Drug Development and Industrial Pharmacy最新文献

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Rutin-enabled improved systemic exposure of doxorubicin via nanostructured lipid carriers: a proof of concept through novel LC-MS/MS analysis. 芦丁通过纳米结构脂质载体改善阿霉素的全身暴露:通过新型LC-MS/MS分析的概念证明。
IF 2.6 4区 医学
Drug Development and Industrial Pharmacy Pub Date : 2026-09-01 Epub Date: 2026-07-18 DOI: 10.1080/03639045.2026.2703044
Neha Agarwal, Avijit Kumar Bakshi, Dilip Panwar, Patil Rohit Santosh, Prabhat Ranjan Mishra
{"title":"Rutin-enabled improved systemic exposure of doxorubicin via nanostructured lipid carriers: a proof of concept through novel LC-MS/MS analysis.","authors":"Neha Agarwal, Avijit Kumar Bakshi, Dilip Panwar, Patil Rohit Santosh, Prabhat Ranjan Mishra","doi":"10.1080/03639045.2026.2703044","DOIUrl":"10.1080/03639045.2026.2703044","url":null,"abstract":"<p><strong>Objective: </strong>The objective of this study was to develop and validate a sensitive LC-MS/MS method for simultaneous quantification of doxorubicin (DOX) and rutin (RUT) in plasma and to apply it as a proof-of-concept to investigate rutin-enabled enhancement of systemic DOX exposure <i>via</i> nanostructured lipid carriers (NLCs).</p><p><strong>Significance: </strong>Poor oral bioavailability and dose-limiting toxicity restrict the clinical utility of DOX. Co-delivery with RUT, a bioactive flavonoid known to improve drug absorption and therapeutic response, may overcome these limitations. A robust bioanalytical strategy is essential to evaluate such combination-based nanotherapeutic systems.</p><p><strong>Methods: </strong>A simultaneous LC-MS/MS method was developed and validated in rat plasma in accordance with ICH guidelines. Dual drug-loaded NLCs were prepared using an emulsification-sonication technique and optimized through a Quality-by-Design approach. The optimized NLCs were characterized for particle size, polydispersity index and zeta potential. <i>In vitro</i> cytotoxicity was evaluated in MDA-MB-231 breast cancer cells, followed by pharmacokinetic studies in rats.</p><p><strong>Results: </strong>The validated method demonstrated excellent linearity, accuracy, precision, recovery, minimal matrix effects, absence of carryover, acceptable stability and robustness. Optimized NLCs exhibited a particle size of 171.27 ± 0.45 nm, a PDI of 0.28 ± 0.01, and a zeta potential of -23.53 ± 0.38 mV. Combination delivery of DOX and RUT resulted in a two-fold reduction in IC<sub>50</sub> values compared with individual drugs. Pharmacokinetic analysis revealed a nearly three-fold increase in DOX AUC<sub>0</sub>-t compared with free DOX.</p><p><strong>Conclusion: </strong>Rutin-enabled NLCs significantly enhance the systemic exposure and therapeutic performance of DOX, validated through a novel simultaneous LC-MS/MS bio-analytical approach.</p>","PeriodicalId":11263,"journal":{"name":"Drug Development and Industrial Pharmacy","volume":" ","pages":"1803-1819"},"PeriodicalIF":2.6,"publicationDate":"2026-09-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"148419580","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}
引用次数: 0
Stimuli-responsive solid lipid nanoparticles for targeted drug delivery in biofilm-resistant infections: advances and challenges. 刺激反应固体脂质纳米颗粒靶向药物递送在生物膜耐药感染:进展和挑战。
IF 2.6 4区 医学
Drug Development and Industrial Pharmacy Pub Date : 2026-09-01 Epub Date: 2026-07-21 DOI: 10.1080/03639045.2026.2703793
Dakshinesh Parameswaran, Suriya Prakaash Kanan, Damodharan Narayanasamy
