European Journal of Pharmaceutics and Biopharmaceutics最新文献

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Liposomal formulations for waterproofing mucosal membranes 用于防水粘膜的脂质体配方
IF 4.4 2区 医学
European Journal of Pharmaceutics and Biopharmaceutics Pub Date : 2025-05-26 DOI: 10.1016/j.ejpb.2025.114757
Luisa Coderch , Lucia Ricci , Meritxell Martí , Saman Bagherpour , Lluïsa Pérez-García , Cristina Alonso
{"title":"Liposomal formulations for waterproofing mucosal membranes","authors":"Luisa Coderch ,&nbsp;Lucia Ricci ,&nbsp;Meritxell Martí ,&nbsp;Saman Bagherpour ,&nbsp;Lluïsa Pérez-García ,&nbsp;Cristina Alonso","doi":"10.1016/j.ejpb.2025.114757","DOIUrl":"10.1016/j.ejpb.2025.114757","url":null,"abstract":"<div><div>Liposome formulations consisting of lipids contained in the stratum corneum have been recently demonstrated to decrease the permeability of mucosae. The permeability barrier of the mucosa is dependent on the presence of specific lipids. The main objective of this work is to reinforce the barrier effect of the oral mucosa with liposomal formulations to decrease permeation. Due to the high similarity in composition and structure between lanolin and human stratum corneum lipids, liposomes were formed with lipids contained in the stratum corneum with two kinds of ceramide or with lanolin. Transmembrane water loss of the two formulations was assessed, obtaining an important diminution for both liposomal formulations. Caffeine, lidocaine, ketoprofen and ivermectin and a virus model were tested on mucosa and on modified mucosa to evaluate the liposomal efficacy.</div><div>A somewhat consistent permeation pattern was obtained for the different membranes: caffeine &gt; lidocaine &gt; ketoprofen &gt; ivermectin. For all drugs and for the virus model, the most effective formulation was the liposomal formulation, consisting of lipids found in the horny layer of the skin. The effect of the lanolin on the transmembrane water loss is not reflected on the drug permeation. Therefore, it is demonstrated the main role of ceramides in the barrier function for drugs and a virus model. Strengthening the barrier function of the mucosa promotes the prevention or reduction of the permeation of different actives, which could be to extrapolate to harmful actives like viruses, pollutants, toxins, contaminants, etc.</div></div>","PeriodicalId":12024,"journal":{"name":"European Journal of Pharmaceutics and Biopharmaceutics","volume":"213 ","pages":"Article 114757"},"PeriodicalIF":4.4,"publicationDate":"2025-05-26","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144166968","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
Lipid-Polyhydroxyalkanoate Hybrid Nanoparticles as Sustainable Platform for mRNA delivery 脂质-聚羟基烷酸酯复合纳米颗粒作为mRNA的可持续药物传递平台。
IF 4.4 2区 医学
European Journal of Pharmaceutics and Biopharmaceutics Pub Date : 2025-05-23 DOI: 10.1016/j.ejpb.2025.114755
Zihnil A.I. Mazrad , Chee Leng Lee , Tianxia Zhang , Nicole M. Warne , Nhu Thao Huynh , Md. Shahruk Nur-A-Tomal , Neil R. Cameron , Leonie van’ t Hag , Colin W. Pouton , Kristian Kempe
{"title":"Lipid-Polyhydroxyalkanoate Hybrid Nanoparticles as Sustainable Platform for mRNA delivery","authors":"Zihnil A.I. Mazrad ,&nbsp;Chee Leng Lee ,&nbsp;Tianxia Zhang ,&nbsp;Nicole M. Warne ,&nbsp;Nhu Thao Huynh ,&nbsp;Md. Shahruk Nur-A-Tomal ,&nbsp;Neil R. Cameron ,&nbsp;Leonie van’ t Hag ,&nbsp;Colin W. Pouton ,&nbsp;Kristian Kempe","doi":"10.1016/j.ejpb.2025.114755","DOIUrl":"10.1016/j.ejpb.2025.114755","url":null,"abstract":"<div><div>The success of mRNA vaccines for the treatment of COVID-19 has generated enormous interest in mRNA therapeutics for