Pharmaceutics最新文献

{"title":"Unraveling Vulnerabilities and Pathways Responsible for AITL Malignancy to Improve Patients' Treatment.","authors":"Chiara Martinello, Adrien Krug, Pau Marin-Escudero, Aurélia Pollet, François Lemonnier, Laurent Boyer, Els Verhoeyen","doi":"10.3390/pharmaceutics18101292","DOIUrl":"https://doi.org/10.3390/pharmaceutics18101292","url":null,"abstract":"<p><p>Angioimmunoblastic T-cell lymphoma (AITL) is an aggressive subtype of peripheral T-cell lymphoma characterized by poor clinical outcomes following conventional CHOP-based chemotherapy and the lack of effective disease-specific therapeutic options. The disease finds its origin in CD4 follicular helper T (Tfh) cells and is driven by recurrent genetic alterations, including mutations in <i>TET2</i>, <i>RHOA</i>, <i>DNMT3A</i>, and <i>IDH2.</i> Despite the rarity of AITL, preclinical models have been fundamental in elucidating disease pathogenesis, identifying key molecular vulnerabilities and providing platforms for the evaluation of novel therapeutic strategies. These studies have highlighted multiple targetable pathways, including aberrant mTOR, T-cell receptor and NF-κB signaling. Additionally, widespread epigenetic alterations in the neoplastic T-cells were uncovered due to mutations in epigenetic modifiers in AITL. More recently, metabolic reprogramming has emerged as an additional therapeutic vulnerability, revealing a strong dependence of AITL cells on mitochondrial respiration and lipid metabolism, particularly the choline metabolic pathway. Advances in the understanding of AITL biology have also accelerated the development of immunotherapeutic strategies. Monoclonal antibodies, antibody-drug conjugates, bispecific antibodies, immune checkpoint inhibitors and chimeric antigen receptor T-cell therapies have shown encouraging preclinical and early clinical activity. Of note, the first preclinical results on an in vivo CAR-T-cell approach for AITL are reported. Here we provide a broad overview of AITL, discussing its biological features, pathogenesis, preclinical models, current treatment landscape, and recent advances in therapeutic approaches.</p>","PeriodicalId":19894,"journal":{"name":"Pharmaceutics","volume":"18 10","pages":""},"PeriodicalIF":6.9,"publicationDate":"2026-10-12","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"149271878","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"An Engineered Floating Nanoparticulate System to Modulate Biopharmaceutical Performance and Therapeutic Efficacy of Tapentadol in Chronic Neuropathic Pain Management.","authors":"Ranju Soni, Sheelu Sharma, Manu Sharma","doi":"10.3390/pharmaceutics18101282","DOIUrl":"https://doi.org/10.3390/pharmaceutics18101282","url":null,"abstract":"<p><p><b>Background:</b> Tapentadol is an effective centrally acting analgesic for treating neuropathic pain. However, its short half-life, high first-pass metabolism, and requirement for frequent dosing limit its therapeutic effect and patient compliance. The purpose of the present innovation was to develop cost-effective tapentadol-loaded floating nanoparticles (TFNs) for sustained oral delivery. <b>Methods:</b> TFNs were prepared using the double emulsion solvent evaporation method. The effects of various formulation and process parameters, including polymer ratio, drug concentration, surfactant concentration and type, sonication time, and external phase volume were systematically studied. Analytical physicochemical characterization, morphology, buoyancy and drug release behavior were carried out. In vivo performance was evaluated by performing pharmacokinetic, tissue distribution, and pharmacodynamics studies in a chronic constriction injury model. <b>Results:</b> The optimized formulation exhibited spherical shape with nano-size (320.66 ± 17.50 nm), and good entrapment efficiency (82.85 ± 6.57%). Analytical characterization confirmed successful drug encapsulation and compatibility with formulation components. The engineered floating nanoparticulate architecture allowed both long gastric drug retention and a controlled drug release, governed by an anomalous diffusion-controlled mechanism. Pharmacokinetic evaluation revealed 3.36-fold higher relative oral bioavailability from TFNs. In addition, 1.49-fold higher drug availability in brain with TFNs was observed. Pharmacodynamic studies demonstrated a marked reduction in neuropathic pain responses, confirming the superior and prolonged analgesic effect of TFNs. <b>Conclusions:</b> The findings establish the developed TFNs as a promising controlled-release system for effective and sustained management of neuropathic pain. Even so, further studies focusing on large-scale production, long-term safety, and clinical evaluation are necessary before the formulation can be advanced for clinical application.