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

Enhancing the therapeutic efficacy of piperine in colorectal cancer: development and evaluation of piperine-loaded PLGA-b-PEG copolymer nanoparticles 提高胡椒碱在结直肠癌中的治疗效果：胡椒碱负载PLGA-b-PEG共聚物纳米颗粒的开发和评价

IF 4.4 2区医学

European Journal of Pharmaceutics and Biopharmaceutics Pub Date : 2025-06-18 DOI: 10.1016/j.ejpb.2025.114796

Nuttapol Risangud , Nisachon Jangpromma , Phraepakaporn Kunnaja , Natthakarn Chiranthanut , Sakda Daduang , Kantapat Chansaenpak , Ruedeemars Yubolphan

{"title":"Enhancing the therapeutic efficacy of piperine in colorectal cancer: development and evaluation of piperine-loaded PLGA-b-PEG copolymer nanoparticles","authors":"Nuttapol Risangud , Nisachon Jangpromma , Phraepakaporn Kunnaja , Natthakarn Chiranthanut , Sakda Daduang , Kantapat Chansaenpak , Ruedeemars Yubolphan","doi":"10.1016/j.ejpb.2025.114796","DOIUrl":"10.1016/j.ejpb.2025.114796","url":null,"abstract":"<div><div>Colorectal cancer (CRC) is the third most common cancer and the second leading cause of cancer-related morbidity and mortality worldwide. Piperine, a natural alkaloid from <em>Piper nigrum L</em>. and <em>Piper longum L.</em>, has shown potential anti-cancer properties, including the ability to induce apoptosis and inhibit cell cycle progression. However, its clinical application is limited by low solubility and poor bioavailability. In this study, we developed piperine-encapsulated PLGA-<em>b</em>-PEG nanoparticles (Pip-PLNP) using a nanoprecipitation method, which achieved a favorable hydrodynamic diameter of approximately 43.8 ± 0.4 nm to 49.1 ± 0.2 nm and high encapsulation efficiency (∼80 %) in a stable, monodisperse form. The anti-cancer effects of Pip-PLNP were evaluated in HCT116 human colorectal carcinoma cells. MTT assays revealed that Pip-PLNP exhibited significant dose- and time-dependent cytotoxicity, with improved potency compared to free piperine. Apoptosis assays demonstrated that Pip-PLNP induced early and late apoptosis more effectively than free piperine. Additionally, cell cycle analysis showed that Pip-PLNP caused G0/G1 phase arrest, consistent with piperine’s known mechanism of action. In conclusion, Pip-PLNP significantly enhances the anti-cancer efficacy of piperine by improving its bioavailability, cytotoxicity, and apoptotic activity, suggesting its potential as a therapeutic approach for colorectal cancer treatment.</div></div>","PeriodicalId":12024,"journal":{"name":"European Journal of Pharmaceutics and Biopharmaceutics","volume":"214 ","pages":"Article 114796"},"PeriodicalIF":4.4,"publicationDate":"2025-06-18","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144321734","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

Amino acid prodrug of capsaicin improves pharmacokinetic properties in the mouse brain and pancreas 辣椒素氨基酸前药改善小鼠大脑和胰腺的药代动力学特性

IF 4.4 2区医学

European Journal of Pharmaceutics and Biopharmaceutics Pub Date : 2025-06-18 DOI: 10.1016/j.ejpb.2025.114797

Janne Tampio , Adéla Králová , Sara Riihioja , Sofia Pitkänen , Magdalena Markowicz-Piasecka , Olli Ihamäki , Katja Savolainen , Sema T. Torunoglu , Aaro J. Jalkanen , Marko Lehtonen , Anu Kauppinen , Jaana Rysä , Kristiina M. Huttunen