various diseases, highlighting the need for robust delivery platforms. Combining the excellent transfection properties of lipids with the high stability of polymeric nanoparticles in a single hybrid system has become an attractive approach to generate next generation mRNA delivery systems. We introduce a modular lipid–polymer hybrid nanoparticle (LPHNP) design based on medium-chain-length polyhydroxyalkanoates (mcl-PHAs) as sustainable alternative to poly(lactic-co-glycolic acid) (PLGA), and a polymer-lipid (DMG-PEG, or poly(2-ethyl-2-oxazoline-myristic acid (PEtOx-MA)). A small library of LPHNPs containing the cationic lipid DOTAP were synthesized using a scalable microfluidic process. Physico-chemical and biological properties of mRNA-LPHNPs were studied. Results showed that the mcl-PHAs (PHA<sub>F10</sub> and PHA<sub>Glu</sub>) derived from <em>Pseudomonas putida</em> can form distinct LPHNPs depending on polymer-to-lipid ratios, and mcl-PHA composition. Cell toxicity, transfection efficiency, serum stability, and the effect of protein interactions was investigated in HeLa cells and human brain endothelial (hCMEC/D3) cells. Importantly, the particles’ biophysical properties and transfection efficacies were not affected after lyophilization and storage at various temperatures for two months. Reporter mRNA was identified across all major organs collected after intravenous injection into mice with limited protein expression in the blood, highlighting the excellent stability of hybrid nanoparticles against blood cell interactions. This approach holds promise for accelerating development of a novel sustainable polymer for mRNA delivery that differs from conventional lipid nanoparticle systems.</div></div>","PeriodicalId":12024,"journal":{"name":"European Journal of Pharmaceutics and Biopharmaceutics","volume":"213 ","pages":"Article 114755"},"PeriodicalIF":4.4,"publicationDate":"2025-05-23","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144141797","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
Impact of various electromagnetic fields on the transdermal permeability of naproxen and the effect of active compound exposure on magnetic field properties 不同电磁场对萘普生透皮通透性的影响及活性化合物暴露对磁场特性的影响
IF 4.4 2区 医学
European Journal of Pharmaceutics and Biopharmaceutics Pub Date : 2025-05-23 DOI: 10.1016/j.ejpb.2025.114715
Rafał Rakoczy , Karolina Zyburtowicz-Ćwiartka , Maciej Konopacki , Anna Nowak , Kararzyna Piotrowska , Anna Muzykiewicz-Szymańska , Łukasz Kucharski , Marian Kordas , Paula Ossowicz-Rupniewska
{"title":"Impact of various electromagnetic fields on the transdermal permeability of naproxen and the effect of active compound exposure on magnetic field properties","authors":"Rafał Rakoczy ,&nbsp;Karolina Zyburtowicz-Ćwiartka ,&nbsp;Maciej Konopacki ,&nbsp;Anna Nowak ,&nbsp;Kararzyna Piotrowska ,&nbsp;Anna Muzykiewicz-Szymańska ,&nbsp;Łukasz Kucharski ,&nbsp;Marian Kordas ,&nbsp;Paula Ossowicz-Rupniewska","doi":"10.1016/j.ejpb.2025.114715","DOIUrl":"10.1016/j.ejpb.2025.114715","url":null,"abstract":"<div><div>Transdermal drug delivery systems present a promising alternative to oral administration, though improving skin permeability of active pharmaceutical ingredients (APIs) remains challenging. This study examines how various electromagnetic fields (EMFs) affect the transdermal permeability of naproxen (NAP) and its physicochemical properties. Using pigskin as a model, NAP permeability was tested under oscillating, pulsed, static, and rotating magnetic fields (RMF), compared to a control group without EMF exposure. The results show significant differences in NAP permeability depending on