AAPS PharmSciTech最新文献

{"title":"Self-emulsifying Delivery System for Improving Biopharmaceutical Performance of a Novel Antitubercular Agent: Formulation Development, Biological Activity and Pharmacokinetic Evaluation","authors":"Gourav Paudwal,&nbsp;Rigzin Dolkar,&nbsp;Anjali Negi,&nbsp;Mahir Bhardwaj,&nbsp;Rashmi Sharma,&nbsp;Parvinder Pal Singh,&nbsp;Prem N. Gupta","doi":"10.1208/s12249-026-03495-3","DOIUrl":"10.1208/s12249-026-03495-3","url":null,"abstract":"<div><p>A nitroimidazole-derived lead (IIIM-019) was developed as a part of our institutional drug discovery program in the area of tuberculosis. This molecule suffers from poor aqueous solubility and to overcome this limitation, lipid-based self-emulsifying drug delivery system (SEDDS) was developed. The SEDDS was characterized for emulsification efficiency, droplet size, stability and drug release. The morphology of SEDDS was investigated by transmission electron microscopy (TEM). The cellular uptake of formulation was assessed in Caco-2 cells and anti-tubercular activity was evaluated in M. tuberculosis H37Rv. Further, the pharmacokinetic profile of formulation was investigated in Balb/C mice. The optimal formulation, F2, was selected based on clarity, particle size, and stability. Characterization studies confirmed that F2 possessed favorable attributes, including a particle size of 120.6 ± 0.7 nm, and thermodynamic stability. The dissolution study revealed significantly enhanced release profile of IIIM-019 from SEDDS compared to its native form. The developed formulation showed uptake in Caco-2 cells and it also exhibited significantly improved anti-tubercular activity. Further, pharmacokinetic study indicated higher plasma exposure and decreased clearance than unformulated IIIM-019. The developed SEDDS formulation increased solubility, dissolution, plasma exposure, and therapeutic effectiveness of IIIM-019, representing a promising carrier for oral administration of investigated anti-tubercular lead.</p><h3>Graphical Abstract</h3><div><figure><div><div><picture><source><img></source></picture></div></div></figure></div></div>","PeriodicalId":6925,"journal":{"name":"AAPS PharmSciTech","volume":"27 7","pages":""},"PeriodicalIF":5.1,"publicationDate":"2026-09-09","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"148918153","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":"Process Analytical Technology Integration in 3D Printing Processes: Benefits and Challenges","authors":"Swaroop J. Pansare,&nbsp;Mohammad Kashif Iqubal,&nbsp;Canberk Kayalar,&nbsp;Bhanu Prakash Dongala,&nbsp;Rizwan Shaikh,&nbsp;Sunil Kumar Thota,&nbsp;Ziyaur Rahman,&nbsp;Mansoor A. Khan","doi":"10.1208/s12249-026-03526-z","DOIUrl":"10.1208/s12249-026-03526-z","url":null,"abstract":"<div><p>Three-dimensional printing (3DP) manufacturing technologies will transform pharmaceutical industry, offering the ability to produce personalized medicine and complex dosage forms with diverse geometries, with the advantage of on-demand dispensing. Maintaining consistent product quality and regulatory compliance pose major challenges in the current landscape due to the inherent variability and multivariate complexity of 3DP. Employing Process Analytical Technology (PAT) with Quality by Design (QbD) and continuous manufacturing (CM) principles provides the necessary framework for real-time monitoring (RTM), control, and understanding of critical process parameters and quality attributes. As a result, key PAT tools are now applied to various 3DP processes such as extrusion-based printing, powder bed fusion, and inkjet printing, utilizing spectroscopic, thermal, imaging, and emerging sensing technologies. Data generated from these tools are further processed using chemometric models, machine learning (ML), and multivariate data analysis for real-time decision-making and closed-loop control, thus enabling smart manufacturing. Although progress has been made, certain challenges remain regarding PAT, model transferability, validation, scalability, data management, and regulatory issues. This promotes a continuously evolving landscape for implementing PAT in 3DP that supports standardization, real-time release testing (RTRT), and lifecycle management. Emerging technologies focus on combining PAT with artificial intelligence (AI), digital twins, and automated feedback systems to develop self-regulating, adaptive 3DP platforms. This review highlights PAT's role as a key element in advancing pharmaceutical 3DP from experimental applications to robust, scalable, and regulatory-compliant manufacturing, offering a comprehensive overview of current technologies, data analytics, regulatory issues, challenges, and future directions in the field.