{"title":"Amino acid prodrug of capsaicin improves pharmacokinetic properties in the mouse brain and pancreas","authors":"Janne Tampio , Adéla Králová , Sara Riihioja , Sofia Pitkänen , Magdalena Markowicz-Piasecka , Olli Ihamäki , Katja Savolainen , Sema T. Torunoglu , Aaro J. Jalkanen , Marko Lehtonen , Anu Kauppinen , Jaana Rysä , Kristiina M. Huttunen","doi":"10.1016/j.ejpb.2025.114797","DOIUrl":"10.1016/j.ejpb.2025.114797","url":null,"abstract":"<div><div>Among several natural products, capsaicin has been studied for its therapeutic properties to treat various chronic diseases. While it has shown promising effects in several disease models, high lipophilicity and strong metabolism limit its therapeutic use to local injections and topical administration. Moreover, high concentrations of capsaicin cause severe adverse effects. Thus, the present study aimed to synthesize a novel phenylalanine-derived prodrug of capsaicin that would utilize L-type amino acid transporter 1 (LAT1) for its delivery. The proposed prodrug strategy aimed to improve capsaicin’s therapeutic effects in the brain and pancreas, where LAT1 is expressed. The results showed that the cellular uptake into microglia, astrocytes, and pancreatic β-cells increased up to 250-fold by a LAT1-mediated delivery. In the <em>in vivo</em> pharmacokinetic study, more stable drug delivery into the pancreas and brain was observed in mice. By the prodrug design, the exposure time was prolonged from 30 min to 90 min, and peak concentrations of capsaicin were lowered. The novel prodrug did not affect human plasma coagulation, nor induce hemolysis or reactive oxygen species production <em>in vitro</em>. Yet, it inhibited mice’s prostaglandin D<sub>2</sub> and E<sub>2</sub> productionafter lipopolysaccharide induction. To summarize, utilization of LAT1 increased prodrug delivery simultaneously in both the pancreas and brain, allowing dual-targeting of capsaicin. This is a beneficial strategy when developing treatment against diseases interlinked in the brain and pancreas, namely neurodegenerative diseases and diabetes.</div></div>","PeriodicalId":12024,"journal":{"name":"European Journal of Pharmaceutics and Biopharmaceutics","volume":"214 ","pages":"Article 114797"},"PeriodicalIF":4.4,"publicationDate":"2025-06-18","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144331513","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

Cationic Green Solid Lipid nanoparticles by the fatty acid coacervation method for gene delivery to the cornea: preliminary studies on cell and isolated tissue models 通过脂肪酸凝聚法将阳离子绿色固体脂质纳米颗粒基因传递到角膜：细胞和分离组织模型的初步研究

IF 4.4 2区医学

European Journal of Pharmaceutics and Biopharmaceutics Pub Date : 2025-06-17 DOI: 10.1016/j.ejpb.2025.114795

Annalisa Bozza , Marina Beraza-Millor , Julen Rodríguez-Castejón , Francisco Andres Soto Arratia , Roberta Cavalli , Ezio Camisassa , Elisabetta Muntoni , Arianna Marengo , Maria Carmen Valsania , Ana del Pozo-Rodríguez , María Ángeles Solinís , Luigi Battaglia

{"title":"Cationic Green Solid Lipid nanoparticles by the fatty acid coacervation method for gene delivery to the cornea: preliminary studies on cell and isolated tissue models","authors":"Annalisa Bozza , Marina Beraza-Millor , Julen Rodríguez-Castejón , Francisco Andres Soto Arratia , Roberta Cavalli , Ezio Camisassa , Elisabetta Muntoni , Arianna Marengo , Maria Carmen Valsania , Ana del Pozo-Rodríguez , María Ángeles Solinís , Luigi Battaglia","doi":"10.1016/j.ejpb.2025.114795","DOIUrl":"10.1016/j.ejpb.2025.114795","url":null,"abstract":"<div><div>Gene augmentation therapy is an emerging approach to treat several corneal diseases, accounting for visual impairment and blindness worldwide. To this aim, in this preliminary experimental study, cationic Solid Lipid Nanoparticles (SLNs), obtained with the fatty acids coacervation method from natural soaps (Green SLNs), were used to prepare non-viral vectors for the green fluorescent protein encoding plasmid DNA (pDNA). Of note, Green SLNs contain oleic acid and the unsaponifiable fraction, that can act as a permeation enhancer and as an antioxidant, respectively. Stable vectors were obtained with and without the inclusion of hyaluronic acid. SLNs-based vectors were tested for pDNA binding/protection/release, and on <em>in vitro</em> and <em>ex vivo</em> corneal models for association and transfection capacity. pDNA was efficiently bound, protected and released from the vectors. <em>In vitro</em> studies on cell models showed a good cells association, but a poor transfection. Promising results were obtained in <em>ex vivo</em> transfection on rabbit corneas, in the case of vectors without hyaluronic acid, probably thanks to their oleic acid content.</div></div>","PeriodicalId":12024,"journal":{"name":"European Journal of Pharmaceutics and Biopharmaceutics","volume":"214 ","pages":"Article 114795"},"PeriodicalIF":4.4,"publicationDate":"2025-06-17","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144366105","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