EMF type, with RMF at 50 Hz yielding the highest cumulative permeation mass (CPM) of 1461.40 ± 256.15 µg/cm<sup>2</sup>, compared to 267.57 ± 41.74 µg/cm<sup>2</sup> for the control. RMF 50 Hz also maximized steady-state flux (J<sub>SS</sub>) and permeability coefficient (K<sub>P</sub>), highlighting its potential for enhanced transdermal delivery. Conversely, static magnetic fields with negative polarization reduced permeation, showing a complex interaction between magnetic fields and skin permeability. The study also found that RMF treatments lowered NAP skin accumulation, improving permeation efficiency. Physicochemical analyses (FTIR, XRD, solubility, and lipophilicity) revealed that while EMF exposure did not significantly change NAP’s crystal structure, it did affect solubility and partition coefficient. This research highlights the potential of optimizing EMF parameters to enhance transdermal drug delivery and provides insights into the physicochemical interactions between EMFs and active compounds. The findings suggest that rotating magnetic fields, particularly at 50 Hz, offer the most significant improvement in drug permeability, which could be beneficial for developing advanced transdermal delivery systems.</div></div>","PeriodicalId":12024,"journal":{"name":"European Journal of Pharmaceutics and Biopharmaceutics","volume":"212 ","pages":"Article 114715"},"PeriodicalIF":4.4,"publicationDate":"2025-05-23","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144116408","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
Corrigendum to “Extracellular vesicles delivered rapamycin to improve the tumor microenvironment and enhance hepatocellular carcinoma immunotherapy” [Eur. J. Pharm. Biopharm. 211 (2025) 114714] “细胞外囊泡递送雷帕霉素改善肿瘤微环境和增强肝癌免疫治疗”的勘误表[欧洲]。j .制药。生物医学工程学报,2011(5):349 - 349。
IF 4.4 2区 医学
European Journal of Pharmaceutics and Biopharmaceutics Pub Date : 2025-05-22 DOI: 10.1016/j.ejpb.2025.114742
Jihua Tian , Huanyu Xu , Zhijie Ma , Jing Wang , Weihao Chen , Jingshu Chen , Qiuyue Sun , Ruiping Zhang
{"title":"Corrigendum to “Extracellular vesicles delivered rapamycin to improve the tumor microenvironment and enhance hepatocellular carcinoma immunotherapy” [Eur. J. Pharm. Biopharm. 211 (2025) 114714]","authors":"Jihua Tian ,&nbsp;Huanyu Xu ,&nbsp;Zhijie Ma ,&nbsp;Jing Wang ,&nbsp;Weihao Chen ,&nbsp;Jingshu Chen ,&nbsp;Qiuyue Sun ,&nbsp;Ruiping Zhang","doi":"10.1016/j.ejpb.2025.114742","DOIUrl":"10.1016/j.ejpb.2025.114742","url":null,"abstract":"","PeriodicalId":12024,"journal":{"name":"European Journal of Pharmaceutics and Biopharmaceutics","volume":"213 ","pages":"Article 114742"},"PeriodicalIF":4.4,"publicationDate":"2025-05-22","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144127004","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
Evaluation of monoclonal antibody formulation propensity for dripping at the filling nozzle tip end 单克隆抗体溶液滴注倾向的评价。
IF 4.4 2区 医学
European Journal of Pharmaceutics and Biopharmaceutics Pub Date : 2025-05-18 DOI: 10.1016/j.ejpb.2025.114746
Sébastien Dasnoy , Lubna Ouchrih El Ghali , Jade Eyuka M’Bembe , Chaimaa Hidan , Manon Favart , Claude Peerboom