</p>","PeriodicalId":19894,"journal":{"name":"Pharmaceutics","volume":"18 10","pages":""},"PeriodicalIF":6.9,"publicationDate":"2026-10-10","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"149271769","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Emerging Technologies in Granulation: Process Analytical Technologies and Modeling Approaches in Pharmaceutical Development and Manufacturing.","authors":"Panagiotis Pentsis, Maria Chountoulesi, Eirini Christodoulou, Natassa Pippa","doi":"10.3390/pharmaceutics18101286","DOIUrl":"https://doi.org/10.3390/pharmaceutics18101286","url":null,"abstract":"<p><p>In the present review, 32 studies, published between 2020 and 2026, were reviewed to identify recent advances in pharmaceutical granulation. Emphasis is placed on the integration of real-time monitoring technologies, recent Process Analytical Technologies (PATs) approaches, the relationships between critical process parameters (CPPs) and critical quality attributes (CQAs) affecting the product, and continuous manufacturing, as well as the implementation of modern data processing models. Increased attention was paid to continuous granulation using twin-screw extrusion, alongside the use of spectroscopic technologies for monitoring the production continuum. Finally, novel modeling approaches are discussed, revealing a transition from solely empirical methods toward hybrid models that combine data analysis tools with mechanistic process understanding and Artificial Intelligence (AI)-driven applications, yielding a new era with the transformation of both batch and continuous manufacturing. The study highlights the integration of PATs, modeling and QbD to enhance process understanding and control, but also challenges from a regulatory framework perspective that resulting from these technological advancements.</p>","PeriodicalId":19894,"journal":{"name":"Pharmaceutics","volume":"18 10","pages":""},"PeriodicalIF":6.9,"publicationDate":"2026-10-10","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"149271947","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"RETRACTED: Mehenni et al. Preparation and Characterization of Spherical Amorphous Solid Dispersion with Amphotericin B. <i>Pharmaceutics</i> 2018, <i>10</i>, 235.","authors":"Lyes Mehenni, Malika Lahiani-Skiba, Guy Ladam, François Hallouard, Mohamed Skiba","doi":"10.3390/pharmaceutics18101283","DOIUrl":"10.3390/pharmaceutics18101283","url":null,"abstract":"<p><p>The journal retracts the article titled \"Preparation and Characterization of Spherical Amorphous Solid Dispersion with Amphotericin B\" [...].</p>","PeriodicalId":19894,"journal":{"name":"Pharmaceutics","volume":"18 10","pages":""},"PeriodicalIF":6.9,"publicationDate":"2026-10-10","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC13655828/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"149169104","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Pyrvinium Attenuates Amiodarone-Induced Pulmonary Fibrosis in Male Rats: Association with Modulation of Wnt/β-Catenin Related Proteins.","authors":"Shaima Kutbi, Hala Attia, Nouf M Alrasheed, Maha M Arafah, Ahlam M Alhusaini, Maha A Al-Amin, Rehab Ali, Wedad S Sarawi","doi":"10.3390/pharmaceutics18101289","DOIUrl":"https://doi.org/10.3390/pharmaceutics18101289","url":null,"abstract":"<p><p><b>Background/Objectives:</b> Amiodarone (AmoD) is an effective antiarrhythmic drug whose use is limited by life-threatening pulmonary fibrosis. Although Wnt/β-catenin signaling contributes to several lung diseases, its involvement in AmoD-induced pulmonary fibrosis remains unknown. This study investigated whether Wnt/β-catenin signaling is altered during AmoD-induced pulmonary fibrosis and whether its pharmacological modulation with pyrvinium (Pyrv) attenuates this toxicity. <b>Methods:</b> Rats were allocated into four groups and treated for five weeks as follows: normal control, AmoD (30 mg/kg/day), Pyrv (60 µg/kg/day), and AmoD + Pyrv. Pulmonary injury and fibrosis were evaluated using histopathological examination, Masson's trichrome staining, immunohistochemical assessment of collagen I, α-smooth muscle actin (α-SMA), and transforming growth factor-β1 (TGF-β1), and measurement of inflammatory cytokines, tumor necrosis factor-α (TNF-α) and interleukin-6 (IL-6), and Th1/Th2-related cytokines. Wnt/β-catenin-associated