Nebulized MSC exosomes promote the transdifferentiation of transitional state cells against acute lung injury through STAT3/Krt8/AQP5 axis 雾化的MSC外泌体通过STAT3/Krt8/AQP5轴促进过渡状态细胞对急性肺损伤的转分化

IF 4.4 2区医学

European Journal of Pharmaceutics and Biopharmaceutics Pub Date : 2025-06-17 DOI: 10.1016/j.ejpb.2025.114792

Yue Tang, Jingyuan Qian, Meng Ding, Rui Ding, Pengwei Yang, Yushun Dou

{"title":"Nebulized MSC exosomes promote the transdifferentiation of transitional state cells against acute lung injury through STAT3/Krt8/AQP5 axis","authors":"Yue Tang, Jingyuan Qian, Meng Ding, Rui Ding, Pengwei Yang, Yushun Dou","doi":"10.1016/j.ejpb.2025.114792","DOIUrl":"10.1016/j.ejpb.2025.114792","url":null,"abstract":"<div><div>The transdifferentiation of alveolar epithelial type II cells (AECIIs) to alveolar epithelial type I cells (AECIs) plays an important role in the epithelial repair in acute lung injury (ALI). Although transitional state cells have been reported to regenerate the alveolar epithelium surface and promote a repair process, the treatment of ALI based on transitional state cells has not been suggested.</div><div>Here, we demonstrate that nebulized mesenchymal stem cell exosomes (MSC exosomes) can be used for ALI and MSC exosomes have the ability to promote the differentiation of transitional state cells into AECIs by regulating the STAT3/Krt8/AQP5 axis. In the in vivo study, immunohistochemistry and immunofluorescence staining results showed that MSC exosomes could reduce the expression of transitional state cells and promote transdifferentiation of AECIIs. In the in vitro study, western blotting (WB) results showed that MSC exosomes downregulated signal transducer and activator of transcription 3 (STAT3) phosphorylation and the expression of transitional state cell specific keratin 8 (Krt8), and upregulated the expression of AECIs specific aquaporin 5 (AQP5). The results indicate that MSC exosomes inhibit STAT3 phosphorylation through STAT3/Krt8/AQP5 axis, promote the transdifferentiation of transitional state cells to AECIs and accelerate the regeneration of alveolar epithelium after LPS-induced lung injury. Regulating transitional state cells to alleviate ALI is suggested for the first time.</div></div>","PeriodicalId":12024,"journal":{"name":"European Journal of Pharmaceutics and Biopharmaceutics","volume":"214 ","pages":"Article 114792"},"PeriodicalIF":4.4,"publicationDate":"2025-06-17","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144470638","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

Applications and prospects of synthetic receptors for therapeutic protein delivery 合成受体在治疗性蛋白质传递中的应用与展望

IF 4.4 2区医学

European Journal of Pharmaceutics and Biopharmaceutics Pub Date : 2025-06-17 DOI: 10.1016/j.ejpb.2025.114789

Danhong Zhou, Yunxuan Chen, Jin He, Qinmeng Zhang, Zhiwei Jiang, Guoli Yang

{"title":"Applications and prospects of synthetic receptors for therapeutic protein delivery","authors":"Danhong Zhou, Yunxuan Chen, Jin He, Qinmeng Zhang, Zhiwei Jiang, Guoli Yang","doi":"10.1016/j.ejpb.2025.114789","DOIUrl":"10.1016/j.ejpb.2025.114789","url":null,"abstract":"<div><div>Synthetic receptors have gained prominence in synthetic biology due to their tunability, simplicity, versatility, and capacity for precise gene editing, which collectively enhance the temporal and spatial control of therapeutic protein delivery. Several types of synthetic receptors have been engineered to deliver specific therapeutic proteins, including G protein-coupled receptor (GPCR)-based receptor systems, modular extracellular sensor architecture (MESA), synthetic Notch (synNotch) receptor, and synthetic intramembrane proteolysis receptors (SNIPRs). These receptors have demonstrated therapeutic potential in targeting tumors, inflammatory immune diseases, central nervous system disorders, arthropathies, and viral infections by delivering specific proteins to diseased tissues. However, several challenges persist, including safety concerns, suboptimal delivery efficiency, and receptor design and optimization complexity. This review summarizes the current types, characteristics, and biomedical applications of synthetic receptors for therapeutic protein delivery, while also addressing their limitations and potential future directions.</div></div>","PeriodicalId":12024,"journal":{"name":"European Journal of Pharmaceutics and Biopharmaceutics","volume":"214 ","pages":"Article 114789"},"PeriodicalIF":4.4,"publicationDate":"2025-06-17","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144366106","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

