European Journal of Pharmaceutics and Biopharmaceutics最新文献_第2页

Development and application of a novel tracer system for the evaluation of temperature exposure of lipid nanoparticles in spray drying and dual centrifugation 一种新型示踪系统的开发和应用，用于评估喷雾干燥和双重离心中脂质纳米颗粒的温度暴露。

IF 4.3 2区医学

European Journal of Pharmaceutics and Biopharmaceutics Pub Date : 2025-10-06 DOI: 10.1016/j.ejpb.2025.114889

Isabelle Klein, Denise Steiner

{"title":"Development and application of a novel tracer system for the evaluation of temperature exposure of lipid nanoparticles in spray drying and dual centrifugation","authors":"Isabelle Klein, Denise Steiner","doi":"10.1016/j.ejpb.2025.114889","DOIUrl":"10.1016/j.ejpb.2025.114889","url":null,"abstract":"<div><div>In recent years, the development of nanocarriers and nanoscale drug delivery systems has become increasingly important, with temperature-intensive processes being an essential part of their preparation and following process steps.</div><div>This study introduced a novel nanoparticular tracer system to track the highest temperatures to which the particles are exposed to during processing by exploiting the monotropic polymorphism of triglycerides. These nanoparticulate systems enabled an estimation of the temperature exposure of formulations in processes that are otherwise inaccessible or very difficult to access. Two tracer systems were developed using the solid lipids tristearin and tripalmitin, with distinct melting temperatures, and applied for the high-energy processes of spray drying and dual centrifugation. In addition, the experiments provided insights into the effect of stabilizers on triglyceride modifications. It was shown that during spray drying, the highest temperature exposure of the nanoparticles during the process was 4.1 °C and 6.6 °C for tristearin and tripalmitin, respectively, above the outlet air temperature of the spray dryer. In addition, the tristearin tracer system was used to investigate the temperature exposure during dual centrifugation, which indicated that with increasing process time of up to 480 min, all particles were progressively exposed to temperatures above their melting temperature.</div></div>","PeriodicalId":12024,"journal":{"name":"European Journal of Pharmaceutics and Biopharmaceutics","volume":"217 ","pages":"Article 114889"},"PeriodicalIF":4.3,"publicationDate":"2025-10-06","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145250539","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

Design-of-experiments based development and in vitro evaluation of a cationic lipid-based triple adjuvanted subunit pertussis vaccine 基于实验设计的基于阳离子脂质的三联佐剂百日咳疫苗的研制和体外评价。

IF 4.3 2区医学

European Journal of Pharmaceutics and Biopharmaceutics Pub Date : 2025-10-03 DOI: 10.1016/j.ejpb.2025.114890

Tavonga T. Mandava , Volker Gerdts , Maryam Ejlali , Ellen K. Wasan

{"title":"Design-of-experiments based development and in vitro evaluation of a cationic lipid-based triple adjuvanted subunit pertussis vaccine","authors":"Tavonga T. Mandava , Volker Gerdts , Maryam Ejlali , Ellen K. Wasan","doi":"10.1016/j.ejpb.2025.114890","DOIUrl":"10.1016/j.ejpb.2025.114890","url":null,"abstract":"<div><div>The use of a cationic lipid nanoparticle based triple adjuvant complex (L-TriAdj) was previously demonstrated to provide great utility in enhancing local intranasal immunity against pertussis. However, the role of lipid composition as a critical product parameter has not been fully elucidated. The aim of this study was to optimize the lipid composition of L-TriAdj using design-of-experiments methodology, and to define the role of lipid composition on the physicochemical properties and in vitro behavior (cellular viability, uptake and cytokine expression) of L-TriAdj pertussis vaccine formulations applied to antigen presenting cells. L-TriAdj formulations were prepared using a thin-film hydration and extrusion method, with admixing of the adjuvant components and antigens. In-vitro experiments were conducted using the MTT assay, confocal imaging and flow cytometry. The DoE approach was used to optimize L-TriAdj vaccine formulations to particle sizes less than 200 nm. Results indicated that increasing the alkyl chain length of phosphatidylcholine (PC) lipids was associated with significant changes in cellular viability, enhancement of cellular uptake and induction of IL-12 and IFN-γ. Varying the ratio between phosphoethanolamine and phosphatidylcholine lipids was associated with significant changes in cellular viability and uptake; however, no significant effects in dendritic cell maturation were noted.</div></div>","PeriodicalId":12024,"journal":{"name":"European Journal of Pharmaceutics and Biopharmaceutics","volume":"217 ","pages":"Article 114890"},"PeriodicalIF":4.3,"publicationDate":"2025-10-03","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145231845","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