{"title":"Stimuli-responsive solid lipid nanoparticles for targeted drug delivery in biofilm-resistant infections: advances and challenges.","authors":"Dakshinesh Parameswaran, Suriya Prakaash Kanan, Damodharan Narayanasamy","doi":"10.1080/03639045.2026.2703793","DOIUrl":"10.1080/03639045.2026.2703793","url":null,"abstract":"<p><strong>Objective: </strong>The aim of this study was to explore the design, mechanisms, and therapeutic potential of stimuli-responsive solid lipid nanoparticles (SLNs) for biofilm-targeted drug delivery, highlighting recent advances and future directions.</p><p><strong>Significance of review: </strong>Biofilm-associated infections present a significant challenge in healthcare owing to the protective extracellular matrix (EPS), which restricts antibiotic penetration and promotes biofilm resistance. SLNs have emerged as promising drug delivery systems owing to their biocompatibility, drug-loading capacity, and controlled release characteristics. Stimuli-responsive SLNs, which release drugs in response to environmental triggers such as pH, enzymes, temperature, and light, offer enhanced targeting and improved drug delivery efficiency to biofilms. Notable preclinical examples include ciprofloxacin, vancomycin, rifampin and tobramycin-all of which have been formulated in SLNs/nanostructured lipid carriers with improved antibiofilm activity versus free drug <i>in vitro</i> and in some <i>in vivo</i> models.</p><p><strong>Key findings: </strong>Preclinical studies have demonstrated that SLN-based formulations significantly reduce biofilm biomass and enhance antibiotic efficacy against biofilm-associated infections. Stimuli-responsive SLNs facilitate deeper penetration of biofilms, thereby improving drug retention and therapeutic outcomes. However, challenges such as limited drug-loading capacity, stability, manufacturability, and clinical translation remain significant barriers to the widespread adoption of SLN-based therapies.</p><p><strong>Conclusions: </strong>Stimuli-responsive SLNs represent a promising strategy for overcoming biofilm resistance and enhancing antibiotic delivery. Although preclinical data are promising, addressing formulation challenges and improving scalability are essential for successful clinical translation. Further research on optimizing SLN design and understanding biofilm interactions will be critical for advancing SLN-based therapies for biofilm-associated infections.</p>","PeriodicalId":11263,"journal":{"name":"Drug Development and Industrial Pharmacy","volume":" ","pages":"1700-1714"},"PeriodicalIF":2.6,"publicationDate":"2026-09-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"148445085","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}
引用次数: 0
Synergistic anticancer potential of andrographolide and paclitaxel: a dose-reduction strategy to minimize toxicity and enhance therapeutic efficacy. 穿心莲内酯和紫杉醇的协同抗癌潜力:减少剂量以减少毒性和提高治疗效果。
IF 2.6 4区 医学
Drug Development and Industrial Pharmacy Pub Date : 2026-09-01 Epub Date: 2026-07-03 DOI: 10.1080/03639045.2026.2696023
Romi Singh, Pooja Yadav, Dipti Srivastava, Nirupama Lal, Nishi Tandon, Mohini Chaurasia, S J S Flora
{"title":"Synergistic anticancer potential of andrographolide and paclitaxel: a dose-reduction strategy to minimize toxicity and enhance therapeutic efficacy.","authors":"Romi Singh, Pooja Yadav, Dipti Srivastava, Nirupama Lal, Nishi Tandon, Mohini Chaurasia, S J S Flora","doi":"10.1080/03639045.2026.2696023","DOIUrl":"10.1080/03639045.2026.2696023","url":null,"abstract":"<p><strong>Objective: </strong>To study the synergistic anticancer efficacy of Andrographolide (AG), a bioactive phytochemical with immunomodulator properties, and paclitaxel (PTX), a frontline chemotherapeutic agent, when administered as co-loaded nanoemulsion, to enhance therapeutic outcome with minimal adverse effect.</p><p><strong>Significance: </strong>The proposed nanoemulsion is expected to achieve synergistic anticancer effects, and minimize systemic toxicity.