Journal of Drug Delivery Science and Technology最新文献

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Progress and prospects of synthetic antimicrobial polymers for the treatment of infectious diseases 合成抗微生物聚合物在传染病治疗中的进展与展望
IF 4.5 3区 医学
Journal of Drug Delivery Science and Technology Pub Date : 2025-06-01 DOI: 10.1016/j.jddst.2025.107126
Trinankita Pal , Bijaya Ghosh , Kaushik Mukherjee , Tapan Kumar Giri
{"title":"Progress and prospects of synthetic antimicrobial polymers for the treatment of infectious diseases","authors":"Trinankita Pal ,&nbsp;Bijaya Ghosh ,&nbsp;Kaushik Mukherjee ,&nbsp;Tapan Kumar Giri","doi":"10.1016/j.jddst.2025.107126","DOIUrl":"10.1016/j.jddst.2025.107126","url":null,"abstract":"<div><div>The dreaded bacterial diseases like meningitis, pneumonia, and tuberculosis are seeing a resurgence thanks to the development of antibiotic resistance. The precious antibiotics have been rendered ineffective due to their indiscriminate and widespread application. An innovative therapeutic solution is the need of the hour. As an answer to this demand, synthetic antimicrobial polymers (SAP) have surfaced as a viable alternative. Unlike natural products, the properties of SAP can be controlled by design. Wide-spread research using various approaches has created a plethora of SAP with customizable properties like broad-spectrum antimicrobial activity, low toxicity, and a high barrier to resistance, which could play a significant role in reducing reliance on traditional antibiotics. However, a summary of this progress is unavailable, and this article tries to fill the gaps. This review explores the current state of these polymers, emphasizing their mechanisms of action as well as their efficacy and offering insights into how these materials could transform the treatment of infectious diseases.</div></div>","PeriodicalId":15600,"journal":{"name":"Journal of Drug Delivery Science and Technology","volume":"111 ","pages":"Article 107126"},"PeriodicalIF":4.5,"publicationDate":"2025-06-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144204677","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}
引用次数: 0
Biomimetic hybrid vesicles for colorectal cancer targeting 结肠直肠癌靶向的仿生杂交囊泡
IF 4.5 3区 医学
Journal of Drug Delivery Science and Technology Pub Date : 2025-05-31 DOI: 10.1016/j.jddst.2025.107124
Alice Balboni , Giorgia Ailuno , Mathieu Repellin , Giuseppina Catania , Sara Baldassari , Andrea Petretto , Pierre Yves Dugas , Cédric Chaveroux , Gabriele Caviglioli , Giovanna Lollo
{"title":"Biomimetic hybrid vesicles for colorectal cancer targeting","authors":"Alice Balboni ,&nbsp;Giorgia Ailuno ,&nbsp;Mathieu Repellin ,&nbsp;Giuseppina Catania ,&nbsp;Sara Baldassari ,&nbsp;Andrea Petretto ,&nbsp;Pierre Yves Dugas ,&nbsp;Cédric Chaveroux ,&nbsp;Gabriele Caviglioli ,&nbsp;Giovanna Lollo","doi":"10.1016/j.jddst.2025.107124","DOIUrl":"10.1016/j.jddst.2025.107124","url":null,"abstract":"<div><div>The functionalization of nanosystems with cell-derived materials has been proposed as a promising strategy for targeted drug delivery. This approach combines high colloidal stability and low rate of clearance from the reticuloendothelial system, with a controlled preparation process. In this work, colorectal cancer cells from a murine cell line (CT26 cells) were used as cell membrane (CM) source for the preparation of biomimetic nanosystems intended for cancer cells targeting. The purification from residual genetic material from parent cells was assessed in the CM fraction and the retained protein profile was studied. CT26 CM were used to prepare vesicles, and combined with synthetic lipids at different protein:lipid ratios to obtain hybrids. CM and lipids were hybridized using two techniques: co-extrusion and hydrodynamic mixing using microfluidics. The obtained formulations were