A new biocompatible butyric acid-releasing glucosamine derivative for transdermal delivery. 一种新的生物相容性的经皮释放丁酸葡萄糖胺衍生物。

IF 4.3 2区医学

European Journal of Pharmaceutics and Biopharmaceutics Pub Date : 2025-10-01 Epub Date: 2025-08-05 DOI: 10.1016/j.ejpb.2025.114832

Marica Erminia Schiano, Ritamaria Di Lorenzo, Teresa Di Serio, Loretta Lazzarato, Barbara Rolando, Konstantin Chegaev, Elisabetta Marini, Chiara Billi, Mariarosaria Cuozzo, Fabiana Filogamo, Stefania Albrizio, Carlo Irace, Maria Grazia Ferraro, Marialuisa Piccolo, Federica Sodano, Maria Grazia Rimoli, Sonia Laneri

{"title":"A new biocompatible butyric acid-releasing glucosamine derivative for transdermal delivery.","authors":"Marica Erminia Schiano, Ritamaria Di Lorenzo, Teresa Di Serio, Loretta Lazzarato, Barbara Rolando, Konstantin Chegaev, Elisabetta Marini, Chiara Billi, Mariarosaria Cuozzo, Fabiana Filogamo, Stefania Albrizio, Carlo Irace, Maria Grazia Ferraro, Marialuisa Piccolo, Federica Sodano, Maria Grazia Rimoli, Sonia Laneri","doi":"10.1016/j.ejpb.2025.114832","DOIUrl":"10.1016/j.ejpb.2025.114832","url":null,"abstract":"<p><p>The carrier prodrug approach is a well-established medicinal chemistry strategy adopted to refine the physicochemical and biopharmaceutical properties of parent drugs. In the present work, this strategy was applied to improve the transdermal delivery of butyric acid (BA) by employing D-glucosamine (N-Glc), a natural and non-toxic molecule, as a carrier. Accordingly, the design and synthesis of a new carrier prodrug, N-glucosamine tetrabutyrate (3-amino-6-((butyryloxy)methyl)tetrahydro-2H-pyran-2,4,5-triyl tributyrate, N-Glc-BE) is reported. The physicochemical profile of N-Glc-BE was comprehensively evaluated, including its chemical and enzymatic stability under different pH conditions and in human serum, as well as its lipophilicity and solubility. N-Glc-BE exhibited chemical stability across a wide pH range but underwent enzymatic hydrolysis in the presence of esterase, with a half-life of 8 min in human serum. The prodrug also showed favorable solubility and lipophilicity for transdermal application. Skin permeation studies using Franz diffusion cells demonstrated that N-Glc-BE primarily accumulated in the epidermis and dermis and gradually reached the receptor compartment, allowing sustained release of the parent compound, BA. Furthermore, N-Glc-BE was shown to be biocompatible in preclinical human skin models, including primary skin cell cultures. In conclusion, the novel, odorless prodrug N-Glc-BE represents a promising candidate for the transdermal delivery of BA, a molecule with recognized biological activity but poor physicochemical properties. The use of N-Glc as a carrier not only provides a non-toxic delivery platform but also capitalizes on its kwon role in skin health and function.</p>","PeriodicalId":12024,"journal":{"name":"European Journal of Pharmaceutics and Biopharmaceutics","volume":" ","pages":"114832"},"PeriodicalIF":4.3,"publicationDate":"2025-10-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144783856","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

Degradable glycyrrhetinic acid functionalized mesoporous silica nanoparticles enhanced liver cancer therapy 可降解甘草次酸功能化介孔二氧化硅纳米颗粒增强肝癌治疗。

