Journal of Drug Delivery Science and Technology最新文献

{"title":"A synergistic microemulsion approach with cetyl myristoleate and hyaluronic acid for enhanced osteoarthritis therapy: In vitro and in vivo evaluation","authors":"Emre Şefik Çağlar ,&nbsp;Mehmet Evren Okur ,&nbsp;Bircan Kolbaşı ,&nbsp;Mustafa Şahin ,&nbsp;Yağmur Özhan ,&nbsp;Hande Sipahi ,&nbsp;İlknur Keskin ,&nbsp;Bahtiyar Demiralp ,&nbsp;Yüksel Antepüzümü Bolat ,&nbsp;Hatice Yeşim Karasulu ,&nbsp;Neslihan Üstündağ Okur","doi":"10.1016/j.jddst.2025.106694","DOIUrl":"10.1016/j.jddst.2025.106694","url":null,"abstract":"<div><div>Osteoarthritis is characterized by persistent pain and dysfunction in the joints due to joint deformity and degradation. This study intended to develop a new microemulsion formulation of hyaluronic acid incorporating cetyl myristoleate for intra-articular administration and pain control related to arthritis. A titration method was utilized to formulate the microemulsions. The formulations were assessed for clarity, pH, droplet size, polydispersity index, zeta potential, and <em>in vitro</em> release analysis. Additionally, CHON-001 healthy human cartilage fibroblast cells were assessed for cytocompatibility. The chosen formulation was examined <em>in vivo</em> in rats. The characterisation investigations revealed that the droplet diameters of the blank, hyaluronic acid loaded and both hyaluronic acid and cetyl myristoleate added as an excepient to the formulation used in <em>in vivo</em> studies were found 25.23 ± 3.14 nm, 36.35 ± 2.10 nm and 78.8 ± 0.4 nm, respectively. PDI values of the mentioned formulations were 0.298 ± 0.035, 0.232 ± 0.006 and 0.250 ± 0.032. The drug concentration in the formulations varied from 9.7 ± 0.2 to 9.9 ± 0.2 mg/mL. Cell culture tests demonstrated that the formulations had cytocompatible profiles. <em>In vivo</em> studies, Mankin scoring was performed to both show the occurrence of osteoarthritis and to demonstrate improvement. At the end of the study, it was observed that the hyaluronic acid-loaded cetyl myristoleate added formulation statistically significantly increased the improvement compared to the control group and the market product. MMP3 and caspase-3 positive cells were examined by immunohistochemical method. In the results obtained, the addition of cetyl myristoleate as an excipient to the formulation loaded with hyaluronic acid showed a synergistic effect and decreased MMP3 expression in a statistically significant way. However, the number of Caspase-3 positive cells was also significantly reduced in the group to which the formulation was applied. Transmission electron microscope images revealed that in the osteoarthritis animal group, cell integrity were disrupted, microvilli structures degenerated and vacuolization was detected in the cytoplasm of the chondrocytes. The cells showed normal morphology when compared with the patient in the animal groups.In conclusion, the created microemulsion technology may provide a more effective and prolonged therapy of hyaluronic acid in the treatment of osteoarthritis compared to conventional medications.</div></div>","PeriodicalId":15600,"journal":{"name":"Journal of Drug Delivery Science and Technology","volume":"106 ","pages":"Article 106694"},"PeriodicalIF":4.5,"publicationDate":"2025-02-06","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143378027","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":"Enhanced cytotoxicity of phyto-synthesized silver oxide nanostructures loaded with bleomycin sulfate for anticancer application","authors":"Amina Jabeen ,&nbsp;Abdulhameed Khan ,&nbsp;Pervaiz Ahmad ,&nbsp;Awais Khalid ,&nbsp;Satam Alotibi ,&nbsp;Imen Kebaili ,&nbsp;Syed Fakhar Abbas","doi":"10.1016/j.jddst.2025.106695","DOIUrl":"10.1016/j.jddst.2025.106695","url":null,"abstract":"<div><div>Biomaterials-based