compared in terms of physicochemical properties, protein content and membrane hybridization. The insertion of artificial phospholipids in hybrid vesicles enabled to improve the production yield. The internalization and selectivity of biomimetic vesicles into parent cells compared to different cell types was assessed <em>in vitro</em>, likewise their biocompatibility in 2D and 3D cell cultures. The obtained results demonstrated that purified and stable bio-inspired nanosystems were developed with high throughput, evidencing the superiority of microfluidics in terms of material conservation and process standardization. Moreover, significantly improved cellular uptake of the developed systems was observed when compared to artificial liposomes, reaching the highest value in the homotypic internalization to parent cells.</div></div>","PeriodicalId":15600,"journal":{"name":"Journal of Drug Delivery Science and Technology","volume":"111 ","pages":"Article 107124"},"PeriodicalIF":4.5,"publicationDate":"2025-05-31","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144212279","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}
引用次数: 0
Nanofibrillated cellulose injectable implants loaded with Raloxifene hydrochloride and bioactive glass nanoparticles for bone regeneration: in-vitro and in-vivo study
IF 4.5 3区 医学
Journal of Drug Delivery Science and Technology Pub Date : 2025-05-31 DOI: 10.1016/j.jddst.2025.107083
Rabab Kamel , Sara A.M. El-Sayed , Mostafa Mabrouk , Hanan H. Behere , Nahla A. El-Wakil , Rehab F. Abdel-Rahman , Mohamed S. Amer , Nermeen A. Elkasabgy
{"title":"Nanofibrillated cellulose injectable implants loaded with Raloxifene hydrochloride and bioactive glass nanoparticles for bone regeneration: in-vitro and in-vivo study","authors":"Rabab Kamel ,&nbsp;Sara A.M. El-Sayed ,&nbsp;Mostafa Mabrouk ,&nbsp;Hanan H. Behere ,&nbsp;Nahla A. El-Wakil ,&nbsp;Rehab F. Abdel-Rahman ,&nbsp;Mohamed S. Amer ,&nbsp;Nermeen A. Elkasabgy","doi":"10.1016/j.jddst.2025.107083","DOIUrl":"10.1016/j.jddst.2025.107083","url":null,"abstract":"<div><div>Nanofibrillated cellulose (NFC) injectable implants loaded with raloxifene hydrochloride and bioactive glass (magnesium phosphate; MPh) for treating bone defects were prepared. MPh was prepared using a simple chemical precipitation method and characterized which showed its porous, amorphous nature and a particle size of 10–20 nm. Then, MPh was loaded in different concentrations in NFC/Poloxamer to formulate the implants. The flow rate values indicated acceptable injectability compared to Betolvex™. Adding MPh decreased the flow rate, with higher concentrations having slower flow rates. The drug release profiles of the formulations varied, with the addition of the highest MPh concentration (3 %w/v) sustaining the drug release up to 17 days. SEM images showed a porous dense matrix after contact with release medium. The healing power and rate of the formulation in male Albino rats with induced tibial bone defects were investigated. The macroscopic examination showed no signs of infection or osteolytic responses. The treated groups showed better healing compared to untreated group, with the double-dosed group exhibiting the fastest progress. Histopathological findings showed complete healing with the developed formulation particularly when double-dosed. Overall, the injectable implant provided enhanced bone healing through the synergistic actions of its components, especially when double-dosed.</div></div>","PeriodicalId":15600,"journal":{"name":"Journal of Drug Delivery Science and Technology","volume":"111 ","pages":"Article 107083"},"PeriodicalIF":4.5,"publicationDate":"2025-05-31","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144242904","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}
引用次数: 0