</p><p><strong>Key findings: </strong>Cytotoxic potential of AG and PTX at various molar concentrations using Chou-Talalay method were determined. A synergistic ratio (1:1) was identified and used as coloaded nanoemulsion. The system was optimized for particle size, zeta potential and encapsulation efficiency. Thermal and spectral characterization techniques were employed to evaluate drug identity and compatibility, while HPLC-based analytical method was developed for simultaneous quantification of AG and PTX in % entrapment and drug release samples. Further evaluated for MTT test, cell uptake study, scratch migration test, apoptosis and cell cycle arrest. Tumor regression test confirmed therapeutic efficacy and acute toxicity test ensure the safety of developed formulation. The AG-PTX nanoemulsion exhibited enhanced cellular uptake, cell apoptosis, and cell-cycle arrest <i>in vitro</i> compared to monotherapies. <i>In vivo</i> studies using a syngeneic tumor (invasive mammary carcinoma) bearing mouse model demonstrated significant tumor regression (10-fold), improved and reduced systemic toxicity, as shown by stable body weight and histopathological assays.</p><p><strong>Conclusion: </strong>Co-delivery of AG and PTX <i>via</i> targeted nanocarrier offers a promising dose reduction strategy to circumvent the dose limiting toxicity of PTX while maintaining/enhancing its anticancer efficacy. Further, the findings suggest a translational potential for AG as a chemosensitizer in combination therapy regimens.</p>","PeriodicalId":11263,"journal":{"name":"Drug Development and Industrial Pharmacy","volume":" ","pages":"1768-1789"},"PeriodicalIF":2.6,"publicationDate":"2026-09-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"148337990","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}
引用次数: 0
Rosuvastatin-metformin co-processing: enhanced dissolution, oral bioavailability, and therapeutic efficacy through a solvent-minimized approach. 瑞舒伐他汀-二甲双胍协同加工:通过溶剂最小化方法增强溶出度、口服生物利用度和治疗效果。
IF 2.6 4区 医学
Drug Development and Industrial Pharmacy Pub Date : 2026-09-01 Epub Date: 2026-07-25 DOI: 10.1080/03639045.2026.2703986
Soha M El-Masry, Shaimaa K Mostafa, Shaimaa M Khedr, Abeer E Abdelwahab, Sally A Helmy
{"title":"Rosuvastatin-metformin co-processing: enhanced dissolution, oral bioavailability, and therapeutic efficacy through a solvent-minimized approach.","authors":"Soha M El-Masry, Shaimaa K Mostafa, Shaimaa M Khedr, Abeer E Abdelwahab, Sally A Helmy","doi":"10.1080/03639045.2026.2703986","DOIUrl":"10.1080/03639045.2026.2703986","url":null,"abstract":"<p><strong>Objective: </strong>Rosuvastatin calcium (ROS) exhibits poor aqueous solubility and dissolution-limited oral absorption. This study aimed to develop an oral co-processed fixed-dose combination of ROS and metformin HCl (MET) to enhance ROS dissolution and oral bioavailability.</p><p><strong>Significance: </strong>This work highlights wet co-grinding as a simple, solvent-minimized approach for improving the biopharmaceutical performance of ROS while supporting fixed-dose combination development.</p><p><strong>Methods: </strong>Rosuvastatin/metformin (ROS/MET) co-processed systems were prepared using a solvent-minimized wet co-processing approach. The formulations were evaluated for drug content and characterized using Fourier-transform infrared spectroscopy (FTIR), powder X-ray diffraction (PXRD), thermal analysis (DSC/TGA), and scanning electron microscopy (SEM). <i>In vitro</i> dissolution studies were performed to assess drug dissolution behavior. <i>In vivo</i> comparative pharmacokinetic evaluation in rats (<i>n</i> = 3 per group) assessed oral bioavailability, <i>in vitro</i>-<i>in vivo</i> correlation (IVIVC) analysis and liver biodistribution, while anti-hyperlipidemic efficacy was assessed in hyperlipidemic rats (<i>n</i> = 6 per group) through biochemical and histopathological analyses.</p><p><strong>Results: </strong>The co-processed mixtures significantly enhanced rosuvastatin dissolution, with the 20:500 ROS ratio (F2) showing the best performance. Across pH 1.2, 4.5, and 6.8, F2 achieved Q5 values of 73.6%, 82.5%, and 92.7%, respectively, compared with 12.4%, 19.9%, and 28.6% for unprocessed ROS. Correspondingly, dissolution efficiency increased from 21.3-42.6% for ROS to 76.2-90.4% for F2. Comparative pharmacokinetic evaluation revealed a 21.5% increase in relative bioavailability, a 1.34-fold increase in Cmax, and a more rapid onset of action compared to unprocessed rosuvastatin. Additionally, the co-processed F2 demonstrated improved liver drug distribution and superior anti-hyperlipidemic effects in poloxamer 407-induced hyperlipidemic rats.