Targeting fungal keratitis: In vivo efficacy of corneal-targeting and non-targeting peptides against Fusarium dimerum 靶向真菌性角膜炎：角膜靶向和非靶向肽对二角镰刀菌的体内疗效

IF 4.4 2区医学

European Journal of Pharmaceutics and Biopharmaceutics Pub Date : 2025-06-17 DOI: 10.1016/j.ejpb.2025.114793

Aditi Arora , Prasanjeet Kaur , Shikha Yadav , Priyanka P Srivastava , Shilpi Minocha , Sushmita G Shah , Archana Chugh

{"title":"Targeting fungal keratitis: In vivo efficacy of corneal-targeting and non-targeting peptides against Fusarium dimerum","authors":"Aditi Arora , Prasanjeet Kaur , Shikha Yadav , Priyanka P Srivastava , Shilpi Minocha , Sushmita G Shah , Archana Chugh","doi":"10.1016/j.ejpb.2025.114793","DOIUrl":"10.1016/j.ejpb.2025.114793","url":null,"abstract":"<div><div>Fungal keratitis is a major contributor to monocular blindness, globally. This is because, application of conventional topical therapy yields poor outcomes owing to the poor penetration and fungistatic nature of these antifungal agents. Cell penetrating peptides (CPPs) with potent antifungal effect may provide a solution to address these challenges. In this study, the antifungal efficacy of two CPPs: a corneal-targeting peptide (CorTS 1) and a non-targeting peptide (Tat<sub>2</sub>) was evaluated. Both peptides effectively inhibited the growth of <em>Fusarium dimerum</em> hyphae by modulating membrane permeability <em>in vitro.</em> Additionally, these peptides demonstrated successful <em>trans</em>-epithelial penetration in rabbit eyes and exhibited superior therapeutic effects compared to commercially available natamycin ophthalmic suspension in mouse model of <em>Fusarium</em> keratitis. While Tat<sub>2</sub> showed greater antifungal potency, its non-specific targeting and anti-inflammatory properties suggest its potential utility in early-stage fungal keratitis. In contrast, CorTS 1, with its corneal-targeting capability, may be more effective for treating late-stage deep stromal keratitis. These findings highlight the potential of biologically active CPPs as promising new therapies for fungal keratitis.</div></div>","PeriodicalId":12024,"journal":{"name":"European Journal of Pharmaceutics and Biopharmaceutics","volume":"214 ","pages":"Article 114793"},"PeriodicalIF":4.4,"publicationDate":"2025-06-17","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144331514","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 coiled coil-based pre-targeting drug delivery system for precise treatment of breast cancer 一种用于精确治疗乳腺癌的盘绕式预靶向药物输送系统

IF 4.4 2区医学

European Journal of Pharmaceutics and Biopharmaceutics Pub Date : 2025-06-17 DOI: 10.1016/j.ejpb.2025.114794

Chaoyu Zhang , Wenjie Sheng , T.M. Mohiuddin , Marwah Al-Rawe , Roland Schmitz , Marcus Niebert , Felix Zeppernick , Ivo Meihold-Heerlein , Ahmad Fawzi Hussain