IF 4.3 2区医学

European Journal of Pharmaceutics and Biopharmaceutics Pub Date : 2025-09-30 DOI: 10.1016/j.ejpb.2025.114880

Zhenhua Li , Junjie Zhang , Chuanyong Fan , Kaifang Wu , Jiaping Liu , Yaru Zhang , Zehao Dong , Fang Dong , Lu Xu

引用次数: 0

Polystyrene beads for efficient temperature control and drug nanoparticle production in wet stirred media milling 聚苯乙烯珠有效的温度控制和药物纳米颗粒生产在湿搅拌介质研磨。

IF 4.3 2区医学

European Journal of Pharmaceutics and Biopharmaceutics Pub Date : 2025-09-30 DOI: 10.1016/j.ejpb.2025.114879

Hamidreza Heidari , Wren McAleer , Gulenay Guner , Donald J. Clancy , Ecevit Bilgili

{"title":"Polystyrene beads for efficient temperature control and drug nanoparticle production in wet stirred media milling","authors":"Hamidreza Heidari , Wren McAleer , Gulenay Guner , Donald J. Clancy , Ecevit Bilgili","doi":"10.1016/j.ejpb.2025.114879","DOIUrl":"10.1016/j.ejpb.2025.114879","url":null,"abstract":"<div><div>This study explores the effects of stirrer speed, bead loading, and bead size on the evolution of mill outlet temperature during the wet stirred media milling (WSMM) of fenofibrate suspensions using crosslinked polystyrene (CPS) beads. Key parameters, including mill outlet temperature, particle size, suspension viscosity, and power consumption, were systematically measured. Power-law correlations were established to link the normalized temperature rise and power consumption with process parameters, revealing that stirrer speed exerts the greatest influence on both metrics, followed by bead loading and size. Notably, all milling runs, even under the highest power density conditions, were completed in a single cycle, eliminating the need for intermittent milling. The maximum temperature rise observed was 25 °C. Moreover, a microhydrodynamic (MHD) model was developed to investigate the influence of process parameters on MHD metrics, establishing correlations between median particle size, dimensionless temperature, and MHD parameters. The results demonstrated that an increased average frequency of particle compression is directly associated with higher temperature rise and finer particle sizes, underscoring the role of MHD parameters in governing thermal behavior and particle size reduction. Furthermore, comparison with yttrium-stabilized zirconia (YSZ) beads showed that CPS beads generated significantly lower heat while achieving comparable particle size reductions, making them particularly advantageous for milling thermally labile drugs. This study highlights the suitability of CPS beads for efficient and controlled WSMM, providing a promising alternative to YSZ beads for applications requiring stringent temperature control.</div></div>","PeriodicalId":12024,"journal":{"name":"European Journal of Pharmaceutics and Biopharmaceutics","volume":"217 ","pages":"Article 114879"},"PeriodicalIF":4.3,"publicationDate":"2025-09-30","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145212109","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

About the impact of hydrophilic organic solvents on the emulsifying properties of self-emulsifying drug delivery systems (SEDDS) 研究了亲水有机溶剂对自乳化给药系统乳化性能的影响。

IF 4.3 2区医学

European Journal of Pharmaceutics and Biopharmaceutics Pub Date : 2025-09-29 DOI: 10.1016/j.ejpb.2025.114877

Ahmad Saleh , Khush Bakhat Afzal , Florina Veider , Soheil Haddadzadegan , Andreas Bernkop-Schnürch