{"title":"Evaluation of monoclonal antibody formulation propensity for dripping at the filling nozzle tip end","authors":"Sébastien Dasnoy ,&nbsp;Lubna Ouchrih El Ghali ,&nbsp;Jade Eyuka M’Bembe ,&nbsp;Chaimaa Hidan ,&nbsp;Manon Favart ,&nbsp;Claude Peerboom","doi":"10.1016/j.ejpb.2025.114746","DOIUrl":"10.1016/j.ejpb.2025.114746","url":null,"abstract":"<div><div>Nonionic surfactants are commonly used as excipients in monoclonal antibody formulations. The interfacial activity of surfactants may contribute to the elongation of solution droplets at the filling nozzle tip end, leading to dripping that may impact dose accuracy and process consistency. Axisymmetric drop shape analysis was used to evaluate the propensity of monoclonal antibody solution droplets for elongation in the presence of a nonionic surfactant (polysorbate 20, polysorbate 80, poloxamer 188, Brij®<!--> <!-->35, Brij®<!--> <!-->58 or FM1000). A droplet was created using a syringe and dosing needle, or a pump and filling nozzle. Droplet elongation rate was defined as the slope of a linear regression of droplet interfacial surface area over time. An increase in elongation rate led to a quicker occurrence of droplet pinch-off, meaning a higher propensity for dripping. Elongation rate increased with both initial droplet volume and surfactant concentration. The evolution of elongation rate with initial droplet volume provided some insights into interface stretching capacity. We propose droplet elongation rate as an indicator of monoclonal antibody formulation propensity for dripping.</div></div>","PeriodicalId":12024,"journal":{"name":"European Journal of Pharmaceutics and Biopharmaceutics","volume":"213 ","pages":"Article 114746"},"PeriodicalIF":4.4,"publicationDate":"2025-05-18","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144110168","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
Spray freeze drying as a novel drying process for the formulation of probiotic powders containing Lacticaseibacillus rhamnosus GG 喷雾冷冻干燥是制备鼠李糖乳杆菌GG益生菌粉的一种新型干燥工艺
IF 4.4 2区 医学
European Journal of Pharmaceutics and Biopharmaceutics Pub Date : 2025-05-18 DOI: 10.1016/j.ejpb.2025.114748
A. Steegmans , M. Plitzko , B. Luy , S. Lebeer , F. Kiekens
{"title":"Spray freeze drying as a novel drying process for the formulation of probiotic powders containing Lacticaseibacillus rhamnosus GG","authors":"A. Steegmans ,&nbsp;M. Plitzko ,&nbsp;B. Luy ,&nbsp;S. Lebeer ,&nbsp;F. Kiekens","doi":"10.1016/j.ejpb.2025.114748","DOIUrl":"10.1016/j.ejpb.2025.114748","url":null,"abstract":"<div><div>Spray freeze drying was evaluated as a drying process for the formulation and stabilization of probiotic powders This technology combines spray freezing into cold vapour followed by rotational bulk freeze drying, and was investigated to combine the benefits of both spray drying and freeze-drying. What sets this system apart from other studies using this technology, is that the feed suspension was sprayed into cooled atmosphere instead of spraying directly into liquid nitrogen. To ensure droplet formation, a rather more dripping than spraying technique known as laminar jet break up is used, whereas other spray freeze drying techniques use binary nozzles, single fluid pressure nozzles, ultrasonic nozzles or rotary nozzles. Moreover, the principles of rotatory freeze-drying were used for bulk lyophilization which results in freeze dried microparticles instead of a freeze dried cake. This study examined the parameters related to the spraying head and their impact on bacterial viability and powder particle size. Secondly, the feasibility of dynamic lyophilization by applying rotary freeze drying to the frozen substrate was studied. Furthermore, the powder density, flow and hygroscopic properties were monitored to assess the downstream processability for industrial manufacturing. Cell reduction of at least 1,0 log CFU/g was reported, with a maximum remaining cell concentration of 7,4 log CFU/g in the dried product. The particle size of the almost perfect microspheres ranged from 532 ± 35 µm using a 300 µm nozzle orifice and 739 ± 57 µm using a 400 µm nozzle orifice with a mean sphericity of 0,97. Hygroscopicity investigations reported a critical point at 40 % relative humidity where collapse of the microspheres occurred. The overall process yield was 92,1 ± 4,2 % on average.</div></div>","PeriodicalId":12024,"journal":{"name":"European Journal of Pharmaceutics and Biopharmaceutics","volume":"212 ","pages":"Article 114748"},"PeriodicalIF":4.4,"publicationDate":"2025-05-18","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144089318","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