</p><p><strong>Conclusion: </strong>The co-processing of rosuvastatin with metformin presents a solvent-minimized and effective strategy to enhance the dissolution, bioavailability, and therapeutic efficacy of rosuvastatin. This approach holds promise for the clinical management of complex conditions such as dyslipidemia and type 2 diabetes mellitus.</p>","PeriodicalId":11263,"journal":{"name":"Drug Development and Industrial Pharmacy","volume":" ","pages":"1849-1868"},"PeriodicalIF":2.6,"publicationDate":"2026-09-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"148445120","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}
引用次数: 0
Sustainable nanomaterial production from fruit waste: green synthesis of ZnO nanoparticles for antioxidant, antimicrobial, and therapeutic applications in wound healing and cancer therapy. 从水果废料中可持续生产纳米材料:用于伤口愈合和癌症治疗的抗氧化、抗菌和治疗应用的ZnO纳米颗粒的绿色合成。
IF 2.6 4区 医学
Drug Development and Industrial Pharmacy Pub Date : 2026-09-01 Epub Date: 2026-07-03 DOI: 10.1080/03639045.2026.2695097
Abdulsalam A Alqahtani, Abdulhakim M Saeed, Afroze Alam, Kalyani Pathak, Jon Jyoti Sahariah, Osman Ae Elnoubi, Basel A Abdel-Wahab, Saeed Alqahtani, Noura M Alshiban, Marwa B Bakir, Mohammad Zaki Ahmad
{"title":"Sustainable nanomaterial production from fruit waste: green synthesis of ZnO nanoparticles for antioxidant, antimicrobial, and therapeutic applications in wound healing and cancer therapy.","authors":"Abdulsalam A Alqahtani, Abdulhakim M Saeed, Afroze Alam, Kalyani Pathak, Jon Jyoti Sahariah, Osman Ae Elnoubi, Basel A Abdel-Wahab, Saeed Alqahtani, Noura M Alshiban, Marwa B Bakir, Mohammad Zaki Ahmad","doi":"10.1080/03639045.2026.2695097","DOIUrl":"10.1080/03639045.2026.2695097","url":null,"abstract":"<p><strong>Objective: </strong>Green synthesis of zinc oxide (ZnO) nanoparticles (NPs) using the aqueous extract of fruit waste, investigating their antioxidants, antimicrobial, anticancer, and wound healing properties.</p><p><strong>Significance: </strong>This study presents an eco-friendly synthesis of ZnO NPs that repurpose organic fruit waste, contributing to sustainable practices in nanomaterial production. The potential applications of ZnO NPs as antioxidant, antimicrobial, and anticancer agents, as well as their role in wound healing are explored.</p><p><strong>Methods: </strong>ZnO NPs were synthesized using the aqueous extract of fruit waste, and were characterized using UV-Visible spectroscopy, dynamic light scattering (DLS), X-ray powder diffraction (XRD), Fourier transform infrared (FTIR), and SEM-EDX. Antioxidant activity was measured using the 2,2-diphenyl-1-picrylhydrazyl (DPPH) assay. Cytotoxicity was assessed on A549 lung carcinoma cells, and antimicrobial activity was tested against <i>Staphylococcus aureus</i> and <i>Pseudomonas aeruginosa</i>. A gel formulation containing chitosan (CS) and <i>Aloe vera</i> (CS-AV)/ZnO NPs was evaluated for wound healing in an infected wound model.</p><p><strong>Results: </strong>The synthesized ZnO NPs exhibited nanoscale size, good colloidal stability, and polygonal morphology. They demonstrated strong antioxidant activity, dose-dependent cytotoxicity against A549 cells, and significant antibacterial effects. Incorporation of ZnO NPs into the CS-AV gel markedly enhanced wound healing, achieving complete wound closure by Day 21. Histopathological analysis further confirmed improved tissue regeneration, as evidenced by reduced inflammation, increased fibrosis, and well-developed collagen formation.</p><p><strong>Conclusion: </strong>Fruit waste-derived ZnO NPs offer promising antimicrobial, antioxidant, anticancer, and wound healing properties.</p>","PeriodicalId":11263,"journal":{"name":"Drug Development and Industrial Pharmacy","volume":" ","pages":"1750-1767"},"PeriodicalIF":2.6,"publicationDate":"2026-09-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"148327602","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}