proteins, including Wnt3a, active β-catenin, and glycogen synthase kinase-3β (GSK-3β), were evaluated by Western blotting. <b>Results:</b> AmoD induced marked pulmonary architectural disruption, inflammatory cell infiltration, increased lung weight/body weight ratio, collagen deposition, and increased expression of TGF-β1, α-SMA, and collagen I, as well as increased levels of TNF-α, IL-6, and disruption of Th1/Th2 immune balance. At the molecular level, AmoD increased Wnt3a, active β-catenin, and the p-GSK-3β/total GSK-3β ratio. Co-administration of Pyrv significantly attenuated the histopathological, inflammatory, immune, and fibrotic alterations and reduced the AmoD-associated changes in Wnt/β-catenin-related proteins. <b>Conclusions:</b> The findings indicate that AmoD-induced pulmonary injury and fibrosis are associated with modulation of Wnt/β-catenin related proteins and that Pyrv treatment attenuates these pathological changes. Targeting this pathway could be a promising protective strategy to prevent fibrogenesis during AmoD treatment.</p>","PeriodicalId":19894,"journal":{"name":"Pharmaceutics","volume":"18 10","pages":""},"PeriodicalIF":6.9,"publicationDate":"2026-10-10","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"149271900","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"A Mesalazine-Aloperine Co-Amorphous System for Simultaneous Dissolution Enhancement, Permeability Improvement, and Synergistic Anti-Ulcerative Colitis Activity: A Combined Pharmaceutics and Network Pharmacology Study.","authors":"Huan Su, Ningzi Guo, Song Yuan, Junyi Huang, Ningyi Wei, Hui Xu, Yang Liu","doi":"10.3390/pharmaceutics18101288","DOIUrl":"https://doi.org/10.3390/pharmaceutics18101288","url":null,"abstract":"<p><p><b>Background/Objectives:</b> Mesalazine (MSZ), the first-line therapy for ulcerative colitis (UC), is a BCS Class IV drug limited by poor aqueous solubility and low intestinal permeability, which together restrict colonic drug delivery and therapeutic efficacy. This study aimed to develop a co-amorphous (CAM) system of MSZ and aloperine (ALO) to enhance MSZ dissolution and permeation while achieving anti-UC synergy. <b>Methods:</b> The MSZ-ALO CAM system was prepared via solvent evaporation and characterized by PXRD, DSC, FTIR, and ¹H NMR. Equilibrium solubility, intrinsic dissolution rate (IDR), and in vitro permeability were assessed under biorelevant pH conditions. Physical stability was evaluated under long-term and accelerated conditions. Network pharmacology predicted potential therapeutic targets and synergistic mechanisms. <b>Results:</b> Solid-state characterization confirmed a homogeneous single-phase CAM system stabilized mainly by a carboxylate-ammonium ionic bond and hydrogen bonding. At pH 4.5, where MSZ solubility was lowest, equilibrium solubility and IDR increased up to 71.9-fold and 35.8-fold, respectively. In vitro permeability at pH 6.5 increased 2-fold. The system remained physically stable for eight months under dry conditions and withstood accelerated stresses without recrystallization. Network pharmacology identified 51 shared targets among MSZ, ALO, and UC, enriched in MAPK, HIF-1, and AMPK pathways; core hubs included HSP90AA1, SRC, CASP3, GSK3B, and ALB. <b>Conclusions:</b> This study presented the first MSZ-ALO CAM system that simultaneously addresses the dual solubility and permeability barriers of MSZ and provided a multi-target pharmacological basis for synergistic UC therapy, offering a promising pharmaceutical strategy for colon-targeted delivery.</p>","PeriodicalId":19894,"journal":{"name":"Pharmaceutics","volume":"18 10","pages":""},"PeriodicalIF":6.9,"publicationDate":"2026-10-10","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"149271722","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Artificial Intelligence-Based Quality Control of Pharmaceutical Tablets: A Visual Dataset and Benchmark for Automated Defect Detection.","authors":"Tahir Mahmood, Sabi Ur Rehman, Arslan Niamat, Sung Jae Lee, Kang Ryoung Park","doi":"10.3390/pharmaceutics18101287","DOIUrl":"https://doi.org/10.3390/pharmaceutics18101287","url":null,"abstract":"<p><p><b>Background/Objectives</b>: Automated visual inspection of pharmaceutical tablets is increasingly important for detecting manufacturing defects and maintaining consistent product quality. Progress in artificial intelligence-based defect classification is, however, constrained by the scarcity of publicly accessible image datasets covering defective tablets under diverse visual conditions. This study introduces the PharmaVision (PV) dataset, a public visual dataset and benchmark for classifying normal and defective compressed tablets. <b>Methods</b>: The PV dataset contains 640 smartphone-acquired images spanning varied tablet products, backgrounds, and lighting, with fixed tablet-level splits (190/190 training, 30/30 validation, and 100/100 test images for the normal and defective classes, respectively). Twelve representative architectures spanning classical convolutional networks, mobile networks, and vision transformers were benchmarked under an identical protocol using accuracy, precision, recall, and harmonic mean of precision and recall (F1-score), with 95% confidence intervals and paired statistical tests. Cross-dataset generalization was assessed on the independent pillQC dataset without fine-tuning, and efficiency was profiled using parameters, Giga floating-point operations (GFLOPs), latency, and throughput. <b>Results:</b> EfficientNetV2-S achieved the highest F1-score on the PV test set (88.56%), although paired statistical tests did not distinguish it from Xception (87.08%) or Swin-B (85.71%). On pillQC, GoogLeNet and EfficientNetV2-S showed the strongest cross-dataset performance, whereas both vision transformers declined relative to their in-domain results. AlexNet gave the highest theoretical throughput (602.41 frames per second (FPS), median latency 1.66 ms), whereas ShuffleNetV2 and MobileNetV3-small offered the smallest parameter counts. <b>Conclusions</b>: In-domain accuracy, cross-dataset robustness, and measured latency diverged, with no single architecture best on all three axes. The PV dataset, code, and evaluation protocol are publicly available on GitHub to support reproducible AI-based tablet quality control.</p>","PeriodicalId":19894,"journal":{"name":"Pharmaceutics","volume":"18 10","pages":""},"PeriodicalIF":6.9,"publicationDate":"2026-10-10","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"149271779","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Brazilian Red Propolis Extract-Loaded Colloidal Systems Derived from Microemulsion Compositions: Physicochemical, Antioxidant, and Antileishmanial Properties.","authors":"Salvana P M Costa, Ighor C Barreto, Kathylen V F Dos Santos, Nataly C S Gama, Monique A Vila Nova, Victor Hugo V Sarmento, Louisianny G da Rocha, Irinaldo D Basílio, Camila M B R G Panjwanig, Ticiano G do Nascimento","doi":"10.3390/pharmaceutics18101284","DOIUrl":"https://doi.org/10.3390/pharmaceutics18101284","url":null,"abstract":"<p><p><b>Background/Objectives</b>: Brazilian red propolis is a rich source of isoflavonoids with promising antioxidant and antileishmanial activities. However, its poor aqueous solubility and chemical instability limit its pharmaceutical application. This study aimed to develop microemulsion-based systems containing high concentrations of Brazilian red propolis extract (RPE) and evaluate their physicochemical properties, phytochemical composition, antioxidant capacity, and antileishmanial activity. <b>Methods</b>: Pseudoternary phase diagrams were constructed by water titration to select suitable microemulsion compositions. RPE was subsequently incorporated into the selected compositions to obtain RPE-loaded colloidal systems. The three selected RPE-free microemulsions and their corresponding RPE-loaded systems were characterized by pH, electrical conductivity, dynamic light scattering, rheological measurements, and polarized light microscopy (PLM). The RPE-loaded systems were further evaluated for phenolic marker content, antioxidant activity, and in vitro activity against <i>Leishmania</i> infantum. <b>Results</b>: Three RPE-loaded colloidal systems (F2-RPE12, F3-RPE30, and F4-RPE50) were developed. F2-RPE12 exhibited characteristics consistent with an oil-in-water microemulsion. Conductivity and PLM indicated physicochemical changes after RPE incorporation in F3-RPE30 and F4-RPE50, with localized birefringent features at higher RPE concentrations. Among the RPE-loaded systems, F4-RPE50 showed the highest phenolic and flavonoid contents and antioxidant activity. The RPE-loaded systems exhibited lower IC₅₀ values than RPE alone, with IC₅₀ values of 3.14, 2.28, and 0.56 µg·mL^-1 for F2-RPE12, F3-RPE30, and F4-RPE50, respectively, compared with 5.90 µg·mL^-1 for RPE. <b>Conclusions</b>: Overall, F4-RPE50 showed the most favorable phytochemical and biological performance, and the physicochemical and optical changes observed in the RPE-loaded systems open new avenues for investigating the relationship between structural organization and formulation performance.