Stabilising indocyanine green J-aggregate theranostics in biological milieu via liposomal envelopment 脂质体包膜在生物环境中稳定吲哚菁绿j聚集体的疗效。
IF 4.4 2区 医学
European Journal of Pharmaceutics and Biopharmaceutics Pub Date : 2025-05-14 DOI: 10.1016/j.ejpb.2025.114747
Hamoud Alotaibi , Taher Hatahet , Wafa’ T. Al-Jamal
{"title":"Stabilising indocyanine green J-aggregate theranostics in biological milieu via liposomal envelopment","authors":"Hamoud Alotaibi ,&nbsp;Taher Hatahet ,&nbsp;Wafa’ T. Al-Jamal","doi":"10.1016/j.ejpb.2025.114747","DOIUrl":"10.1016/j.ejpb.2025.114747","url":null,"abstract":"<div><div>Indocyanine green (ICG) J-aggregate (IJA) is a self-assembled ICG with a red-shift absorption band, enabling better tissue penetration than the monomeric ICG. Despite its superior photoacoustic imaging capabilities and heating stability to ICG, IJA suffers from low optical stability in aqueous and biological media, jeopardising its biomedical applications. The present work focused on loading p-IJA into liposomes to enhance its promising therapeutic and imaging applications. To optimise IJA loading into liposomes, we investigated the effect of lipid bilayer composition (lipid melting points, cholesterol, DSPE-PEG<sub>2000</sub>, and lipid charge) on the encapsulation of pre-formed IJA (p-IJA) into liposomes. Our findings showed the significance of high melting point lipids, high cholesterol, and DSPE-PEG<sub>2000</sub> contents for persevering p-IJA following loading into liposomes. Moreover, low percentages (∼5 mol %) of positively charged (DOTAP) or negatively charged (DSPG) lipids could still be incorporated into our liposomes without affecting p-IJA loading. Promisingly, p-IJA-liposomes enhanced p-IJA optical stability in a range of biological media, such as serum proteins, blood and collagen. Finally, lyophilised p-IJA-liposomes for long-term storage were successfully prepared. The present study solely focused on evaluating the enhanced photothermal stability of p-IJA following liposome envelopment. Nevertheless, our lipid-enveloped p-IJA could offer a biodegradable and stable platform for multimodal applications, including photoacoustic imaging, photothermal therapy (PTT), photodynamic (PDT), nanobubble-mediated ablation, and combination therapy with chemotherapeutics agents.</div></div>","PeriodicalId":12024,"journal":{"name":"European Journal of Pharmaceutics and Biopharmaceutics","volume":"213 ","pages":"Article 114747"},"PeriodicalIF":4.4,"publicationDate":"2025-05-14","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144086144","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
Influence of tear fluid properties on physicochemical, mucoadhesion and ocular penetration characteristics of transfersomes 泪液性质对转移体理化、黏附及眼内渗透特性的影响。
IF 4.4 2区 医学
European Journal of Pharmaceutics and Biopharmaceutics Pub Date : 2025-05-11 DOI: 10.1016/j.ejpb.2025.114745
Santosh Bhujbal , Priyanka Agarwal , Soma Sengupta , Cornelia M. Keck , Ilva D. Rupenthal