引用次数: 0
Computational and experimental approaches for HPMCAS-based solid dispersions of abiraterone acetate: formulation, characterization, and biopharmaceutical enhancement evaluation. 基于hpmcas的醋酸阿比特龙固体分散体的计算和实验方法:配方、表征和生物制药增强评价。
IF 2.6 4区 医学
Drug Development and Industrial Pharmacy Pub Date : 2026-08-21 DOI: 10.1080/03639045.2026.2719750
Namrata S Desai, Amol S Shete, Snehal S Patil, Priyanka P Shinde, Anuj R Yadav, Yadishma A Gaude, Somdatta Y Chaudhari, Anita V Malusare
{"title":"Computational and experimental approaches for HPMCAS-based solid dispersions of abiraterone acetate: formulation, characterization, and biopharmaceutical enhancement evaluation.","authors":"Namrata S Desai, Amol S Shete, Snehal S Patil, Priyanka P Shinde, Anuj R Yadav, Yadishma A Gaude, Somdatta Y Chaudhari, Anita V Malusare","doi":"10.1080/03639045.2026.2719750","DOIUrl":"10.1080/03639045.2026.2719750","url":null,"abstract":"<p><strong>Objective: </strong>To enhance the solubility and dissolution rate of poorly watersoluble drug Abiraterone Acetate (ABA) by developing solid dispersions using hydroxypropyl methylcellulose acetate succinate (HPMCAS-LF).</p><p><strong>Significance: </strong>Enhancing the biopharmaceutical performance of ABA is crucial due to its extremely poor solubility and dissolution characteristics. The present study demonstrates that HPMCAS-LF-based solid dispersion effectively improves the physicochemical performance of ABA through enhanced solubility, dissolution, and <i>in vitro</i> drug diffusion.</p><p><strong>Methods: </strong>Molecular dynamics (MD) simulations were conducted over 100 ns to evaluate the stability and structural behavior of the ABA-HPMCAS-LF complex, with analyses including root mean square deviation (RMSD), radius of gyration and solvent-accessible surface area. Binding free energy was measured using MM-GBSA calculations. Solid dispersions were prepared using cogrinding and solvent assisted cogrinding techniques and characterized by FTIR, PXRD, thermal analysis (TGA/DTG-DTA), SEM, and solid-state<sup>13</sup>C NMR. Solubility, <i>in vitro</i> dissolution, <i>in vitro</i> drug diffusion, hygroscopicity, and anticancer activity were assessed.</p><p><strong>Results: </strong>The ABA-HPMCAS-LF complex exhibited dynamic stability, with RMSD stabilization at 6-7 Å and a binding free energy of -33.45 kcal/mol, indicating strong van der Waals, lipophilic, and Coulombic interactions. Solid dispersions demonstrated a 1.07 to 16.72-fold increase in solubility compared to pure ABA, and <i>in vitro</i> release enhanced drug dissolution across different media. Diffusion increased by 6.36-fold in simulated gastric fluid (SGF 1.2) and 2.55-fold in phosphate buffer (pH 6.8) relative to pure ABA.</p><p><strong>Conclusion: </strong>The solid dispersion of ABA with HPMCAS-LF significantly improved solubility, dissolution, and diffusion, highlighting its potential for enhanced oral bioavailability and improved therapeutic outcomes.</p>","PeriodicalId":11263,"journal":{"name":"Drug Development and Industrial Pharmacy","volume":" ","pages":"1-16"},"PeriodicalIF":2.6,"publicationDate":"2026-08-21","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"148757755","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}
引用次数: 0
Design space optimization of roller compaction incorporating mill type and process parameters to mitigate loss of tabletability using a Box-Behnken experimental design. 采用Box-Behnken实验设计,结合磨机类型和工艺参数对辊压实设计空间进行优化,以减轻可压实性损失。
IF 2.6 4区 医学
Drug Development and Industrial Pharmacy Pub Date : 2026-08-18 DOI: 10.1080/03639045.2026.2718399
Thus Thareesucheevakul, Chaiyakarn Pornpitchanarong, Praneet Opanasopit, Prin Chaksmithanont, Prasopchai Patrojanasophon