Nano-apatite with Doxycycline for pulp capping: A potential strategy to reduce inflammation and promote pulp healing 纳米磷灰石加强力霉素用于牙髓封盖:一种减少炎症和促进牙髓愈合的潜在策略
IF 4.5 3区 医学
Journal of Drug Delivery Science and Technology Pub Date : 2025-05-31 DOI: 10.1016/j.jddst.2025.107069
K.S. Balamurugan , T. Sangeetha , E. Ranjith Kumar , I. Pradeep , Vasudeva Reddy Minnam Reddy , Woo Kyoung Kim , Amanullah Fatehmulla
{"title":"Nano-apatite with Doxycycline for pulp capping: A potential strategy to reduce inflammation and promote pulp healing","authors":"K.S. Balamurugan ,&nbsp;T. Sangeetha ,&nbsp;E. Ranjith Kumar ,&nbsp;I. Pradeep ,&nbsp;Vasudeva Reddy Minnam Reddy ,&nbsp;Woo Kyoung Kim ,&nbsp;Amanullah Fatehmulla","doi":"10.1016/j.jddst.2025.107069","DOIUrl":"10.1016/j.jddst.2025.107069","url":null,"abstract":"<div><div>The aim of the study is to develop a specialist dental capping agent that is particularly formulated to target pulp inflammation. The study included the synthesis of nano-apatite using Lepidium sativum (nHALS) that was loaded with Doxycycline (nHALS@DXC) utilizing an in vitro model of pulpitis with an O-antigen (O-A). The nanoscale HALS were analysed using scanning electron microscopy (SEM) and Transmission electron microscopy (TEM) to assess their odontogenic properties. The diameter of the nHALS nanoparticles ranged from 20 to 33 nm in width and 80–170 nm in length. Doxycycline has been identified as an appropriate loading material for medicinal applications. While the effect of nHALS@DXC on the odontogenic competence of HDPSCs was not superior to that of nHALS alone, it exhibited a more significant anti-inflammatory effect. The findings indicate that nHALS@DXC has the capacity to serve as an effective agent for pulp capping, perhaps surpassing nHALS in terms of reducing inflammation and activating dental pup cells to enhance pulp repair after injury.</div></div>","PeriodicalId":15600,"journal":{"name":"Journal of Drug Delivery Science and Technology","volume":"111 ","pages":"Article 107069"},"PeriodicalIF":4.5,"publicationDate":"2025-05-31","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144242786","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}
引用次数: 0
Enhanced semaglutide bioavailability via spray freeze dried powder for inhalation: Unveiling safety and broad potential applications 通过喷雾冷冻干粉吸入提高西马鲁肽的生物利用度:揭示安全性和广泛的潜在应用
IF 4.5 3区 医学
Journal of Drug Delivery Science and Technology Pub Date : 2025-05-30 DOI: 10.1016/j.jddst.2025.107112
Riwei Yang , Kaiqi Shi , Qingzhen Zhang , Gang Yang , Shiyang Liu , Shuo Qi , Xiang Luo , Honglei Zhang , Zheng Wang , Fangyan Wang , Jesse Zhu
{"title":"Enhanced semaglutide bioavailability via spray freeze dried powder for inhalation: Unveiling safety and broad potential applications","authors":"Riwei Yang ,&nbsp;Kaiqi Shi ,&nbsp;Qingzhen Zhang ,&nbsp;Gang Yang ,&nbsp;Shiyang Liu ,&nbsp;Shuo Qi ,&nbsp;Xiang Luo ,&nbsp;Honglei Zhang ,&nbsp;Zheng Wang ,&nbsp;Fangyan Wang ,&nbsp;Jesse Zhu","doi":"10.1016/j.jddst.2025.107112","DOIUrl":"10.1016/j.jddst.2025.107112","url":null,"abstract":"<div><div>Semaglutide, a long-acting glucagon-like peptide-1 (GLP-1) analog, has been approved for blood glucose management in Type 2 diabetes (T2D) and obese patients. However, its clinical use is limited by poor oral bioavailability and suboptimal adherence to subcutaneous injections, highlighting the need for alternative delivery routes. In this study, we developed semaglutide dry powder for inhalation (sema-DPI) using spray drying (SD) and spray freeze drying (SFD) techniques, and evaluated their characteristics of particle and pharmacokinetics through modern preparation assessment methods. The results indicated that under similar parameters, SFD-sema-DPI exhibited a rougher particle surface compared to the SD-sema-DPI, which provided better aerodynamic performance. Additionally, SFD-sema showed prolonged plasma presence in rats and enhanced bioavailability. Furthermore, the inhalation safety of SFD-sema-DPI was evaluated in rats. Continuous inhalation at a dose of 4.1 mg/kg/day for 28 days did not produce any significant pulmonary or systemic lesions. Our findings suggest that SFD-sema-DPI may offer a superior alternative for T2D and obese patients.