne threats. For efficient gene delivery to the epithelial cells, it is necessary to ensure rapid passage of the transfection particles through the mucus layer before they are eliminated by mucociliary clearance. We developed mucus-penetrating gene carriers using carbon dots (CDs) synthesized from citric acid and bPEI600. Various strategies were investigated to convert these CDs into muco-inert nanoparticles, including PEGylation and decoration with zwitterionic or mucolytic species. After thorough characterization, we assessed their interactions with a mucus model through turbidimetry and transport measurements, as well as their effects on mucus rheology. The efficacy of the carriers to deliver DNA to various cell models was established. Particularly, Calu-3 cells, cultured at the air-liquid interface to obtain abundant mucus production, were used as a discriminating model to evaluate the potency of CDs to deliver their DNA cargo through mucus. While zwitterion-coated CDs failed to induce significant transgene expression, those with PEG decorations yielded moderate results, and CDs designed as thiol reservoirs for local mucolytic action achieved high transfection rates.</p>","PeriodicalId":12018,"journal":{"name":"European Journal of Pharmaceutical Sciences","volume":" ","pages":"107222"},"PeriodicalIF":4.7,"publicationDate":"2025-07-30","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144764713","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":"Hydroxypropyl cellulose-based lyospheres accelerate dissolution of aprepitant combined with its supersaturation for oral delivery.","authors":"Jan Kožák, Paul Bühlbecker, Annika Rautenberg, Claire Chrétien, Yann Pellequer, Edmont Stoyanov, Alf Lamprecht","doi":"10.1016/j.ejps.2025.107220","DOIUrl":"https://doi.org/10.1016/j.ejps.2025.107220","url":null,"abstract":"<p><p>Spray freeze-drying (SFD) leads to a free-flowing lyophilized powder, providing new therapeutic options. In this work, non-aqueous SFD particles are produced with dimethyl sulfoxide as a spray solvent for obtaining amorphous solid dispersions (ASDs) for oral administration of a poorly water-soluble drug, aprepitant. The SFD process was conducted with the low viscosity hydroxypropyl cellulose grades HPC-SSL or HPC-UL to achieve rapidly dissolving aprepitant powder. Besides different HPC grades, varying solid contents (5 and 10%) and drug-excipient ratios (20/80, 40/60 and 100/0) were explored and compared to film casted ASDs and analysed regarding particle morphology and characteristics, storage stability, in vitro dissolution and in vivo pharmacokinetic studies in rats. Median particle size of the powder formulations ranged between 300 and 500 µm, increasing HPC content led to amorphous formulations, that remained amorphous for 12 months of storage at 25°C. Dissolution at pH 1.2 revealed supersaturation across all SFD samples with concentration values twofold and fourfold the saturation concentration for 40/60 and 20/80 drug-excipient ratios respectively. After oral administration to rats, t_max, c_max and AUC varied between 2.5-4 h, 1.04-1.24 µg/ml and AUCs 5.4-8.1 µg*h/ml respectively. Pharmacokinetic parameters were not affected by HPC grade, but indicate a possible relationship between a decrease of geometric particle density and an increase in bioavailability. Low viscosity HPC grades proved suitable excipients for the use in non-aqueous SFD to produce amorphous, rapidly dissolving, low density powders.</p>","PeriodicalId":12018,"journal":{"name":"European Journal of Pharmaceutical Sciences","volume":" ","pages":"107220"},"PeriodicalIF":4.7,"publicationDate":"2025-07-30","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144764714","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":"Photodynamic drug delivery for cancer therapy: Designing liposomes for light-controlled release and enhanced drug efficacy.","authors":"Tristan Le Clainche, Ahmed Gamal Ali Abdelhamid, Nazareth Milagros Carigga Gutierrez, Marie-Anne Jourdain, Sofia Leo, Lucie Sancey, Amandine Hurbin, Jean-Luc Coll, Bénédicte Elena-Herrmann, Mans Broekgaarden","doi":"10.1016/j.ejps.2025.107221","DOIUrl":"https://doi.org/10.1016/j.ejps.2025.107221","url":null,"abstract":"<p><p>Photodynamics involves the use of photocatalytic compounds that, upon excitation with light, produce reactive oxygen species and have seen widespread applications in the treatment of cancer in the form of photodynamic therapy. Within the field of drug delivery, photodynamics has emerged as a strikingly effective approach for spatiotemporal-controlled drug release by harnessing photochemical redox reactions to destabilize lipid nanoformulations that contain oxidation-susceptible excipients. Despite highly promising outcomes in preclinical models, such controlled release modalities have not yet been explored in clinical cancer trials. This review outlines key design considerations for lipid nanoformulations