</p><h3>Graphical Abstract</h3>\u0000<div><figure><div><div><picture><source><img></source></picture></div></div></figure></div></div>","PeriodicalId":6925,"journal":{"name":"AAPS PharmSciTech","volume":"27 7","pages":""},"PeriodicalIF":5.1,"publicationDate":"2026-09-09","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://link.springer.com/content/pdf/10.1208/s12249-026-03526-z.pdf","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"148918056","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Correction: Use of Incurred Sample Reproducibility Data to Support Long Term Stability of Therapeutic Antibodies in Clinical Bioanalytical Methods","authors":"Catherine L. Brockus,&nbsp;Likitha Venkatesh","doi":"10.1208/s12249-026-03504-5","DOIUrl":"10.1208/s12249-026-03504-5","url":null,"abstract":"","PeriodicalId":6925,"journal":{"name":"AAPS PharmSciTech","volume":"27 7","pages":""},"PeriodicalIF":5.1,"publicationDate":"2026-09-08","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"148910627","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":"pH-Responsive Chitosan-Coated Spanlastic Nanovesicles for Enhanced Lung-Targeted Delivery of Brilliant Blue G in Acute Lung Injury","authors":"Elsayed A. Elmorsy,&nbsp;Ahmed Y. Kira,&nbsp;Sameh Saber,&nbsp;Abdulaziz A. Alsalloom,&nbsp;Mostafa M. Khodeir,&nbsp;Rabab S. Hamad,&nbsp;Mohamed A. M. Ali,&nbsp;Hamad Alsaykhan,&nbsp;Mohammed Alorini,&nbsp;Anis Ahmad Chaudhary,&nbsp;Mohamed R. Abdel-Hamed,&nbsp;Manal M. Kamal,&nbsp;Hagir H. T. Ahmed,&nbsp;Syed Suhail Ahmed,&nbsp;Abdelrahman El-Sayed,&nbsp;Maha M. Amer","doi":"10.1208/s12249-026-03482-8","DOIUrl":"10.1208/s12249-026-03482-8","url":null,"abstract":"<div><p> Acute lung injury (ALI) involves alveolar–capillary barrier disruption, inflammatory amplification, oxidative stress, and loss of alveolar architecture. This study developed pH-responsive chitosan-coated spanlastic nanovesicles as a pharmaceutical platform for lung-targeted delivery of Brilliant Blue G (BBG), a P2X7 receptor antagonist. BBG-loaded spanlastics were prepared by thin-film hydration and optimized using a 2³ factorial design assessing the effects of Span 60:BBG ratio, Span 60:edge activator ratio, and edge activator type on vesicle size, zeta potential, and entrapment efficiency. The optimized formulation was coated with chitosan to achieve surface cationization, enhance colloidal stability, support mucoadhesive interaction with lung tissue, and provide pH-responsive release. BBG-Ch-SPNs exhibited nanoscale size, positive zeta potential, high entrapment efficiency, acceptable hemocompatibility, and sustained drug release, with greater BBG liberation under acidic conditions relevant to inflamed lung microenvironments. Release kinetic analysis supported diffusion-controlled release with pH-dependent polymer relaxation, while stability testing confirmed preservation of vesicle size, surface charge, and drug entrapment over three months. In vivo, BBG-Ch-SPNs improved pulmonary retention and lung exposure compared with free BBG and uncoated spanlastics, demonstrating enhanced lung-targeting efficiency. Therapeutically, BBG-Ch-SPNs reduced BALF protein leakage, LDH activity, NOx levels, and leukocyte influx while preserving alveolar architecture and limiting septal thickening, edema, and inflammatory infiltration. These effects were accompanied by restored antioxidant defenses and suppression of P2X7R/NF-κB/NLRP3 inflammasome signaling. Overall, chitosan-coated spanlastics improved BBG formulation performance, pH-responsive delivery, pulmonary biodistribution, and therapeutic efficacy, supporting their potential as a targeted nanotherapeutic system for ALI.</p><h3>Graphical Abstract</h3>\u0000<div><figure><div><div><picture><source><img></source></picture></div></div></figure></div></div>","PeriodicalId":6925,"journal":{"name":"AAPS PharmSciTech","volume":"27 7","pages":""},"PeriodicalIF":5.1,"publicationDate":"2026-09-08","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"148910444","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":"Development of Carboxymethyl Cellulose–Gelatin Aerogels for Urea Delivery","authors":"Mesa Phonhai,&nbsp;Thunchanok Keawsrikul,&nbsp;Chalida Niamnuy,&nbsp;Paweena Prapainainar,&nbsp;Thongthai Witoon,&nbsp;Manop Charoenchaitrakool","doi":"10.1208/s12249-026-03537-w","DOIUrl":"10.1208/s12249-026-03537-w","url":null,"abstract":"<div><p>Urea is an effective therapeutic agent for the treatment of chronic hyponatremia; however, its high water solubility leads to rapid dissolution, limiting sustained therapeutic efficacy and patient compliance. This study aimed to develop and evaluate controlled-release