</div></div>","PeriodicalId":15600,"journal":{"name":"Journal of Drug Delivery Science and Technology","volume":"111 ","pages":"Article 107112"},"PeriodicalIF":4.5,"publicationDate":"2025-05-30","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144204679","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}
引用次数: 0
Engineering elastin-like polypeptides for polyphenol capture and permeation through an in vitro nasal mucosa barrier 工程弹性蛋白样多肽在体外鼻黏膜屏障中对多酚的捕获和渗透
IF 4.5 3区 医学
Journal of Drug Delivery Science and Technology Pub Date : 2025-05-30 DOI: 10.1016/j.jddst.2025.107119
Derek W. Nelson , Gianna M. Scire , Conrad H. Cheung , Vrushali Varude , Geraldine Quinones , Marvin Bentley , R. Helen Zha , Ryan J. Gilbert
{"title":"Engineering elastin-like polypeptides for polyphenol capture and permeation through an in vitro nasal mucosa barrier","authors":"Derek W. Nelson ,&nbsp;Gianna M. Scire ,&nbsp;Conrad H. Cheung ,&nbsp;Vrushali Varude ,&nbsp;Geraldine Quinones ,&nbsp;Marvin Bentley ,&nbsp;R. Helen Zha ,&nbsp;Ryan J. Gilbert","doi":"10.1016/j.jddst.2025.107119","DOIUrl":"10.1016/j.jddst.2025.107119","url":null,"abstract":"<div><div>Intranasal (IN) administration provides a potential drug delivery route to the brain without passing the blood-brain barrier, allowing for the delivery of larger therapeutics for diseases such as Alzheimer's disease (AD). However, effective IN administration is compromised by mucociliary clearance (MCC) and the use of complex formulations of thermo-gelling modalities to reduce MCC. This study uses biomimetic elastin-like polypeptides (ELPs) to gel at nasal passage temperatures, capture an AD-relevant polyphenol, vescalagin (VSG), and deliver VSG through a nasal mucosa model. First, a library of ELPs was produced bearing either tyrosine, phenylalanine, serine, or leucine guest residues. The phenyl-bearing ELPs elicit a physiologically relevant gelation temperature and have the best VSG drug binding, as determined by a pull-down assay. Next, a di-block ELP was produced with a tyrosine-bearing block for drug binding and phase separation and a leucine-bearing block that remains soluble and presents a polyarginine tag (10xR) for cell interaction. While the di-block ELP resulted in stable microgels compared to mono-block ELPs upon phase separation, adding the 10xR tag mitigated this stability, returning the di-block ELP to coalescence behavior. However, the 10xR tag elicited ELP interaction with RPMI cells, enhanced VSG accumulation at the cell-mucous surface of an in vitro nasal mucosa model, and increased VSG permeation compared to un-tagged ELP or VSG alone. Future work can use these findings to improve ELP design for IN applications and investigate in vivo efficacy.</div></div>","PeriodicalId":15600,"journal":{"name":"Journal of Drug Delivery Science and Technology","volume":"111 ","pages":"Article 107119"},"PeriodicalIF":4.5,"publicationDate":"2025-05-30","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144220884","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}
引用次数: 0
Advances in pH-Sensitive polymer-based Drug delivery systems for targeted therapy in ovarian Cancer: Focus on Olaparib 用于卵巢癌靶向治疗的ph敏感聚合物给药系统的进展:重点是奥拉帕尼
IF 4.5 3区 医学
Journal of Drug Delivery Science and Technology Pub Date : 2025-05-30 DOI: 10.1016/j.jddst.2025.107076
S. Nikitha, D. Manjula, Arfa Nasrine