in photodynamic drug delivery, focusing on their susceptibility to photochemical redox reactions, their ability to induce lysosomal permeabilization, and facilitate microenvironmental priming that enhances tumor permeability. These considerations first highlight the role of specific lipid excipients in determining photodynamic drug release efficiencies. Secondly, the selection of the photosensitizing agents is considered, which ideally absorb light >650nm and exhibit limited leaching. Thirdly, the selected photosensitizing agent and pharmaceutical cargoes may dictate which drug loading approach should be pursued, and how drug release is detected. We particularly highlight the promise of nuclear magnetic resonance (NMR) spectroscopy as it can provide non-destructive quantification of encapsulated and released pharmaceutical cargoes, alongside structural assessments of the lipid nanoformulations, without the need for prior separation or complex sample preparation. Finally, considering the corollary effects of photodynamics on cancer cells and the cancer microenvironment, we emphasize the utility of a multi-model approach to evaluate novel photodynamic drug delivery systems. By providing these design considerations, this review aims to boost the field of photodynamic drug delivery and encourage its exploitation in translational cancer research. Moreover, these aspects are equally relevant to stimulate investigations towards oxidation-responsive drug release triggered by alternative external stimuli, thereby broadening the drug delivery arsenal against cancer.</p>","PeriodicalId":12018,"journal":{"name":"European Journal of Pharmaceutical Sciences","volume":" ","pages":"107221"},"PeriodicalIF":4.7,"publicationDate":"2025-07-30","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144764715","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":"Retraction notice to \"Porphyrins to restrict progression of pancreatic cancer by stabilizing KRAS G-quadruplex: In silico, in vitro and in vivo validation of anticancer strategy\" [European Journal of Pharmaceutical Sciences 125 (2018) Pages 39-53].","authors":"Rudradip Pattanayak, Atish Barua, Amlan Das, Tanima Chatterjee, Adrija Pathak, Pritha Choudhury, Srikanta Sen, Prosenjit Saha, Maitree Bhattacharyya","doi":"10.1016/j.ejps.2025.107196","DOIUrl":"https://doi.org/10.1016/j.ejps.2025.107196","url":null,"abstract":"","PeriodicalId":12018,"journal":{"name":"European Journal of Pharmaceutical Sciences","volume":" ","pages":"107196"},"PeriodicalIF":4.7,"publicationDate":"2025-07-29","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144752778","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":"Intelligent drug codelivery platform for immune microenvironment reconstruction and immunochemotherapy in osteosarcoma treatment","authors":"Yi Zhang ,&nbsp;Yuxuan Wu ,&nbsp;Yuanzhuo Xie,&nbsp;Guojing Liu,&nbsp;Shoufeng Wang","doi":"10.1016/j.ejps.2025.107218","DOIUrl":"10.1016/j.ejps.2025.107218","url":null,"abstract":"<div><div>Immunotherapy has emerged as a new strategy for tumor suppression, but its effectiveness is restricted by the immunosuppressive tumor microenvironment (TME) in the context of osteosarcoma treatment. Therefore, a series of therapies focused on immune activation have been introduced as combination treatments with immunotherapy, especially chemotherapies with the ability to induce immunogenic cell death (ICD). In this study, we designed a nanosized platform (^CCHANP_DOX) to codeliver doxorubicin (DOX) and cisplatin (CDDP) to the tumor site for synergistic killing of malignant cells. Due to the ability of DOX to induce ICD, the immunogenicity of the TME was reconstructed <em>via</em> tumor-specific antigen exposure and dendritic cell maturation. Furthermore, ^CCHANP_DOX treatment increased the sensitivity of tumors to anti-programmed cell death-1 (aPD-1). Our in vivo results demonstrated that the combination of ^CCHANP_DOX and aPD-1 not only successfully depressed tumor growth but also inhibited tumor recurrence and lung metastasis. The enhanced anti-tumor effect can be attributed to the activated immune response and established immune memory. This combination may be a potential immunochemotherapy option for osteosarcoma.