urea delivery systems using biopolymer-based aerogel and xerogel matrices. Urea-loaded aerogel and xerogel composites were prepared from carboxymethyl cellulose (CMC) and surplus gelatin (GE), crosslinked with varying concentrations of glutaraldehyde (GA). The effects of the CMC:GE ratio and GA concentration on gelation behavior, swelling properties, and urea release kinetics were systematically investigated. Structural and thermal characteristics were analyzed using scanning electron microscopy (SEM), X-ray diffraction (XRD), and differential scanning calorimetry (DSC). The CMC:GE ratio significantly influenced the structural and functional properties of the composites. Among the formulations studied, the aerogel with a CMC:GE ratio of 1:3 and 5% (v/v) GA  xhibited the most effective controlled-release performance, providing a markedly prolonged urea release compared with the corresponding xerogel. XRD and DSC analyses indicated that urea was predominantly present in an amorphous or molecularly dispersed state within the aerogel matrix, with traces of residual crystallinity. SEM observations revealed reduced pore size and increased matrix density following urea loading, indicating a more compact internal structure favorable for sustained release. CMC–GE aerogels crosslinked with GA are promising controlled-release carriers for urea. The optimized 1:3 CMC:GE aerogel demonstrated enhanced swelling and significantly slower urea release than xerogels and medical-grade urea, highlighting its potential for sustained urea delivery.</p><h3>Graphical Abstract</h3>\u0000<div><figure><div><div><picture><source><img></source></picture></div></div></figure></div></div>","PeriodicalId":6925,"journal":{"name":"AAPS PharmSciTech","volume":"27 7","pages":""},"PeriodicalIF":5.1,"publicationDate":"2026-09-08","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"148910694","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":"Slugging-induced Mechanistic Coupling of Microcrystalline Cellulose-starch Disintegrants for Enhanced Tablet Disintegration","authors":"Ming Shin Neo,&nbsp;Paul Wan Sia Heng,&nbsp;Celine Valeria Liew","doi":"10.1208/s12249-026-03518-z","DOIUrl":"10.1208/s12249-026-03518-z","url":null,"abstract":"<div><p>Disintegrant performance in insoluble, poorly disintegrating matrices is strongly influenced by how the excipients are assembled at the granule level. This study investigated densified microcrystalline cellulose-starch (MCC-starch, 4:1) granular systems as direct compression disintegrants. In the screening stage, co-processed MCC-starch granules prepared by slugging at 10–190 MPa were incorporated into dibasic calcium phosphate (DCP) tablets at 10–15%, w/w. Disintegration behavior exhibited a strong dependence on slugging pressure, with low-pressure, less dense granules failing to disintegrate the tablets within the 15-min test window, while denser granules progressively shifted performance toward rapid disintegration. Based on these trends, granular densification (12.5%, w/w disintegrant; 190 MPa slugging) was examined with different starch types, maize and rice, and blends. Across both starch groups, tablets formulated with co-processed granules disintegrated significantly faster than tablets incorporating physical mixtures of separately densified components, while tablet tensile strength remained comparable between these formulations. Scanning electron microscopy images supported pressure-dependent changes in granule consolidation. Collectively, the results identify intragranular co-location of MCC and starch within a composite granule, rather than densification alone, as the critical determinant of disintegrant efficiency in DCP tablets, driven by the mechanistic coupling of MCC-mediated wicking and localized starch swelling when wetted.</p><h3>Graphical Abstract</h3>\u0000<div><figure><div><div><picture><source><img></source></picture></div></div></figure></div></div>","PeriodicalId":6925,"journal":{"name":"AAPS PharmSciTech","volume":"27 7","pages":""},"PeriodicalIF":5.1,"publicationDate":"2026-09-08","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://link.springer.com/content/pdf/10.1208/s12249-026-03518-z.pdf","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"148910455","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"An Investigation of Water Vapor Sorption for Improving Reconstitution Pathways of Freeze-Dried Lipid Nanoparticles Stabilized by Trehalose/Mannitol Excipients","authors":"Kyuya Nakagawa,&nbsp;Yuji Senga","doi":"10.1208/s12249-026-03498-0","DOIUrl":"10.1208/s12249-026-03498-0","url":null,"abstract":"<div><p>Lipid-based nanocarriers have been intensively developed to achieve controlled