</p>","PeriodicalId":19894,"journal":{"name":"Pharmaceutics","volume":"18 10","pages":""},"PeriodicalIF":6.9,"publicationDate":"2026-10-10","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"149271788","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Preparation and Investigation of Solvatomorphs of Anti-Tumor Candidate RA-XII.","authors":"Feng Cao, Song Zhang, Qicheng Duan, Haitao Dou, Yinghui Liang, Ninghua Tan","doi":"10.3390/pharmaceutics18101285","DOIUrl":"https://doi.org/10.3390/pharmaceutics18101285","url":null,"abstract":"<p><p>RA-XII, a unique natural cyclopeptide, is a potential anti-colorectal cancer candidate by mainly inhibiting protective autophagy, SREBP-1-dependent lipid biogenesis and suppressing activation of the Akt-mTOR pathway in HCT-116 cells. However, there have been no investigations into its solid forms, and its poor solubility restricts its application in the development of clinical anticancer agents. <b>Background/Objectives</b>: To investigate and develop advantageous medicinal solid forms of RA-XII and further improve its solubility characteristics. <b>Methods</b>: Various recrystallization methods were used to screen crystal forms of RA-XII, and single crystals (Forms I, II and V) were obtained by the vapor diffusion method. The forms were characterized by powder X-ray diffraction (PXRD), spectroscopy (FTIR, Raman), thermal analyses (DSC, TGA) and scanning electron microscopy (SEM). Structural parameters were determined by single crystal X-ray diffraction (SCXRD). The solubility and intrinsic dissolution rate were determined in a pH 7.4 pharmaceutical buffer solution with water. Hirshfeld surface analyses, molecular electrostatic potential surface (MEPs) analyses and molecular dynamics (MD) simulations were employed to reveal differences in hydrogen bond interactions of the crystal structure. <b>Results</b>: Five solvatomorphs and an amorphous form of RA-XII were successfully obtained. Then, three single crystals of Forms I, II and V were obtained, and their conformations were investigated. Hirshfeld surface analyses and crystal structures revealed significant differences in hydrogen bonding interactions and molecular packing. Moreover, MEPs analyses and MD suggested the formation mechanisms of RA-XII solvatomorphs, in which the hydrogen bonding strengths increase between RA-XII and solvent molecules. <b>Conclusions</b>: Form I is physically more stable and exhibits great solubility in water. Form I possesses significant medicinal advantages. These findings provide valuable insights into understanding the solvatomorph mechanisms and the quality control of RA-XII.</p>","PeriodicalId":19894,"journal":{"name":"Pharmaceutics","volume":"18 10","pages":""},"PeriodicalIF":6.9,"publicationDate":"2026-10-10","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"149271771","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Preparation of Excipient-Free Molnupiravir Microparticles for Pulmonary Drug Delivery and Process Evaluation via Machine Learning.","authors":"Juncheng Hu, Yucheng Huang, Jiahao Luo, Jiayi Wang, Haoyang Chen, Minghao Lian, Ning Xue, Xiang Luo, Kaiqi Shi, Bin Dong, Hanhan Li","doi":"10.3390/pharmaceutics18101290","DOIUrl":"https://doi.org/10.3390/pharmaceutics18101290","url":null,"abstract":"<p><p><b>Background/Objective:</b> Molnupiravir (EIDD-2801) was originally designed to treat influenza A virus and showed broad-spectrum antiviral activity, including against influenza virus, Ebola virus, coronavirus and other viruses. <b>Methods:</b> In this study, molnupiravir microparticles were firstly prepared by spray freeze-drying (SFD) and jet milling (JM) methods. Meanwhile, machine learning methodology was applied to evaluate the influence of process parameters such as feeding rate, concentration, and nebulization pressure on powder properties. <b>Results:</b> According to SEM images, the microparticles prepared by SFD presented a porous and near-spherical structure. Moreover, the fine particle fraction (FPF) and mass median aerodynamic diameter (MMAD) of the optimal inhalable powder reached up to 70.19 ± 2.06% and 2.80 ± 0.16 μm, proving the excellent aerodynamic performance. <b>Conclusions:</b> The molnupiravir micropowder showed preliminary short-term storage behavior after storage for 28 days at 25 °C and 60% RH.</p>","PeriodicalId":19894,"journal":{"name":"Pharmaceutics","volume":"18 10","pages":""},"PeriodicalIF":6.9,"publicationDate":"2026-10-10","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"149271890","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}