</div></div>","PeriodicalId":12018,"journal":{"name":"European Journal of Pharmaceutical Sciences","volume":"212 ","pages":"Article 107218"},"PeriodicalIF":4.7,"publicationDate":"2025-07-28","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144750403","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":"Retraction notice to \"Electrospun gold nanorods/graphene oxide loaded-core-shell nanofibers for local delivery of paclitaxel against lung cancer during photo-chemotherapy method\" [European Journal of Pharmaceutical Sciences 164 (2021) 105914].","authors":"Mohammadreza Hasani Azerbaijan, Ehsan Bahmani, Mania Habibi Jouybari, Amir Hassaniazardaryani, Pouya Goleij, Mohammad Akrami, Mohammad Irani","doi":"10.1016/j.ejps.2025.107197","DOIUrl":"https://doi.org/10.1016/j.ejps.2025.107197","url":null,"abstract":"","PeriodicalId":12018,"journal":{"name":"European Journal of Pharmaceutical Sciences","volume":" ","pages":"107197"},"PeriodicalIF":4.7,"publicationDate":"2025-07-28","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144741727","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":"Selection of locally administered ocular tissue-targeting RNA aptamers using in vivo SELEX","authors":"Katja Stenberg ,&nbsp;Sonja Korhonen ,&nbsp;Umair Seemab ,&nbsp;Daniel Miotto Dupont ,&nbsp;Jørgen Kjems ,&nbsp;Paavo Honkakoski ,&nbsp;Astrid Subrizi","doi":"10.1016/j.ejps.2025.107217","DOIUrl":"10.1016/j.ejps.2025.107217","url":null,"abstract":"<div><div>The number of patients affected by retinal diseases is increasing worldwide, and more effective ocular drug delivery strategies are needed. Intravitreal anti-VEGF therapy has reduced the rates of visual impairment and blindness; however, frequent injections cause a significant burden on patients, resulting in poor compliance and therapeutic outcome. Thus, a targeted approach with less invasive administration could extend the dosing intervals and offer a patient-friendly alternative to the current standard of intravitreal injection. Here, <em>in vivo</em> Systematic Evolution of Ligands by Exponential Enrichment (SELEX) was conducted to select ocular tissue-targeting aptamers in rat using topical eye drops and subconjunctival injection. Data analysis of the sequenced aptamer pools revealed significant enrichment of Apt2 and Apt4 in ocular tissues. Their <em>in vivo</em> biodistribution was further evaluated using quantitative real-time PCR (qRT-PCR) at 0.5, 7, and 24 h after subconjunctival administration. Both aptamers accumulated preferentially in posterior ocular tissues, with Apt2 levels exceeding those of the control aptamer by a factor of two at 0.5 h and four at 24 h. This study demonstrates that <em>in vivo</em> SELEX is a viable tool to select ocular tissue-targeting aptamers from the ocular surface. This method could be utilized in the discovery of ocular targeting aptamers for therapeutic purposes and help uncover novel drug targets for various ocular disorders.</div></div>","PeriodicalId":12018,"journal":{"name":"European Journal of Pharmaceutical Sciences","volume":"212 ","pages":"Article 107217"},"PeriodicalIF":4.7,"publicationDate":"2025-07-28","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144741728","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":"From hypothesis to forecasting: The impact of within-subject variability of gastro-intestinal physiology in relation to likelihood of sex-dependent outcome of bioequivalence","authors":"Vijith Roy Titus ,&nbsp;Maitri Sanghavi ,&nbsp;Masoud Jamei ,&nbsp;Amin Rostami-Hodjegan","doi":"10.1016/j.ejps.2025.107213","DOIUrl":"10.1016/j.ejps.2025.107213","url":null,"abstract":"<div><div>There are calls for inclusion of both sexes when conducting bioequivalence (BE) studies as this is not common practice for variety of reasons. There are not many proven cases for sex-dependent outcome of BE studies; hence inclusion of female participants in BE studies is considered as a matter of equity and principle. Most typical BE studies are cross-over design where between-subject variability (including sex effects) plays no role. However, within-subject variability (WSV) can still play a significant role, in passing the BE criteria.</div><div>It has been shown that WSV of gastrointestinal (GI) tract as well as drug disposition factors propagate to the pharmacokinetics, defining the outcome of BE. By applying known sex-based differences in WSV measures of colonic transit time (CTT) and gastric emptying time (GET), we illustrate how hypotheses can be formulated regarding potential sex-dependent outcomes in BE studies. This approach supports informed decision-making on the necessity of including female participants or justifying prudent waivers for their inclusion.</div><div>Virtual Bioequivalence (VBE) assessments were carried out (using VBE module in Simcyp V22 (Certara Predictive Technologies, Sheffield, UK)) where three hypothetical drugs product with distinct dissolution rates were evaluated against multiple virtual test formulation counterparts. The influence of sex-dependent WSV in CTT and GET on VBE outcomes was demonstrated by systematic analysis of discordance between BE in female vs. male subjects. The exercise provided a roadmap for generating hypotheses regarding the propagation of sex differences in physiology to BE outcome.</div></div>","PeriodicalId":12018,"journal":{"name":"European Journal of Pharmaceutical Sciences","volume":"212 ","pages":"Article 107213"},"PeriodicalIF":4.7,"publicationDate":"2025-07-26","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144729004","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}