{"title":"About the impact of hydrophilic organic solvents on the emulsifying properties of self-emulsifying drug delivery systems (SEDDS)","authors":"Ahmad Saleh , Khush Bakhat Afzal , Florina Veider , Soheil Haddadzadegan , Andreas Bernkop-Schnürch","doi":"10.1016/j.ejpb.2025.114877","DOIUrl":"10.1016/j.ejpb.2025.114877","url":null,"abstract":"<div><div>This study presents the first comprehensive evidence that hydrophilic organic solvents markedly accelerate SEDDS emulsification under biorelevant conditions, while maintaining both stability and safety. These findings establish their critical role as functional excipients in the development of advanced oral lipid-based drug delivery systems. Three different hydrophilic organic solvents benzyl alcohol, ethanol and propylene glycol were incorporated into self-emulsifying drug delivery systems (SEDDS). The emulsification time of SEDDS, with and without these solvents, was evaluated in various media, including demineralized water and HEPES buffer pH 5 and 7.5. Additionally, the stability of the formed oily droplets in the presence of bile salts was assessed based on their size distribution, polydispersity index (PDI), and zeta potential. Furthermore, membrane toxicity of the formulations was tested on human red blood cells (RBCs). Due to the incorporation of 30% benzyl alcohol, ethanol and propylene glycol, emulsification time was 12-fold, 8.2-fold and 5.6-fold accellerated, respectively. Furthermore, SEDDS containing the hydrophilic organic solvents benzyl alcohol and ethanol exhibited no significant change in size distribution, PDI and zeta potential when exposed to bile salts. SEDDS containing benzyl alcohol showed the lowest membrane damaging effect of all tested hydrophilic organic solvents. According to these results, the emulsifying properties of SEDDS can be significantly accellerated by the addition of hydrophilic organic solvents, with benzyl alcohol emerging as the most promising option.</div></div>","PeriodicalId":12024,"journal":{"name":"European Journal of Pharmaceutics and Biopharmaceutics","volume":"217 ","pages":"Article 114877"},"PeriodicalIF":4.3,"publicationDate":"2025-09-29","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145206016","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

Poly(vinyl alcohol) cryogels: Effect size of polymer concentration, number of cycles and thawing rate on material properties and dermal drug delivery 聚乙烯醇低温冰箱：聚合物浓度、循环次数和解冻速率对材料性能和皮肤给药的影响大小。

IF 4.3 2区医学

European Journal of Pharmaceutics and Biopharmaceutics Pub Date : 2025-09-28 DOI: 10.1016/j.ejpb.2025.114876

Y. Wiedemann , T. Schmitt , S. Kim , K. Dirnberger , S. Ludwigs , D.J. Lunter

{"title":"Poly(vinyl alcohol) cryogels: Effect size of polymer concentration, number of cycles and thawing rate on material properties and dermal drug delivery","authors":"Y. Wiedemann , T. Schmitt , S. Kim , K. Dirnberger , S. Ludwigs , D.J. Lunter","doi":"10.1016/j.ejpb.2025.114876","DOIUrl":"10.1016/j.ejpb.2025.114876","url":null,"abstract":"<div><div>Poly(vinyl alcohol) (PVA) can be physically cross-linked by repeated freeze–thaw (F-T) cycles, resulting in a cryogel. Despite the growing prevalence of the cryogelation process in the scientific literature, its multivariable nature, particularly the individual and synergistic impact of process variables on material properties, remains under-explored. The present work is the first systematic analysis quantifying the effect sizes associated with the influence of the key process parameters polymer concentration, number of cycles and thawing rates within F-T-cycles on the material properties of PVA cryogels as a drug delivery system for dermal applications. The variables analysed showed both positive and negative correlations with Young’s modulus, gel strength and calculated mesh sizes of the polymer network to varying degrees. Moreover, it uniquely demonstrates the synergistic combination effects between individual process parameters, revealing mutual influences, that had not been characterized systematically before. The excellent suitability as a dermal drug delivery system was also demonstrated by both comparative drug release and drug permeation through the skin using diclofenac sodium as a model drug. Overall, this study provides the first systematic understanding of the impact of cryogelation process parameters on material properties and introduces a new and simple approach to individual selection of specific cryogelation conditions.</div></div>","PeriodicalId":12024,"journal":{"name":"European Journal of Pharmaceutics and Biopharmaceutics","volume":"217 ","pages":"Article 114876"},"PeriodicalIF":4.3,"publicationDate":"2025-09-28","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145198961","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

Rutin/ZnO/mesoporous Silica-based Nano-hydrogel accelerated topical wound healing in albino mice via potential synergistic bioactive response 芦丁/ZnO/介孔硅基纳米水凝胶通过潜在的协同生物活性反应加速白化小鼠局部伤口愈合。

