Drug Development and Industrial Pharmacy最新文献

{"title":"Combating breast cancer-associated metastasis using paclitaxel and tranilast-loaded human serum albumin nanoparticles.","authors":"Naitik Jain, Syed Shahrukh, Paras Famta, Saurabh Shah, Ganesh Vambhurkar, Dadi A Srinivasarao, Anamika Sharma, Giriraj Pandey, Suraj Wagh, Swapnil Shinde, Anjesh Khan, Prashanth Kumar, Saurabh Srivastava","doi":"10.1080/03639045.2025.2509861","DOIUrl":"10.1080/03639045.2025.2509861","url":null,"abstract":"<p><strong>Objective: </strong>The objective of the current study is to combat breast cancer-associated metastasis using paclitaxel (PTX) and tranilast (TRA)-loaded human serum albumin (HSA) nanoparticles.</p><p><strong>Significance: </strong>This combinatorial therapy uses microtubule stabilizing agent PTX, along with TGFβ inhibitor TRA. TRA may offer an improved therapeutic effect in breast cancer by inhibiting cell proliferation and metastasis.</p><p><strong>Methods: </strong>Inspired by the remarkable anticancer properties of both drugs, they were encapsulated into HSA nanoparticles to enhance tumor site-specific drug accumulation and ensure sustained release over a prolonged period. The HSA nanoparticles were fabricated using the desolvation method and optimized using a Box-Behnken design (BBD) with a three-level, two-factor approach. Further, these nanoparticles were characterized using TEM, FTIR, XRD, and particle size. <i>In vitro</i> experiments were conducted using the MDA-MB-231 cell line, employing cell viability, cellular uptake, nuclear staining, scratch assay, and cell cycle analysis.</p><p><strong>Key findings: </strong><i>In vitro</i> release kinetics reveal sustained PTX and TRA release from HSA nanoparticles. Wound healing assay depicted improved anti-migratory activity of PTX-TRA-NPs (30 nM to 75 µM). Furthermore, the novel combination treatment caused G2/M phase cell cycle arrest, as indicated by cell cycle analysis.</p><p><strong>Conclusion: </strong>HSA nanoparticles enhance the delivery and accumulation of hydrophobic drugs (PTX and TRA) in breast cancer cells, offering improved therapeutic outcomes. This combinatorial strategy permits further preclinical investigation for synergistic breast cancer management.</p>","PeriodicalId":11263,"journal":{"name":"Drug Development and Industrial Pharmacy","volume":" ","pages":"786-798"},"PeriodicalIF":2.4,"publicationDate":"2025-07-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144119088","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Formulation of semi solid dosage forms for topical application utilizing quality by design (QbD) approach.","authors":"Eni Bushi, Ledjan Malaj, Piera Di Martino, Gentjan Mataj, Brunilda Myftari","doi":"10.1080/03639045.2025.2498521","DOIUrl":"10.1080/03639045.2025.2498521","url":null,"abstract":"<p><strong>Objective: </strong>Over the last few decades, there have been advancements in our comprehension of the design and development of topical semisolid formulations; however, they still follow an empirical development. Our study focuses on building a framework for designing and developing topical semisolid products using 'Quality by Design' (QbD) approach.</p><p><strong>Methods: </strong>A literature review was conducted to identify and list the factors related to the design and development of topical semi-solid dosage forms using Quality by Design approach. The information extracted from the relevant articles was used to build a QbD framework based on four main pillars: Define the Quality Target Product Profile (QTPP); identify Critical Quality Attributes (CQAs); identify Critical Material Attributes (CMAs) and Critical Process Parameters (CPPs); understand how CMAs and CPPs affect CQAs and establish a control strategy.</p><p><strong>Results: </strong>Some typical elements of the QTPP for topical products include dosage form, route of administration, shelf life, critical quality attributes of the final formulation. Critical material attributes such as characteristics of API (molecular weight, lipophilicity, solubility, metamorphosis events, and polymorphism), characteristics of excipients, and critical process parameters (temperature, heating and cooling rates, mixing speed, pumping speed, order of addition) are identified and explained for their impact on CQAs.