{"title":"A coiled coil-based pre-targeting drug delivery system for precise treatment of breast cancer","authors":"Chaoyu Zhang , Wenjie Sheng , T.M. Mohiuddin , Marwah Al-Rawe , Roland Schmitz , Marcus Niebert , Felix Zeppernick , Ivo Meihold-Heerlein , Ahmad Fawzi Hussain","doi":"10.1016/j.ejpb.2025.114794","DOIUrl":"10.1016/j.ejpb.2025.114794","url":null,"abstract":"<div><h3>Background</h3><div>Antibody-drug conjugates (ADCs) consist of an antibody linked to a cytotoxic agent. To optimize the efficacy of ADCs, our study developed a pre-targeting drug delivery system based on the specific interaction between two synthetic coiled-coil proteins, Zip1 and Zip2. The targeting vehicle was composed of Zip2-fused single-chain variable fragments, while the toxic vehicle consisted of Zip1 conjugated to cytotoxic agent monomethyl auristatin E via SNAP-tag.</div></div><div><h3>Methods</h3><div>The targeting activities of the pre-targeting reagents were evaluated using various techniques, including flow cytometry, fluorescence microscopy, cell viability and apoptosis assays, and ex vivo multiplex immunofluorescence.</div></div><div><h3>Results</h3><div>The pre-targeting complexes demonstrated specific binding and internalization in breast cancer cell lines, as assessed by flow cytometry and fluorescence microscopy. Furthermore, cell death was observed in antigen-expressing cell lines upon triggering apoptosis at nanomolar concentrations.</div></div><div><h3>Conclusions</h3><div>Given the heterogeneous tumor environment and individual differences, separating the “targeting” and “killing” steps enables targeting molecules to bind to different antigens, followed by the application of the Zip1-drug complex without requiring antibody engineering. Our study highlights the potential of this pre-targeting system to efficiently deliver drugs, offering a promising strategy to address challenges faced by ADCs, such as poor tissue penetration, low accumulation, and “on-target, off-tumor” toxicity.</div></div>","PeriodicalId":12024,"journal":{"name":"European Journal of Pharmaceutics and Biopharmaceutics","volume":"214 ","pages":"Article 114794"},"PeriodicalIF":4.4,"publicationDate":"2025-06-17","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144306164","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

Advancing forced degradation studies: Design of experiments for enhanced structure-function relationship analysis in biotherapeutics 推进强制降解研究：生物治疗中增强结构-功能关系分析的实验设计。

IF 4.4 2区医学

European Journal of Pharmaceutics and Biopharmaceutics Pub Date : 2025-06-14 DOI: 10.1016/j.ejpb.2025.114787

Klaus Kronsbein , Verena Nold , Armin Böhrer , Beate Presser , Tanja Gaissmaier , Katharina Schindowski , Boris Mizaikoff , Florian Krattenmacher

{"title":"Advancing forced degradation studies: Design of experiments for enhanced structure-function relationship analysis in biotherapeutics","authors":"Klaus Kronsbein , Verena Nold , Armin Böhrer , Beate Presser , Tanja Gaissmaier , Katharina Schindowski , Boris Mizaikoff , Florian Krattenmacher","doi":"10.1016/j.ejpb.2025.114787","DOIUrl":"10.1016/j.ejpb.2025.114787","url":null,"abstract":"<div><div>Understanding the relationship between structure and function is crucial in drug development. Recombinant proteins present unique challenges when establishing structure–function relationships (SFR) due to the extensive options for potential modifications across numerous residues. Even simple stress studies lack degradation selectivity as they lead to multiple, simultaneous modifications. Co-occurring modifications at amino acid residues make direct correlations with a specific stressor and resolving the causal impact on functionality difficult. The introduction of more variance into the data set would reduce the correlation structure. In this study, we demonstrate the feasibility and benefits of a multifactorial design approach for SFR establishment. Design of experiments (DoE) allows for the parallel investigation of stress factors via combined experiments, resulting in a higher variance of stress conditions and consequently a broader variation in degradation. This approach enables a more insightful correlation analysis along with model-based data evaluation strategies, thereby facilitating significantly improved data interpretation results during SFR studies.</div></div>","PeriodicalId":12024,"journal":{"name":"European Journal of Pharmaceutics and Biopharmaceutics","volume":"214 ","pages":"Article 114787"},"PeriodicalIF":4.4,"publicationDate":"2025-06-14","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144309781","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

Nanoformulated cannabidiol for skin disorders: A GRADE-based systematic review of therapeutic evidence and efficacy 纳米配方大麻二酚治疗皮肤病：基于grade的治疗证据和疗效的系统评价