IF 4.3 2区医学

European Journal of Pharmaceutics and Biopharmaceutics Pub Date : 2025-09-25 DOI: 10.1016/j.ejpb.2025.114875

Huma Butt , Haji Muhammad Shoaib Khan , Muhammad Sohail , Amina Izhar , Farhan Siddique , Maryam Bashir , Usman Aftab , Hasnain Shaukat

{"title":"Rutin/ZnO/mesoporous Silica-based Nano-hydrogel accelerated topical wound healing in albino mice via potential synergistic bioactive response","authors":"Huma Butt , Haji Muhammad Shoaib Khan , Muhammad Sohail , Amina Izhar , Farhan Siddique , Maryam Bashir , Usman Aftab , Hasnain Shaukat","doi":"10.1016/j.ejpb.2025.114875","DOIUrl":"10.1016/j.ejpb.2025.114875","url":null,"abstract":"<div><div>Burn wounds are the leading cause of accidental topical injuries. To avoid the chances of delayed healing and microbial infiltration, treating the wound with a potent antimicrobial and anti-inflammatory topical formulation is mandatory. The optimized Z-R/MSN gel was fabricated using a novel blend of rutin-loaded mesoporous silica nanoparticles and zinc oxide, using Design Expert software to augment topical wound healing. The <em>in silico</em> molecular docking of Rutin-ZnO molecular complex presented H-bonding interactions with amino acid residues LYS183 of the catalytic loop and amino acid ASP200 of the DFG motif, with a bond distance ranging from 3.01 Å to 3.32 Å. Moreover, the hydrophobic interactions with ASP133, TYR134, and ASN186 contributed to the significant inhibition of enzyme activity with a G-score of −8.7 kcal/mol. Topical application of Z-R/MSN gel has shown significant wound contraction (98.35 % ± 0.03) in albino mice models compared to blank gel (60.67 % ± 0.06). Zones of inhibition exhibited by Z-R/MSN for <em>Klebsiella</em> spp., <em>S. aureus</em>, <em>P. aeruginosa</em>, and <em>E. coli</em> were 29.21 mm ± 2.39, 29.27 mm ± 1.83, 29.69 mm ± 2.68, and 33.14 mm ± 2.23, respectively. This research proved that Z-R/MSN gel accelerated topical wound-healing and provided robust antimicrobial protection to the wound. Further investigations on this innovative formulation may expand its commercial applications in clinical dermatology.</div></div>","PeriodicalId":12024,"journal":{"name":"European Journal of Pharmaceutics and Biopharmaceutics","volume":"216 ","pages":"Article 114875"},"PeriodicalIF":4.3,"publicationDate":"2025-09-25","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145181894","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

Development of in vitro-in vivo correlation for establishing patient-centric quality standards of dissolution for lamotrigine extended-release tablets 建立以患者为中心的拉莫三嗪缓释片溶出度质量标准的体内外相关性研究进展。

IF 4.3 2区医学

European Journal of Pharmaceutics and Biopharmaceutics Pub Date : 2025-09-23 DOI: 10.1016/j.ejpb.2025.114874

Ahmed Zidan , Abu Bakar Siddique , Maha Shaklah , Om Anand , Thomas O’Connor , Muhammad Ashraf