{"title":"Design space optimization of roller compaction incorporating mill type and process parameters to mitigate loss of tabletability using a Box-Behnken experimental design.","authors":"Thus Thareesucheevakul, Chaiyakarn Pornpitchanarong, Praneet Opanasopit, Prin Chaksmithanont, Prasopchai Patrojanasophon","doi":"10.1080/03639045.2026.2718399","DOIUrl":"10.1080/03639045.2026.2718399","url":null,"abstract":"<p><strong>Objective: </strong>This study aimed to investigate the effects of mill type and process parameters on granule and tablet quality attributes during roller compaction and to develop a design space for optimizing granule flowability and tablet tensile strength.</p><p><strong>Significance: </strong>Roller compaction improves granule flowability but can reduce tabletability. Mill type remains underexplored despite its potential impact on granule properties and downstream tablet performance.</p><p><strong>Methods: </strong>Microcrystalline cellulose-based granules were prepared by roller compaction and milled using bar and knife rotors. The effects of screen size, mill speed, roll force, and mill type were evaluated using a Box-Behnken design. Granule size distribution, bed density, compressibility, flowability, granule shape, and tablet tensile strength were measured. Design space analysis was conducted using predefined criteria for angle of repose and tablet tensile strength.</p><p><strong>Results: </strong>Mill type significantly interacted with process parameters, leading to distinct trends in granule size, density, compressibility, and flowability. Larger screen size and higher roll force produced coarser and denser granules, improving flowability. However, higher roll force reduced tablet tensile strength. Opposite effects of mill speed were observed between the two rotor types, which may be associated with differences in milling mechanism and material-retention behavior within the milling chamber. Design space analysis identified limited operating regions satisfying both flowability and tablet strength criteria, and the model-predicted conditions were experimentally verified.</p><p><strong>Conclusions: </strong>Mill type was an important factor influencing roller compaction performance and should be considered during process optimization. The formulation- and equipment-specific design space enabled simultaneous optimization of granule flowability and tablet tensile strength.</p>","PeriodicalId":11263,"journal":{"name":"Drug Development and Industrial Pharmacy","volume":" ","pages":"1-14"},"PeriodicalIF":2.6,"publicationDate":"2026-08-18","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"148720162","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}
引用次数: 0
Leveraging bile acid transporters for enhanced liver targeting and anti-alcoholic efficacy of tectoridin via liposomal delivery. 利用胆汁酸转运体通过脂质体给药增强莪术苷的肝脏靶向性和抗酒精作用。
IF 2.6 4区 医学
Drug Development and Industrial Pharmacy Pub Date : 2026-08-01 Epub Date: 2026-06-19 DOI: 10.1080/03639045.2026.2676198
Xia Cao, Yaping Yang, Michael Adu-Frimpong, Hong Chen, Lili Yuan, Jollibekov Berdiyar, Jiangnan Yu, Qilong Wang, Ximing Xu
{"title":"Leveraging bile acid transporters for enhanced liver targeting and anti-alcoholic efficacy of tectoridin via liposomal delivery.","authors":"Xia Cao, Yaping Yang, Michael Adu-Frimpong, Hong Chen, Lili Yuan, Jollibekov Berdiyar, Jiangnan Yu, Qilong Wang, Ximing Xu","doi":"10.1080/03639045.2026.2676198","DOIUrl":"10.1080/03639045.2026.2676198","url":null,"abstract":"<p><strong>Objective: </strong>This study focused on improving the delivery of tectoridin, an anti-alcoholic compound from Pueraria flower, which suffers from poor solubility and low bioavailability when taken orally. To address this, we designed a biomimetic liposome system that targets the liver by harnessing the body's natural bile acid transport pathways.</p><p><strong>Significance: </strong>Successful clinical translation of many insoluble natural products, including tectoridin, is limited by their unfavorable pharmacokinetics. A liver-targeted strategy utilizing physiological transporters offers a promising means to enhance hepatic delivery and therapeutic efficacy, thereby addressing a critical hurdle in the development of plant-derived pharmaceuticals.