{"title":"Advances in pH-Sensitive polymer-based Drug delivery systems for targeted therapy in ovarian Cancer: Focus on Olaparib","authors":"S. Nikitha,&nbsp;D. Manjula,&nbsp;Arfa Nasrine","doi":"10.1016/j.jddst.2025.107076","DOIUrl":"10.1016/j.jddst.2025.107076","url":null,"abstract":"<div><div>With an importance on OLA(Olaparib), this review scrutinizes the developments in pH-sensitive polymer-based drug delivery systems for targeted therapy in ovarian cancer(OC). The article studies the methods of increasing bioavailability and solubility of OLA using pH-sensitive polymers compared to traditional polymers. It describes the mechanisms of conjugation of OLA, provides examples of pH-sensitive polymers, the methods of their synthesis, the ways of functionalization and modification. This review describes how this drug, when integrated with nanotechnology using this pH-sensitive polymer, offers enhanced therapeutic effects by specifically targeting OC cells while reducing the systemic toxicity towards the normal cells, which surpasses the efficacy and toxicity of traditional forms like tablets, and capsules, while explaining how this system better overcomes medication resistance than available conventional forms. The paper discusses regulatory subjects for clinical application as well as problems with polymer manufacturing, stability, and biocompatibility. Lastly, it looks at prospective future avenues, such as progressions in multi-responsive systems, precision medicine integration with nanotechnology, and possible combination therapy with OLA for synergistic effects. While identifying the need for more study to overcome current obstacles, the conclusion highlights the extensive potential of pH-sensitive polymers in enhancing the results of OC treatment.</div></div>","PeriodicalId":15600,"journal":{"name":"Journal of Drug Delivery Science and Technology","volume":"111 ","pages":"Article 107076"},"PeriodicalIF":4.5,"publicationDate":"2025-05-30","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144204678","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}
引用次数: 0
Progress on drug nanoparticle manufacturing: exploring the adaptability of batch bottom-up approaches to continuous manufacturing
IF 4.5 3区 医学
Journal of Drug Delivery Science and Technology Pub Date : 2025-05-30 DOI: 10.1016/j.jddst.2025.107120
Clarinda Costa , Luis Padrela
{"title":"Progress on drug nanoparticle manufacturing: exploring the adaptability of batch bottom-up approaches to continuous manufacturing","authors":"Clarinda Costa ,&nbsp;Luis Padrela","doi":"10.1016/j.jddst.2025.107120","DOIUrl":"10.1016/j.jddst.2025.107120","url":null,"abstract":"<div><div>Approximately 40 % of approved drugs and 90 % of small molecule drug candidates in development suffer from poor solubility, limiting their delivery and efficiency on site. Nanomanufacturing, particularly the production of drug nanoparticles and nanosuspensions, offers a solution by enhancing dissolution rates. However, traditional batch processes face challenges in particle size control, downstream processing, throughput, yield, and scalability. Continuous manufacturing (CM) presents a promising alternative, enabling the production of drug nanosystems in a streamlined, continuous scheme that reduces intermediate steps, footprint, and cost. CM also supports improved process control, real-time monitoring, and scalability through parallelization rather than traditional scale-up. This review examines recent advancements in adapting batch bottom-up technologies to continuous processes, focusing on the critical process parameters, critical material attributes and key quality attributes for nanoparticle production, integration of continuous methods, and the associated challenges of implementation in pharmaceutical manufacturing, including downstream processing, scale-up, and regulatory considerations.</div></div>","PeriodicalId":15600,"journal":{"name":"Journal of Drug Delivery Science and Technology","volume":"111 ","pages":"Article 107120"},"PeriodicalIF":4.5,"publicationDate":"2025-05-30","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144242902","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}