{"title":"Influence of tear fluid properties on physicochemical, mucoadhesion and ocular penetration characteristics of transfersomes","authors":"Santosh Bhujbal ,&nbsp;Priyanka Agarwal ,&nbsp;Soma Sengupta ,&nbsp;Cornelia M. Keck ,&nbsp;Ilva D. Rupenthal","doi":"10.1016/j.ejpb.2025.114745","DOIUrl":"10.1016/j.ejpb.2025.114745","url":null,"abstract":"<div><div>Due to changes in the tear fluid properties in dry eye disease (DED), eye drop performance may be altered. This study investigated the impact of tear fluid properties on the physicochemical, mucoadhesion and ocular penetration characteristics of transfersome (TFS) eye drops. Specifically, the effect of tear fluid pH and osmolarity on vesicle size, polydispersibility index (PDI) and zeta potential (ZP) of unloaded as well as curcumin- and tonabersat-loaded TFS were studied. Finally, the effect of altered tear fluid properties on corneal penetration of curcumin TFS was investigated using ex vivo porcine corneo-scleral discs. A significant increase in vesicle size and PDI was observed for curcumin and tonabersat TFS suspended in healthy and DED tears compared to water. Moreover, the ZP measured in water shifted towards neutral in the case of healthy and DED tears, suggesting reduced electrostatic stability of the vesicles. Deeper tissue penetration was observed for curcumin TFS suspended in water compared to TFS suspended in healthy tears, with significantly less penetration for TFS mixed with DED tears. This study confirmed that tear fluid properties significantly influence TFS characteristics and thus their penetration ability, highlighting the importance of evaluating ocular drug delivery systems under physiological conditions that reflect the disease state.</div></div>","PeriodicalId":12024,"journal":{"name":"European Journal of Pharmaceutics and Biopharmaceutics","volume":"212 ","pages":"Article 114745"},"PeriodicalIF":4.4,"publicationDate":"2025-05-11","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143984596","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
Small milk-derived extracellular vesicles: Suitable vehicles for oral drug delivery? 乳源性细胞外小泡:口服给药的合适载体?
IF 4.4 2区 医学
European Journal of Pharmaceutics and Biopharmaceutics Pub Date : 2025-05-10 DOI: 10.1016/j.ejpb.2025.114744
Nidhi Seegobin , Marissa Taub , Cécile Vignal , Christophe Waxin , Victoria Chris , Atheer Awad , Sudaxshina Murdan , Abdul W Basit
{"title":"Small milk-derived extracellular vesicles: Suitable vehicles for oral drug delivery?","authors":"Nidhi Seegobin ,&nbsp;Marissa Taub ,&nbsp;Cécile Vignal ,&nbsp;Christophe Waxin ,&nbsp;Victoria Chris ,&nbsp;Atheer Awad ,&nbsp;Sudaxshina Murdan ,&nbsp;Abdul W Basit","doi":"10.1016/j.ejpb.2025.114744","DOIUrl":"10.1016/j.ejpb.2025.114744","url":null,"abstract":"<div><div>Current treatments for inflammatory bowel disease often fail due to systemic side effects, but bovine milk-derived extracellular vesicles (EVs) show promise for targeted delivery to inflamed gut tissue via the leaky gut effect. This study assessed the stability of EVs as drug carriers in simulated gastrointestinal (GI) fluids and their efficacy in a colitis mouse model. EVs were characterised after incubation in PBS at various pH levels, and their lipid bilayer stability in biorelevant GI fluids was evaluated using the polar probe laurdan. Two small molecules, acridine orange (lipophilic) and riboflavin (hydrophilic), were loaded into EVs to test their release under GI conditions, while unloaded EVs were investigated for therapeutic effect via oral gavage or rectal enema in a colitis mouse model. Although no significant changes in EVs’ physical properties were observed at different pH levels, lipid bilayer damage was evident in acidic (p ≤ 0.05) and enzyme-rich environments (p ≤ 0.01). Acridine orange release was significant (p ≤ 0.05), but<!