IF 4.4 2区医学

European Journal of Pharmaceutics and Biopharmaceutics Pub Date : 2025-06-13 DOI: 10.1016/j.ejpb.2025.114784

Bakr Ahmed , Simrandeep Kaur , Srishti Naryal , Aanchal Devi , Muskan Kathpalia , Rohan M. Shah , Indu Pal Kaur

{"title":"Nanoformulated cannabidiol for skin disorders: A GRADE-based systematic review of therapeutic evidence and efficacy","authors":"Bakr Ahmed , Simrandeep Kaur , Srishti Naryal , Aanchal Devi , Muskan Kathpalia , Rohan M. Shah , Indu Pal Kaur","doi":"10.1016/j.ejpb.2025.114784","DOIUrl":"10.1016/j.ejpb.2025.114784","url":null,"abstract":"<div><div>Cannabidiol (CBD), a non-psychoactive chemical derived from <em>Cannabis sativa L</em>., has significant dermatological potential due to its antiinflammatory, antioxidant, and wound healing attributes. However, its clinical usage is limited by instability, minimal skin penetration, and poor solubility. Nanotechnology-based delivery systems such as pickering emulsions, cryogels, lipid nanoparticles, and nanomicelles have emerged as promising strategies to enhance localized skin delivery, improve penetration, enable sustained release, and reduce adverse effects. According to this analysis of 16 papers and 18 patents (2019-2024), CBD that has been nanoformulated offers improved tolerability, sustained release, and skin delivery. According to GRADE review, impacts on dermal absorption, inflammation, and wound healing demonstrated intermediate certainty, but outcomes such as skin penetration, controlled release, and safety showed high certainty. Applications for acne, psoriasis, and eczema show enhanced patient compliance and efficacy. Despite clinical and regulatory obstacles, nano-CBD platforms provide a safe, focused, and efficient approach to improving dermatological care.</div></div>","PeriodicalId":12024,"journal":{"name":"European Journal of Pharmaceutics and Biopharmaceutics","volume":"214 ","pages":"Article 114784"},"PeriodicalIF":4.4,"publicationDate":"2025-06-13","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144297563","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

Drug loading mechanism of hollow hydroxyapatite microcapsules 空心羟基磷灰石微胶囊的载药机制

IF 4.4 2区医学

European Journal of Pharmaceutics and Biopharmaceutics Pub Date : 2025-06-13 DOI: 10.1016/j.ejpb.2025.114785

Jonas Kost, Nathalie Peyer, Jörg Huwyler, Maxim Puchkov

{"title":"Drug loading mechanism of hollow hydroxyapatite microcapsules","authors":"Jonas Kost, Nathalie Peyer, Jörg Huwyler, Maxim Puchkov","doi":"10.1016/j.ejpb.2025.114785","DOIUrl":"10.1016/j.ejpb.2025.114785","url":null,"abstract":"<div><div>Inorganic hydroxyapatite microcapsules are innovative drug delivery devices tailored for oral drug delivery. They were designed as novel excipients, the so-called template inverted particles (TIP), to assist in preparing the orally disintegrating tablets. This study characterized the drug loading capacity using 11 clinically relevant drugs covering all BCS classes, focusing on midazolam HCl, ivermectin, ibuprofen, and metronidazole benzoate. An exceptionally high drug loading capacity of 45 % (v/v) was observed for all studied drugs. Compaction of loaded TIP resulted in mechanically stable tablets with tensile strengths of up to 6 MPa and disintegrating in a few seconds upon contact with water. Accelerated dissolution of encapsulated drugs is explained by the microcapsules’ high specific surface area and the inhibited crystallization due to spacial constraints for some tested drugs. Efficient drug loading into TIP’s internal hollow cavity structure is facilitated by a self-loading mechanism, eliminating the need for complex, drug-specific loading strategies. A mathematical model is presented to describe the self-loading mechanism of TIP, which is responsible for exclusive drug deposition within the cavity of the particles. We demonstrate that TIP, being a versatile and cost-effective platform technology, has the potential to facilitate the formulation development process of patient-friendly medicines.</div></div>","PeriodicalId":12024,"journal":{"name":"European Journal of Pharmaceutics and Biopharmaceutics","volume":"214 ","pages":"Article 114785"},"PeriodicalIF":4.4,"publicationDate":"2025-06-13","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144297562","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