</p><p><strong>Conclusions: </strong>Proper characterization of the API and drug delivery system will increase the likelihood of developing a stable, pleasing, and tolerable topical formulation and minimize the risk of failure.</p>","PeriodicalId":11263,"journal":{"name":"Drug Development and Industrial Pharmacy","volume":" ","pages":"670-678"},"PeriodicalIF":2.4,"publicationDate":"2025-07-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143981638","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Enhancing gliclazide solubility using solid dispersions with carboxymethyl chitosan and polyvinylpyrrolidone K30 as polymeric carriers.","authors":"Berivan Ajeel Ibrahim, Nozad Rashid Hussein, Huner Kamal Omer, Abdelbary Elhissi, Iftikhar Khan","doi":"10.1080/03639045.2025.2506651","DOIUrl":"10.1080/03639045.2025.2506651","url":null,"abstract":"<p><strong>Background: </strong>Gliclazide (Glz) is a second-generation sulfonylurea antidiabetic drug, used to treat type II diabetes mellitus. Glz is a class II drug according to the biopharmaceutic classification system (BCS), indicating that it has high permeability and poor aqueous solubility.</p><p><strong>Objective: </strong>This study aimed to improve the solubility of Glz <i>via</i> the solid dispersion method.</p><p><strong>Methods: </strong>Solid dispersions of the drug were formulated using carboxymethyl chitosan (CMch) and polyvinyl pyrrolidone K30 (PVP K30) in varying drug to carrier ratios (1:1, 1:3, and 1:5 w/w) using kneading and solvent evaporation methods. The solubility of Glz solid dispersions was compared with the pure Glz and co-grounded mixtures of the drug.</p><p><strong>Results: </strong>Both carriers exhibited a noticeable increment in solubility and dissolution rate compared to the drug alone. Glz: CMch (1:5 w/w ratio) formulation made by the kneading method exhibited an increased solubility by approximately nine folds (337.79 ± 4.22 µg/ml) as compared to Glz alone (38.74 ± 4.69 µg/ml). However, the greatest improvement in drug dissolution rate was observed in the dispersion made with 1:5 w/w drug to PVP K30 using the solvent evaporation method, and the percentage drug release reached 100% after 30 min. Solid dispersions characterization manifested the compatibility between the drug and carriers, with alteration in particle morphology, and reduction in drug crystallinity.</p><p><strong>Conclusion: </strong>Overall, solid dispersion using CMch has shown to be an excellent approach for enhancing the solubility and dissolution of the class II drug Glz.</p>","PeriodicalId":11263,"journal":{"name":"Drug Development and Industrial Pharmacy","volume":" ","pages":"735-746"},"PeriodicalIF":2.4,"publicationDate":"2025-07-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144132174","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Patient-centered innovations in ambulatory care: developing a fixed-dose tablet to enhance adherence for patients with chronic diseases.","authors":"Saleh F Alqifari, Hanan Alshareef, Hesham M Tawfeek, Palanisamy Amirthalingam, Sadeem F Alharbi, Rahaf M Alatawi, Hayaa T Alahmari, Khulood A Qasem, Ghareb M Soliman","doi":"10.1080/03639045.2025.2513407","DOIUrl":"10.1080/03639045.2025.2513407","url":null,"abstract":"<p><strong>Objective: </strong>To improve medication adherence in patients with chronic diseases by developing a tablet formulation containing a combination of metformin, atorvastatin, aspirin, and enalapril maleate. Significance: Effectively managing chronic diseases often requires multiple medications, which can result in low patient adherence and suboptimal therapeutic outcomes. Developing a combination tablet is an effective modality to address this issue.