</p><p><strong>Methods: </strong>Following bioactivity-guided isolation and identification of tectoridin, cholic acid-functionalized liposomes (LPs-tectoridin) were designed to actively target hepatocyte-specific transporters (NTCP/OATPs). The formulation was optimized and characterized for particle size, encapsulation efficiency, and <i>in vitro</i> dissolution. Pharmacokinetic, tissue distribution, and pharmacodynamic evaluations were performed in a rat model of ethanol-induced intoxication and liver injury.</p><p><strong>Results: </strong>The optimized liposomes exhibited a mean particle size of 157.55 ± 0.23 nm, a high encapsulation efficiency (>85%), and significantly improved the dissolution rate of tectoridin. <i>In vivo</i>, LPs-tectoridin increased the oral bioavailability (AUC<sub>0</sub>-<sub>24</sub>) by 2.11-fold and enhanced hepatic accumulation by 3-fold compared to free tectoridin. The formulation demonstrated superior anti-intoxication and hepatoprotective effects, notably reducing serum ALT and AST levels by 49.95% and 35.20%, respectively, and elevating hepatic SOD activity by 2.04-fold.</p><p><strong>Conclusions: </strong>This study not only confirms tectoridin as a principal anti-alcoholic constituent but also establishes a robust liver-targeted liposomal platform that harnesses intrinsic bile acid transport pathways. The strategy significantly improves the solubility, bioavailability, and therapeutic performance of tectoridin, offering a viable approach for enhancing the delivery of poorly soluble natural products in drug development.</p>","PeriodicalId":11263,"journal":{"name":"Drug Development and Industrial Pharmacy","volume":" ","pages":"1516-1530"},"PeriodicalIF":2.6,"publicationDate":"2026-08-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"148249504","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}
引用次数: 0
Pre-formulation study of 3D-printed topical film by semisolid extrusion incorporated with spray-dried extract of Punica granatum Linn. 半固态挤压加喷雾干燥石榴提取物3d打印外用膜的预配方研究。
IF 2.6 4区 医学
Drug Development and Industrial Pharmacy Pub Date : 2026-08-01 Epub Date: 2026-05-29 DOI: 10.1080/03639045.2026.2677648
José Roberto da Costa Rodrigues, João Victor Rocha Bitú, Camylla Janiele Lucas Tenório, Janaína Carla Barbosa Machado, Luiz Alberto Lira Soares, Magda Rhayanny Assunção Ferreira
{"title":"Pre-formulation study of 3D-printed topical film by semisolid extrusion incorporated with spray-dried extract of <i>Punica granatum</i> Linn.","authors":"José Roberto da Costa Rodrigues, João Victor Rocha Bitú, Camylla Janiele Lucas Tenório, Janaína Carla Barbosa Machado, Luiz Alberto Lira Soares, Magda Rhayanny Assunção Ferreira","doi":"10.1080/03639045.2026.2677648","DOIUrl":"10.1080/03639045.2026.2677648","url":null,"abstract":"<p><strong>Objective: </strong>To develop semisolid extrusion (SSE) 3D-printed topical films containing spray-dried extract (SDE) of <i>Punica granatum</i> Linn. leaves and determine how formulation properties and infill architecture influence film performance.</p><p><strong>Significance: </strong>Three-dimensional printing is a promising platform for individualized topical dosage forms with controlled geometry and composition. However, successful incorporation of herbal active ingredients into semisolid printable matrices requires appropriate preformulation to ensure printability, structural fidelity, and preservation of bioactive compounds after processing.</p><p><strong>Method: </strong>Printing inks containing <i>P. granatum</i> leaf SDE and biopolymers were screened using physicochemical, mechanical, and printability-related parameters, including collapse factor, printing angle, and printability. Films were then produced by SSE 3D printing with cubic or grid infill and characterized for tensile behavior, disintegration time, and total polyphenol recovery.