{"title":"Development of in vitro-in vivo correlation for establishing patient-centric quality standards of dissolution for lamotrigine extended-release tablets","authors":"Ahmed Zidan , Abu Bakar Siddique , Maha Shaklah , Om Anand , Thomas O’Connor , Muhammad Ashraf","doi":"10.1016/j.ejpb.2025.114874","DOIUrl":"10.1016/j.ejpb.2025.114874","url":null,"abstract":"<div><div>In vitro-in vivo correlation (IVIVC) studies have been commonly used for assessing the impact of formulation and manufacturing changes on drug performance. The current study developed an IVIVC to establish patient-centric quality standards (PCQS) for dissolution using lamotrigine extended release (ER) 300 mg tablets as model formulation. Dissolution of Lamotrigine ER tablets was tested using various dissolution apparatus (USP II & III), dissolution media (biorelevant, non-bio relevant), media composition, pH, and hydrodynamics. The plasma lamotrigine concentration time profiles following oral administration were simulated using a physiologically based pharmacokinetic (PBPK) model. This PBPK model was developed and verified using plasma lamotrigine profiles following administration of lamotrigine intravenous (IV) solution and oral immediate-release (IR) tablets. Model verification results showed accurate prediction of Cmax and AUC following IV and IR lamotrigine administration with confidence level exceeding 95 %. Various IVIVC models were investigated using dissolution data of fast, medium, and slow ER lamotrigine 300 mg tablets manufactured in-house. Optimal IVIVC models were obtained using a second order polynomial and a two-compartment Loo-Riegelman deconvolution. The results of IVIVC goodness of fit showed that the dissolution condition in standard compendial media using USP apparatus II established a Level A IVIVC. This IVIVC model passed both internal and external validation criteria. Using these dissolution conditions, a PCQS of ≤10 % release at 2 h, ≤45 % at 6 h, and ≥80 % at 18 h was derived. In conclusion, this study demonstrates that a PCQS for lamotrigine ER tablets dissolution can be established using verified PBPK and validated IVIVC model and offers a reliable approach for assessment of product performance.</div></div>","PeriodicalId":12024,"journal":{"name":"European Journal of Pharmaceutics and Biopharmaceutics","volume":"216 ","pages":"Article 114874"},"PeriodicalIF":4.3,"publicationDate":"2025-09-23","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145148282","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

Thermosensitive chitosan-oxidized dextran-β-glycerophosphate sodium injectable hydrogel for enhanced solubility and prolonged release of ethinylestradiol: a novel long-acting contraceptive platform 热敏壳聚糖氧化葡聚糖-β-甘油磷酸钠注射水凝胶增强溶解度和延长释放乙炔雌二醇：一个新的长效避孕平台。

IF 4.3 2区医学

European Journal of Pharmaceutics and Biopharmaceutics Pub Date : 2025-09-22 DOI: 10.1016/j.ejpb.2025.114872

Xuena Zhang , Fengqiang Zhang , Chongwei Yin , Juan Xu , Ting Wang

{"title":"Thermosensitive chitosan-oxidized dextran-β-glycerophosphate sodium injectable hydrogel for enhanced solubility and prolonged release of ethinylestradiol: a novel long-acting contraceptive platform","authors":"Xuena Zhang , Fengqiang Zhang , Chongwei Yin , Juan Xu , Ting Wang","doi":"10.1016/j.ejpb.2025.114872","DOIUrl":"10.1016/j.ejpb.2025.114872","url":null,"abstract":"<div><div>Ethinylestradiol (EE) is a clinically used estrogen with antifertility effects that is poorly water soluble, limiting bioavailability and preventing long-term release when administered orally. This study addresses these challenges through the development of a novel injectable thermosensitive hydrogel that both improves hydrophobic EE dispersion and enables sustained <em>in vivo</em> release, presenting significant potential for long-term contraception. Carboxymethyl-β-cyclodextrin (CM-β-CD) was synthesized to encapsulate EE, therebyenhancing its solubility and distribution in the hydrogel matrix. We found that hydrogels prepared by adding 0.5% (w/v) oxidized dextran (ODex) to the chitosan/sodium β-glycerophosphate (CS/ODex/β-GP) system exhibited mechanical strength favorable for cell growth compared to conventional CS/β-GP, resolved the problems of poor stability and mechanical strength of CS/β-GP hydrogels, and ensured effective retention and delivery <em>in vivo</em>. A 240h drug release study demonstrated the hydrogel’s ability to sustain release, highlighting its potential to prolong contraceptive efficacy. Biocompatibility testing showed cell viability in excess of 85%. FTIR and SEM characterization further confirmed the functional structure and morphology of the hydrogel. This thermosensitive injection system provides a promising platform for the long-term release of hydrophobic drugs such as EE,providingan innovative approach toextendedcontraceptivedelivery.</div></div>","PeriodicalId":12024,"journal":{"name":"European Journal of Pharmaceutics and Biopharmaceutics","volume":"216 ","pages":"Article 114872"},"PeriodicalIF":4.3,"publicationDate":"2025-09-22","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145136997","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