</p><p><strong>Methods: </strong>To test the patient perception, an online survey was distributed patients with chronic diseases. Based on the survey results, combination tablets were prepared by direct compression using a multifunctional excipient (PROSOLV^® EASYtab). The compatibility between the drugs and excipients was studied using differential scanning calorimetry (DSC) and Fourier-transform infrared (FT-IR) spectroscopy. The tablets were evaluated for weight uniformity, friability, hardness, thickness, diameter, disintegration time, uniformity of drug content, and <i>in vitro</i> drug release.</p><p><strong>Results: </strong>Most participants reported issues with non-adherence, but expressed a strong positive perception of combination tablets, particularly regarding their effectiveness in improving their condition. DSC and FT-IR studies confirmed the compatibility of the investigated drugs with each other and the used excipient. The tablets fulfilled the European Pharmacopeia 2014 specifications for the tested parameters. The release of all four drugs was fast and a cumulative percent drug release of approximately 50-85% was observed after 15 min.</p><p><strong>Conclusions: </strong>These findings highlight the significant potential of the combination tablets as a single-dose delivery system, allowing the simultaneous administration of multiple medications for patients with chronic diseases, thereby enabling more effective and streamlined management.</p>","PeriodicalId":11263,"journal":{"name":"Drug Development and Industrial Pharmacy","volume":" ","pages":"826-835"},"PeriodicalIF":2.4,"publicationDate":"2025-07-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144172920","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"A review article on transethosomes: revolutionizing drug delivery through transdermal patches.","authors":"Siddharam Loni, Suma U S, R Zohmingliani, Sumanth Sumanth","doi":"10.1080/03639045.2025.2507688","DOIUrl":"10.1080/03639045.2025.2507688","url":null,"abstract":"<p><p>Transethosomes, advanced nanovesicular carriers, have emerged as a revolutionary drug delivery system, particularly for transdermal patches. Combining the structural flexibility of ethosomes and the penetration-enhancing properties of surfactants, transethosomes offer remarkable advantages in overcoming the skin barrier to deliver a broad range of therapeutic agents. These vesicles enhance drug permeation, improve bioavailability, and enable controlled and sustained release, making them a promising alternative to conventional drug delivery methods. This review explores the unique composition, mechanisms of action, and penetration pathways of transethosomes while highlighting their application in various therapeutic areas, including pain management, dermatology, and hormone replacement therapies. Additionally, the article discusses the potential for transethosomes to target specific skin layers or cells, improving drug localization and minimizing systemic side effects. Current challenges, such as formulation stability, variability in skin types, and regulatory hurdles, are critically analyzed, alongside underexplored areas like large biomolecule delivery and multi-drug systems. Emerging trends, including personalized medicine, combination therapies, and stimuli-responsive formulations, are also reviewed, emphasizing the future potential of transethosomes in drug delivery innovation. By addressing these aspects, this article provides comprehensive insights into the transformative role of transethosomes in revolutionizing transdermal drug delivery systems.</p>","PeriodicalId":11263,"journal":{"name":"Drug Development and Industrial Pharmacy","volume":" ","pages":"691-701"},"PeriodicalIF":2.4,"publicationDate":"2025-07-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144093103","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Storage and in-use stability of an excipient enhanced growth (EEG) synthetic lung surfactant powder formulation.","authors":"Mohammad A M Momin, Connor Howe, Worth Longest, Michael Hindle","doi":"10.1080/03639045.2025.2508845","DOIUrl":"10.1080/03639045.2025.2508845","url":null,"abstract":"<p><strong>Objective: </strong>To evaluate the storage and in-use stability of a novel synthetic lung surfactant (SLS) excipient enhanced growth (EEG) powder formulation.