引用次数: 0
Enhancing luteolin solubility through solid dispersion-based oral gels: A novel approach for periodontal disease treatment 通过固体分散型口腔凝胶增强木犀草素的溶解度:一种治疗牙周病的新方法
IF 4.5 3区 医学
Journal of Drug Delivery Science and Technology Pub Date : 2025-05-30 DOI: 10.1016/j.jddst.2025.107121
Maria Koromili , Afroditi Kapourani , Konstantina Chaclioutaki , Nikoletta Christoudia , Spyros Pettas , Dimitra Dafou , Theodoros Sklaviadis , Dimitrios A. Andreadis , Spyros Papageorgiou , Andreana N. Assimopoulou , Konstantinos Xanthopoulos , Dimitrios N. Fatouros , Panagiotis Barmpalexis
{"title":"Enhancing luteolin solubility through solid dispersion-based oral gels: A novel approach for periodontal disease treatment","authors":"Maria Koromili ,&nbsp;Afroditi Kapourani ,&nbsp;Konstantina Chaclioutaki ,&nbsp;Nikoletta Christoudia ,&nbsp;Spyros Pettas ,&nbsp;Dimitra Dafou ,&nbsp;Theodoros Sklaviadis ,&nbsp;Dimitrios A. Andreadis ,&nbsp;Spyros Papageorgiou ,&nbsp;Andreana N. Assimopoulou ,&nbsp;Konstantinos Xanthopoulos ,&nbsp;Dimitrios N. Fatouros ,&nbsp;Panagiotis Barmpalexis","doi":"10.1016/j.jddst.2025.107121","DOIUrl":"10.1016/j.jddst.2025.107121","url":null,"abstract":"<div><div>Luteolin (LUT) is a bioactive flavonoid with numerous pharmacological properties, such as antioxidant, antimicrobial, and anti-cancer activity. A prominent example of LUT's properties concerns its administration for the treatment of periodontal disease. However, its low water solubility poses a serious challenge regarding its formulation into an effective dosage form. To this end, the present study investigates the incorporation of LUT's solid dispersions (SDs) into oral gels, as a way to improve LUT solubility in saliva for the treatment of periodontitis. Initially, SDs of LUT were formulated at drug-to-polymer weight ratios of 1:9 and 1:12 using either polyethylene glycol 6000 (PEG) or poloxamer P188 (P188), employing both melting and solvent evaporation techniques. Subsequently, these drug-loaded SDs were integrated into oral gels designed for the local treatment of periodontal disease within the mouth. The SDs resulted in a remarkable solubility enhancement for LUT, showing up to a 16-fold increase compared to its pure crystalline form. Physicochemical characterization using differential scanning calorimetry (DSC) and powder X-ray diffractometry (pXRD), revealed that LUT was amorphously dispersed within the SDs, while ATR-FTIR spectroscopy indicated the presence of significant molecular interactions between the drug and the matrix/carriers. The gels containing the SDs of LUT displayed appropriate rheological properties for handling and storage, while the <em>in vitro</em> dissolution studies in simulated saliva revealed that the PEG SD-based oral gels were able to significantly enhance LUT's release. Moreover, cell viability studies, which examined two promising SDs (one with PEG and one with P188), revealed negligible cytotoxicity, suggesting that the prepared formulations exhibit favorable and non-toxic characteristics. In addition, <em>in vitro</em> assays demonstrated that the formulations retained LUT's anti-inflammatory effect. Finally, <em>ex vivo</em> permeation studies using porcine buccal tissue demonstrated that P188-based SD, incorporated into a placebo gel, enhanced the ability of LUT to partition into and accumulate within the mucosal tissue, resulting in more than three-times the accumulation compared to the gel containing the neat drug. Therefore, the preparation of SD oral gels for LUT can be regarded as a prospective technique with strong potential for the improvement of the API's solubility and hence, its administration in the oral cavity for the topical treatment against periodontitis.</div></div>","PeriodicalId":15600,"journal":{"name":"Journal of Drug Delivery Science and Technology","volume":"111 ","pages":"Article 107121"},"PeriodicalIF":4.5,"publicationDate":"2025-05-30","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144204680","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}