--> <!-->riboflavin remained encapsulated, and no therapeutic effect was observed with unloaded EVs <em>in vivo</em>. These results suggest that physical characterisation alone does not reflect EV stability, that bovine milk EVs have limited potential for oral drug delivery and are better suited for hydrophilic drugs.</div></div>","PeriodicalId":12024,"journal":{"name":"European Journal of Pharmaceutics and Biopharmaceutics","volume":"212 ","pages":"Article 114744"},"PeriodicalIF":4.4,"publicationDate":"2025-05-10","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143942524","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
Ceftriaxone-loaded albumin-based nanoparticles incorporated into in situ ionic sensitive nasal gels: Development, characterization, and nasal drug deposition studies 负载头孢曲松的白蛋白纳米颗粒纳入原位离子敏感鼻腔凝胶:开发、表征和鼻腔药物沉积研究
IF 4.4 2区 医学
European Journal of Pharmaceutics and Biopharmaceutics Pub Date : 2025-05-09 DOI: 10.1016/j.ejpb.2025.114743
Sandra Aulia Mardikasari , Gábor Katona , Laura Nižić Nodilo , Anita Hafner , Livije Kalogjera , Dijana Zadravec , László Orosz , Katalin Burian , György Tibor Balogh , Ildikó Csóka
{"title":"Ceftriaxone-loaded albumin-based nanoparticles incorporated into in situ ionic sensitive nasal gels: Development, characterization, and nasal drug deposition studies","authors":"Sandra Aulia Mardikasari ,&nbsp;Gábor Katona ,&nbsp;Laura Nižić Nodilo ,&nbsp;Anita Hafner ,&nbsp;Livije Kalogjera ,&nbsp;Dijana Zadravec ,&nbsp;László Orosz ,&nbsp;Katalin Burian ,&nbsp;György Tibor Balogh ,&nbsp;Ildikó Csóka","doi":"10.1016/j.ejpb.2025.114743","DOIUrl":"10.1016/j.ejpb.2025.114743","url":null,"abstract":"<div><div>Ceftriaxone (CFT) is recommended as the drug of choice for the empirical treatment of bacterial meningitis. However, conventional drug delivery has difficulty in crossing the blood–brain barrier (BBB), leading to insufficient therapeutic efficacy. Therefore, nasal drug administration emerged as a viable strategy, providing the opportunity for brain-targeted delivery to reach effective brain concentrations. In this work, we present the development of <em>in situ</em> nasal gels of CFT-loaded albumin nanoparticles for nose-to-brain delivery. The obtained formulations were characterized in terms of particle size, zeta potential, entrapment efficiency, expansion coefficient, droplet size distribution, <em>in vitro</em> drug release, permeability assay, nasal deposition studies, and antibacterial activities. The BBB-PAMPA permeability assay showed that the <em>in situ</em> nasal gels CFT formulation with 0.2% gellan gum (CFT-GG0.2%) has the highest permeation flux of all. Moreover, nasal deposition studies utilizing a 3D-printed human nasal cavity model revealed that CFT-GG0.2% was able to provide higher CFT concentration in the olfactory area. Interestingly, the developed <em>in situ</em> nasal gels formulation could successfully retain the antibacterial activities of CFT against <em>S. agalactiae, H. influenzae,</em> and <em>N. meningitidis</em>. Altogether, the <em>in situ</em> nasal gels formulation has the potential as a suitable delivery platform for CFT administration through the nose-to-brain delivery pathway.</div></div>","PeriodicalId":12024,"journal":{"name":"European Journal of Pharmaceutics and Biopharmaceutics","volume":"212 ","pages":"Article 114743"},"PeriodicalIF":4.4,"publicationDate":"2025-05-09","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143947489","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}
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