</p><p><strong>Significance: </strong>Aerosol delivery of surfactant formulations could address limitations of current instilled surfactant replacement therapy for neonatal respiratory distress syndrome. A stable surfactant powder formulation is essential for this approach.</p><p><strong>Methods: </strong>SLS-EEG powder was spray-dried from a formulation of dipalmitoyl -phosphatidylcholine (DPPC), surfactant protein B peptide mimic (B-YL), mannitol, sodium chloride, and l-leucine. Powders were filled into hydroxypropyl methylcellulose (HPMC) capsules and stored in aluminum-aluminum blisters at 25  °C, 5  °C and -20 °C (all ± 2 °C) and 40 ± 5% relative humidity (RH) for 6 months. Physicochemical and aerosol properties were assessed post-spray drying and post-storage. In-use stability was assessed by exposing powders to 22 °C/45% RH for 30 and 120 min and 30 °C/75% RH for 120 min before dry powder inhaler (DPI) actuation.</p><p><strong>Results: </strong>DPPC content remained stable for 6 months at all storage temperatures. Powder morphology and particle size were unchanged at 5 °C and -20 °C, but altered at 25 °C. Solid-state stability and surface activity were unaffected. Emitted doses remained high (>95%) after 3 months using an infant air-jet DPI, though <i>in vitro</i> lung deposition decreased from ∼50% to ∼40% and ∼30% at 3 and 6 months. In-use exposure of the formulation in device to 22 °C/45% RH caused no lung deposition changes, but it declined at 30 °C/75% RH (∼40% vs. ∼50%).</p><p><strong>Conclusions: </strong>A synthetic lung surfactant EEG powder formulation with physicochemical stability and acceptable aerosol performance up to 6 months storage has been successfully produced.</p>","PeriodicalId":11263,"journal":{"name":"Drug Development and Industrial Pharmacy","volume":" ","pages":"747-757"},"PeriodicalIF":2.4,"publicationDate":"2025-07-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144109846","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Augmented anticancer efficacy of <i>Ailanthus Excelsa</i>-loaded lipidic nanocarriers for breast cancer treatment: <i>in-vitro</i> and <i>in-vivo</i> evaluation.","authors":"Neama Ibrahim, Sarah Yahia, Rabab M El-Sherif, Ibrahim M El-Sherbiny","doi":"10.1080/03639045.2025.2509869","DOIUrl":"10.1080/03639045.2025.2509869","url":null,"abstract":"<p><strong>Background: </strong>One of the most lethal forms of cancer that impacts women worldwide is breast cancer (BC). The treatment results are influenced by multiple factors, such as the phase of diagnosis, hereditary and hormonal influences, medication resistance, and metastases. <i>Ailanthus Excelsa</i> (AE) crude extract is rich in antioxidants and possesses potent anticancer properties, as demonstrated in tests on MCF-7 cells. Additionally, both lavender oil (LO) and tea tree oil (TTO) have potential cytotoxicity against cancer.</p><p><strong>Objectives: </strong>The purpose of this study was to boost the potency and solubility of AE against breast cancer <i>via</i> its loading in lipidic nanocarriers (LNPs) whose structure is based on a mixture of LO and TTO.</p><p><strong>Methods: </strong>The particle size, stability, and zeta potential of AE-loaded LNPs were examined over 6 months, and the measurements confirmed the good stability of the newly developed AE-LNPs.</p><p><strong>Results: </strong>The AE-LNPs have demonstrated a stronger anticancer impact compared to free AE and plain LNPs, where IC₅₀ values were found to be 36.88 ± 3.09, 22.09 ± 2.13, and 7.49 ± 0.67 µg/ml for plain NPs, free AE, and AE-LNPs, respectively. Furthermore, the AE-LNPs exhibited more pronounced anticancer effects in the Ehrlich ascites <i>in-vivo</i> tumor model, accompanied by significant antiproliferative and antioxidant properties. The immunohistochemical analysis of BCL-2 in tumor tissue validated the apoptotic activity of AE-LNPs.</p><p><strong>Conclusion: </strong>This study is the first to examine the formulation of the newly developed AE-loaded LNPs, demonstrating their efficacy in producing anti-proliferative effects and their considerable promise for BC treatment.