引用次数: 0
Impact of quercetin conjugated silver nanoparticles on neuroinflammation, endothelial permeability, and pharmacokinetics in vivo against genotype T4, Acanthamoeba polyphaga 槲皮素共轭银纳米颗粒对T4基因型多食棘阿米巴体内神经炎症、内皮通透性和药代动力学的影响
IF 4.5 3区 医学
Journal of Drug Delivery Science and Technology Pub Date : 2025-05-30 DOI: 10.1016/j.jddst.2025.107116
Sara S. Abdel-Hakeem , Mahmoud Abdel-Zaher Abdel-Samiee , Mona Mohamed Ali Khalaf , Gamal Hassan Abed
{"title":"Impact of quercetin conjugated silver nanoparticles on neuroinflammation, endothelial permeability, and pharmacokinetics in vivo against genotype T4, Acanthamoeba polyphaga","authors":"Sara S. Abdel-Hakeem ,&nbsp;Mahmoud Abdel-Zaher Abdel-Samiee ,&nbsp;Mona Mohamed Ali Khalaf ,&nbsp;Gamal Hassan Abed","doi":"10.1016/j.jddst.2025.107116","DOIUrl":"10.1016/j.jddst.2025.107116","url":null,"abstract":"<div><div><em>Acanthamoeba</em> spp., pose a growing global health concern due to their association with granulomatous amoebic encephalitis (GAE), particularly in immunocompromised individuals. Treatment options remain limited and often ineffective due to drug resistance, delayed diagnosis, and the parasite's ability to induce neuroinflammation and disrupt the blood-brain barrier (BBB). Therefore, this study investigates, for the first time, the therapeutic role of quercetin-conjugated silver nanoparticles (Q-AgNPs) in modulating neuroinflammatory responses, enhancing endothelial barrier integrity, and improving pharmacokinetic properties of this nanoformulation in an experimental model. A total of 105 male mice were divided into seven groups, representing both immunocompetent and immunosuppressed animals, with appropriate control groups. Q-AgNPs were synthesized and characterized using spectrophotometer, transmission electron microscope, zeta-potential, loading efficiency, <em>invitro</em> release analysis, and FTIR analysis. Hematological indices showed improvement over time with treatment, with significant increases in erythrocytes, hemoglobin, and hematocrit levels, alongside gradual reduction in humoral inflammatory reaction. Additionally, Q-AgNPs treatment reduced proinflammatory cytokines (TNF-α and IL-1β) and BBB permeability marker (MMP9), while significantly increasing anti-inflammatory cytokine (IL-10). Histopathological examinations showed that Q-AgNPs alleviated neural lesions and glial cell reaction. Immunohistochemical analysis highlighted the role of Q-AgNPs in reducing the trans-endothelial immune cell migration and in delaying GAE-induced brain atrophy through decreased PECAM-1 gene expression in the brain regions. Molecular docking revealed that Q-AgNPs had a strong binding affinity with the mitochondrial respiratory protein NAD2, offering enhanced pharmacokinetic properties compared to quercetin alone. This study support Q-AgNPs as a promising therapeutic strategy to combat <em>A. polyphaga</em>-induced GAE by modulating neuroinflammation pathways and improving drug delivery.</div></div>","PeriodicalId":15600,"journal":{"name":"Journal of Drug Delivery Science and Technology","volume":"111 ","pages":"Article 107116"},"PeriodicalIF":4.5,"publicationDate":"2025-05-30","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144221017","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}
引用次数: 0
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