drug delivery and maintain pharmacological stability, especially, for mRNA-based vaccines. Freeze-drying is commonly recognized as a key technique that allows nanoparticles to be converted into a dry form, stored under ambient conditions, and reconstituted at time of use. This study investigated the influence of reconstitution conditions of freeze-dried lipid nanoparticles (LNPs) stabilized with trehalose or trehalose/mannitol mixtures on disintegration and aggregation upon rehydration. Direct water pipetting and water vapor sorption methods were applied to reconstitute the freeze-dried specimens. When LNPs were reconstituted by the water pipetting, a slight decrease in particle size and a significant increase in particle number concentration were observed. On the other hand, when reconstituted by the pipetting subsequent to the water vapor sorption, slight increases in particle size and particle number concentration were observed. These results suggested that the water pipetting lead significant disintegration of LNPs whereas the water vapor sorption inhibited the particle damage and lead slight aggregation. However, when the duration of the water vapor sorption time was prolonged, the LNPs could be disintegrated due to the crystallization of trehalose. The addition of mannitol delayed the trehalose crystallization, and restricted the disintegration of LNPs upon rehydration. A practical suggestion based on this study would be to use a formulation of trehalose and mannitol mixture, allow it to absorb water vapor until the glass–rubber transition, and rehydrate before the crystallization of trehalose, which would be an appropriate reconstitution path to allow the LNP to be retained its original formation.</p><h3>Graphical Abstract</h3>\u0000<div><figure><div><div><picture><source><img></source></picture></div></div></figure></div></div>","PeriodicalId":6925,"journal":{"name":"AAPS PharmSciTech","volume":"27 7","pages":""},"PeriodicalIF":5.1,"publicationDate":"2026-09-08","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"148910580","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":"Advances and Hurdles of PLGA-Based Therapy for Pancreatic Cancer","authors":"Nusaiba Al-Nemrawi,&nbsp;Ghena Majdi AbuAlna’aj,&nbsp;Razan Ahmad AL Hazaimeh,&nbsp;Shaikha Adnan Al-Quraan,&nbsp;Noor Ahmad Bani Yaseen,&nbsp;Fatima Hameedat,&nbsp;Flávia Sousa","doi":"10.1208/s12249-026-03508-1","DOIUrl":"10.1208/s12249-026-03508-1","url":null,"abstract":"<p>Pancreatic cancer (PC) is one of the most aggressive malignancies, with a very low 5-year survival rate due to late diagnosis, rapid metastasis, and resistance to conventional therapies. The pancreas’s deep anatomical location complicates early detection, and most patients present with advanced or metastatic disease, limiting surgical options. Current chemotherapy regimens often face challenges such as systemic toxicity, poor tumor penetration, and acquired chemoresistance. To overcome these limitations, poly(lactic-co-glycolic acid) (PLGA)-based nanoparticles (NPs) have emerged as a promising strategy for targeted drug delivery in PC treatment. PLGA NPs offer controlled drug release, enhanced bioavailability, and reduced off-target effects. Their surface can be functionalized with ligands to actively target PC cells, improving therapeutic efficacy while minimizing damage to healthy tissues. Additionally, PLGA NPs can encapsulate chemotherapeutics, siRNA, or immunomodulators, enabling combination therapy to combat drug resistance and tumor microenvironment barriers. Recent advances in nanomedicine highlight the potential of PLGA-based systems to enhance tumor accumulation, overcome stromal resistance, and improve therapy outcomes. This review discusses the current challenges in PC treatment, the role of PLGA NPs in targeted drug delivery, and future perspectives for clinical translation. Integrating PLGA NPs could revolutionize PC therapy, offering hope for improved survival and quality of life.