</p>","PeriodicalId":11263,"journal":{"name":"Drug Development and Industrial Pharmacy","volume":" ","pages":"799-810"},"PeriodicalIF":2.4,"publicationDate":"2025-07-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144119081","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Modified sodium caseinate-based nanomicelles for enhanced chemotherapeutics against breast cancer via improved cellular uptake and cytotoxicity.","authors":"Farah Rehan, Md Emranul Karim, Nafees Ahemad, Omer Salman Qureshi, Seemal Jelani, Siew Hua Gan, Ezharul Hoque Chowdhury","doi":"10.1080/03639045.2025.2495849","DOIUrl":"10.1080/03639045.2025.2495849","url":null,"abstract":"<p><strong>Objective: </strong>Poor prognosis, drug resistance, and lower drug loading capacity of the delivery systems lead to therapeutic failures of breast cancers. Herein, we functionalized sodium caseinate nanomicelles (NaCNs) with the divalent calcium (Ca²⁺) and the glucose (Glc) to increase the loading capacity of micelles for higher cellular uptake and cytotoxicity against breast cancer cells.</p><p><strong>Methodology: </strong>Modification of casein micelles was confirmed through Fourier transform infrared spectra (FTIR). Triple quadrupole liquid chromatography-mass spectrometry (TQOF-LCMS/MS) was utilized as a simple, rapid, and sensitive method for protein corona quantification around casein through SwissProt.Mus_musculus database and through <i>de novo</i> sequencing. Un-modified and modified casein micelles were further characterized through field emission scanning electron microscope (FESEM), high resolution-transmission electron microscope (HR-TEM), and energy-dispersive X-ray (EDX). Whereas, sodium dodecyl sulfate-polyacrylamide gel electrophoresis (SDS-PAGE) was used for protein separation and analysis during micelles formation.</p><p><strong>Results: </strong>Calcium divalent modified sodium caseinate nanomicelles (Ca-NaCNs) and glucose-modified sodium caseinate nanomicelles (Glc-NaCNs) were successfully developed, demonstrating a significantly improved micellar stability. Glc-NaCNs-DOX showed a zeta size of 297.13 ± 15.66 nm with an improved zeta potential of -13.73 ± 0.579 with a drug loading efficiency (DLE) of 86% as compared to our previously published casein formulations since the modified versions involved more soluble casein in the protein micelle matrix, Whereas, Ca-NaCNs-DOX also showed an IC₅₀ value of approximately 197.1 nm as compared to IC₅₀ of free DOX (341.8 nm) and when compared to unmodified DOX loaded formulations (<i>p</i> < .001).</p><p><strong>Conclusion: </strong>Modified NaCNs exhibit the potential to be investigated further as a novel delivery system for similar active moieties to maximize their therapeutic effects.</p>","PeriodicalId":11263,"journal":{"name":"Drug Development and Industrial Pharmacy","volume":" ","pages":"702-719"},"PeriodicalIF":2.4,"publicationDate":"2025-07-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143987477","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Assessment of Cytotoxic Effects of Quercetin Nanoemulgel on Different Skin Cancer cell lines.","authors":"Joshna Booravilli, Janaki Devi Sirisolla","doi":"10.1080/03639045.2025.2509274","DOIUrl":"10.1080/03639045.2025.2509274","url":null,"abstract":"<p><strong>Objective: </strong>Quercetin, a polyphenolic flavonoid with antioxidant and anticancer effects, has limited use due to poor water solubility. The objective of this study was to improve the therapeutic effectiveness of quercetin by developing a topical quercetin nanoemulgel.</p><p><strong>Method: </strong>By optimizing the oil (clove oil) and smix ratio (Tween 20:propylene glycol), quercetin nanoemulsion was prepared by spontaneous emulsification method and then evaluated. The optimized nanoemulsion was further prepared to form quercetin nanoemulgel.