</p><p><strong>Results: </strong>Preformulation screening enabled selection of inks suitable for SSE printing and successful production of structured topical films containing the herbal extract. Infill architecture significantly influenced film performance. Grid-patterned films showed greater rupture force (4.98 ± 0.66 N) and longer disintegration time (25.54 min) than cubic-patterned films (3.54 ± 0.55 N and 22.58 min, respectively), indicating greater mechanical resistance and slower matrix disruption. In contrast, cubic-patterned films showed higher total polyphenol recovery (34.491 vs. 27.037 g pyrogallol equivalents).</p><p><strong>Conclusion: </strong>SSE 3D printing proved to be a feasible technological strategy for obtaining candidate topical films containing <i>P. granatum</i> leaf SDE. The results demonstrate that both preformulation attributes and infill design influence key preliminary performance parameters, including structural integrity, disintegration, mechanical behavior, and polyphenol recovery. These findings support the use of internal architecture as a formulation tool to modulate film properties; however, further adhesion, release, permeation/retention, and dose uniformity studies are required to confirm the suitability of the system for topical application.</p>","PeriodicalId":11263,"journal":{"name":"Drug Development and Industrial Pharmacy","volume":" ","pages":"1531-1545"},"PeriodicalIF":2.6,"publicationDate":"2026-08-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"147986682","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}
引用次数: 0
Recent advances in cationic material integration for enhanced antimicrobial formulations. 增强型抗菌配方中阳离子材料集成的最新进展。
IF 2.6 4区 医学
Drug Development and Industrial Pharmacy Pub Date : 2026-08-01 Epub Date: 2026-06-01 DOI: 10.1080/03639045.2026.2680188
Sara Salatin, Shirin Ahmadi, Parvin Abedi Ghobadloo, Maryam Azarfarin, Samin Hamidi
{"title":"Recent advances in cationic material integration for enhanced antimicrobial formulations.","authors":"Sara Salatin, Shirin Ahmadi, Parvin Abedi Ghobadloo, Maryam Azarfarin, Samin Hamidi","doi":"10.1080/03639045.2026.2680188","DOIUrl":"10.1080/03639045.2026.2680188","url":null,"abstract":"<p><strong>Objective: </strong>To review recent advances in cationic antimicrobial systems - including surfactants, polymers, peptides, quaternary ammonium-based materials, and ionic-liquid-derived agents - and to summarize emerging strategies aimed at combating antibiotic-resistant bacteria.</p><p><strong>Significance of review: </strong>Cationic antimicrobial compounds provide a promising alternative to traditional antibiotics due to their membrane-disruptive action mediated by electrostatic interactions. This mechanism enables broad-spectrum activity while reducing the potential for resistance development.</p><p><strong>Key findings: </strong>A comprehensive evaluation of recent literature reveals substantial progress across multiple cationic antimicrobial platforms. Enhanced surfactants with improved membrane-disrupting efficiency, advanced cationic polymer architectures with greater biocompatibility, and engineered antimicrobial peptides (AMPs) with tunable properties have been reported. Furthermore, quaternary ammonium-based polymeric systems and rapidly expanding ionic-liquid antimicrobials demonstrate significant potential for diverse therapeutic and material applications.</p><p><strong>Conclusions: </strong>Cationic antimicrobial agents are advancing through varied chemical designs and formulation strategies, offering effective tools against resistant bacterial strains. Continued innovation across surfactant, polymer, peptide, and ionic-liquid systems highlights their increasing promise for both clinical and industrial implementation.</p>","PeriodicalId":11263,"journal":{"name":"Drug Development and Industrial Pharmacy","volume":" ","pages":"1443-1461"},"PeriodicalIF":2.6,"publicationDate":"2026-08-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"148028152","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}
引用次数: 0
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