</p>","PeriodicalId":6925,"journal":{"name":"AAPS PharmSciTech","volume":"27 7","pages":""},"PeriodicalIF":5.1,"publicationDate":"2026-09-08","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"148910598","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":"Oral Gastro-resistant Formulations – State of the Art, Advances and Prospects: A Review","authors":"Maja Frankiewicz,&nbsp;Bartosz Maciejewski,&nbsp;Malgorzata Sznitowska","doi":"10.1208/s12249-026-03529-w","DOIUrl":"10.1208/s12249-026-03529-w","url":null,"abstract":"<div><p>Gastro-resistant oral dosage forms remain essential for protecting acid-labile active pharmaceutical ingredients, reducing gastric irritation, and enabling site-specific intestinal or colonic drug delivery. Although conventional enteric coatings are well established, their <i>in vivo</i> performance remains affected by gastric pH variability, food intake, alcohol exposure, gastric residence time, coating integrity, and interindividual differences in gastrointestinal transit. Advanced platforms, including ready-to-fill enteric capsules, hot-melt technologies, three-dimensional printing, electrospinning, micro- and nanocarriers, and pH-responsive hydrogels, have been proposed to overcome these limitations, but many remain at an experimental or early translational stage. This narrative review critically evaluates gastro-resistant oral formulations from technological, physiological, and regulatory perspectives. It compares established and emerging technologies with respect to release mechanisms, material requirements, processing constraints, acid-resistance performance, translational maturity, scalability, regulatory acceptability, and commercial feasibility. Recent advances, including rapid-release double-coating concepts and dual pH- and microbiota-triggered colonic delivery systems, are also discussed. Overall, the field is moving from simple gastric protection toward more predictive and functionally complex oral drug delivery platforms. Future progress will depend on biorelevant dissolution testing, stronger <i>in vitro</i>–<i>in vivo</i> correlations, quality-by-design approaches, process analytical technologies, greener manufacturing, and regulatory pathways capable of accommodating innovative materials and personalized oral therapeutics.</p></div>","PeriodicalId":6925,"journal":{"name":"AAPS PharmSciTech","volume":"27 7","pages":""},"PeriodicalIF":5.1,"publicationDate":"2026-09-08","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://link.springer.com/content/pdf/10.1208/s12249-026-03529-w.pdf","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"148910314","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Next-Generation Solid Dispersion of Andrographolide Attenuated Inflammation and Oxidative Stress in an Activated RAW264.7 Macrophage-Based In Vitro Model Relevant to Ulcerative Colitis","authors":"Pawan Devangan,&nbsp;Dinesh Kumar Chandanpalli,&nbsp;Atul Mourya,&nbsp;Jitender Madan","doi":"10.1208/s12249-026-03528-x","DOIUrl":"10.1208/s12249-026-03528-x","url":null,"abstract":"<div><p>Ulcerative colitis (UC) is fundamentally mediated by macrophage-driven immune dysregulation that amplifies mucosal inflammation. Andrographolide (AGD) has potent anti-inflammatory and antioxidant properties; however, AGD shows poor water solubility and bioavailability. To surmount these challenges, next-generation solid dispersion of AGD with soluplus and TPGS was engineered via the solvent evaporation method. Optimized SD8 demonstrated a ~ 7.14-fold upsurge in solubility, 18.78 ± 0.98% drug content, 93.86 ± 3.19% assay, micellar colloid size of 220.5 ± 20.8 nm, and ζ-potential of -4.18 ± 0.03 mV in aqueous dispersion. ATR-FTIR and ¹H-NMR analyses indicated that the –OH group of AGD participated in intermolecular hydrogen bonding with soluplus and TPGS. Moreover, the halo diffraction pattern, the vanishing of the endothermic peak, the lack of birefringence under polarized light, and the loss of crystallinity collectively confirmed the amorphous nature of SD8. SD8 exhibited ~ 2.06-fold decline of contact angle, ~ 4.70- and ~ 2.94-fold boosts in dissolution rate in simulated intestinal fluid (SIF) and simulated colonic fluid (SCF), respectively, and ~ 40.7-fold upsurge in apparent permeability coefficient compared to AGD. SD8 markedly enhanced cytoprotection over AGD, evidenced by significantly lower IC₅₀ values in both lipopolysaccharide (LPS)-activated (7.17 ± 0.15-µg/mL; <i>P</i> &lt; 0.0001) and H₂O₂-exposed (7.92 ± 0.15-µg/mL; <i>P</i> &lt; 0.01) RAW264.7 macrophages. SD8 significantly suppressed LPS-induced NO production (<i>P</i> &lt; 0.05) and pro-inflammatory mediators (IL-1β, IL-6, TNF-α; <i>P</i> &lt; 0.0001). SD8 markedly reduced ROS levels, significantly restored antioxidant enzymes SOD (<i>P</i> &lt; 0.0001), CAT (<i>P</i> &lt; 0.001), GSH (<i>P</i> &lt; 0.0001), and lowered TBARS (<i>P</i> &lt; 0.0001) with respect to H₂O₂-exposed RAW264.7 cells. In conclusion, SD8 represents an auspicious drug delivery tactic for further preclinical evaluation to advance its translational potential in the therapeutic management of UC.</p></div>","PeriodicalId":6925,"journal":{"name":"AAPS PharmSciTech","volume":"27 7","pages":""},"PeriodicalIF":5.1,"publicationDate":"2026-09-08","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"148910320","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}