</p><p><strong>Results: </strong>According to evaluation studies, the optimized quercetin nanoemulsion (QUE NE 3) exhibited stability with a negative zeta potential (-38.2 mV), a tiny particle size (98.2 nm), and high entrapment effectiveness (96.36%). The optimized nanoemulsion was formulated into a nanoemulgel (QUE NEG 3). Studies on <i>ex vivo</i> drug release of quercetin nanoemulgel (QUE NEG 3) showed improved permeability, with cumulative drug release of 93.56 ± 1.16% in 8 h, which was greater than standard quercetin gel (QG) and drug free loaded nanoemulgel (DFL NEG). This was proved by CLSM which shows the delivery of QUE NEG 3 into the dermis. Dose-dependent inhibitory effects were found in cytotoxicity assays conducted on skin cancer cell lines (TE 354.T, A431, and A375) by using the MTT assay. The results demonstrated that quercetin nanoemulgel (QUE NEG 3) showed higher cytotoxicity of 66.52% especially against A431 cells. Hence proving its ability to treat squamous cell carcinoma.</p><p><strong>Conclusion: </strong>These findings imply that the quercetin nanoemulgel is a viable drug delivery method for enhancing quercetin's solubility and therapeutic efficacy.</p>","PeriodicalId":11263,"journal":{"name":"Drug Development and Industrial Pharmacy","volume":" ","pages":"771-785"},"PeriodicalIF":2.4,"publicationDate":"2025-07-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144109840","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Simple but novel taxifolin@pro-glycymicelles as effective treatment for acetaminophen overdose-induced hepatotoxicity: preparation, in vitro characterizations, and in vivo experimental evaluations.","authors":"Yao Dong, Ling Zhang, Xixi Song, Xiaoli Chen, Yuyan He, Xianggen Wu, Mengshuang Li","doi":"10.1080/03639045.2025.2525968","DOIUrl":"10.1080/03639045.2025.2525968","url":null,"abstract":"<p><strong>Objective: </strong>To develop a simple but novel formulation named TAX@pro-glycymicelles with glycyrrhizin as the nanomaterial encapsulating taxifolin (TAX).</p><p><strong>Significance: </strong>TAX@pro-glycymicelles, simply prepared with two generally recognized as safe phytochemicals, demonstrated excellent characteristics, improved oral bioavailability of TAX, and strong effects against hepatotoxicity.</p><p><strong>Methods: </strong>TAX@pro-glycymicelles were prepared, and its physicochemical properties were determined. Safety assays, oral bioavailability in rats, treatment effects and mechanisms on liver injury in mice were also inflicted on TAX@pro-glycymicelle.</p><p><strong>Results: </strong>TAX@pro-glycymicelles were simply prepared, and the obtained powder demonstrated good storage stability and could be rapidly solubilized into water solutions to be clear nano-glycymicelle solutions. The apparent aqueous solubility of TAX from TAX@pro-glycymicelles was exceptionally improved to higher than 40 mg/ml. The <i>in vitro</i> release of TAX@pro-glycymicelles was also accelerated, and their <i>in vitro</i> antioxidative activity increased. Hemolysis and hen's egg test-chorioallantoic membrane assays showed that TAX@pro-glycymicelles exhibited good safety profiles. Oral bioavailability of TAX@pro-glycymicelles was approximately 32.1% higher than that of bare TAX in rats. TAX@pro-glycymicelles was also found to have a stronger dose-dependent treatment effect on acetaminophen overdose-induced hepatotoxicity in mice than bare TAX, including decreasing liver-to-body and spleen-to-body weight ratios, significantly decreasing alanine aminotransferase and aspartate aminotransferase levels in serum, decreasing inflammation and oxidative stress cytokine levels in livers, and reversing severe histological damage to liver tissues. The mechanisms of inhibiting oxidative stress and blocking high-mobility group box 1 signaling-related proinflammatory cytokines were involved in these strong treatment effects.</p><p><strong>Conclusions: </strong>TAX@pro-glycymicelles were found to be promising nano-formulations for treating acetaminophen overdose-induced hepatotoxicity.</p>","PeriodicalId":11263,"journal":{"name":"Drug Development and Industrial Pharmacy","volume":" ","pages":"1-16"},"PeriodicalIF":2.4,"publicationDate":"2025-06-30","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144505095","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}