innovative targeted anticancer drug delivery systems with enhanced efficacy and limited side effects are highly required for effective monotherapy. The current work is an attempt to establish a novel bleomycin sulfate-loaded silver oxide nanostructures (AgONS-BLM) by using <em>Mentha spicata</em>-mediated synthesized silver oxide nanostructures (AgONS) and anticancer drug bleomycin sulfate (BLM) for potential anticancer applications. The cytotoxicity of Bleomycin sulfate loaded silver oxide nanostructures (AgONS-BLM) was assessed against breast cancer (MCF-7), Rhabdomyosarcoma (RD), and normal mouse embryonic fibroblast (NIH 3T3) cell lines by MTT and live/dead cell staining assays. At 0.09 mg/mL concentration of bleomycin, the synthesized AgONS-BLM nanostructure exhibited 93 % drug encapsulation efficiency with moderate stability as indicated by −24 mV zeta potential. Moreover, the synthesized AgONS-BLM nanostructure released 90 % and 79 % of the drug-loaded at pH 5 and 7.5, respectively. Furthermore, at 0.08 mg/ml concentration of AgONS-BLM, the viability of MCF-7 and RD cell lines reduced to 42 % and 44 %, respectively. The cytotoxic effect of AgONS-BLM was more pronounced as compared to bleomycin and AgONPs, alone. In addition, the cytotoxic effect of AgONS-BLM was more potent towards cancerous cells than normal cells in a dose-dependent manner. The preliminary results suggest that AgONS-BLM might be a promising anticancer drug delivery system for effective oncotherapy and further in vivo investigation of its potential anticancer applications is required.</div></div>","PeriodicalId":15600,"journal":{"name":"Journal of Drug Delivery Science and Technology","volume":"106 ","pages":"Article 106695"},"PeriodicalIF":4.5,"publicationDate":"2025-02-06","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143386604","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":"Recent advances and future prospects of engineered exosomes as advanced drug and gene delivery systems","authors":"Waleed Y. Rizg ,&nbsp;Majed A. Alghamdi ,&nbsp;Sherif El Saadany ,&nbsp;Osama A. Madkhali ,&nbsp;Anjana Karunakaran Nair ,&nbsp;Md Abdur Rashid ,&nbsp;Sabna Kotta","doi":"10.1016/j.jddst.2025.106696","DOIUrl":"10.1016/j.jddst.2025.106696","url":null,"abstract":"<div><div>Engineered exosomes (eEXOs) are promising nanocarriers for targeted drug and gene delivery. This review explores advancements in EXO engineering, including surface modifications to enhance targeting and uptake, loading techniques for diverse cargoes, and methods to improve stability and circulation time. eEXOs have potential in delivering small-molecule drugs, nucleic acids, and proteins for treating cancer, cardiovascular, neurodegenerative, and inflammatory diseases. Future prospects include integrating artificial intelligence and 3D bioprinting with EXO engineering for advanced therapeutic nanocarriers. Artificial and shape-eEXOs are also promising, offering a biocompatible platform for precise therapies across various diseases.</div></div>","PeriodicalId":15600,"journal":{"name":"Journal of Drug Delivery Science and Technology","volume":"106 ","pages":"Article 106696"},"PeriodicalIF":4.5,"publicationDate":"2025-02-06","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143379272","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 cell-derived vesicles by extrusion, a novel docetaxel drug delivery system for lung cancer","authors":"Javiera Carrasco-Rojas ,&nbsp;Gabriela Zavala ,&nbsp;Rafael Contreras-Lopez ,&nbsp;Belén Olivares ,&nbsp;Miriam Aarsund ,&nbsp;Marit Inngjerdingen ,&nbsp;Tuula A. Nyman ,&nbsp;Felipe I. Sandoval ,&nbsp;Orlando Ramírez ,&nbsp;Jessica Alarcón-Moyano ,&nbsp;Paulo Díaz-Calderón ,&nbsp;José Antonio Jara-Sandoval ,&nbsp;Christina M.A.P. Schuh","doi":"10.1016/j.jddst.2025.106693","DOIUrl":"10.1016/j.jddst.2025.106693","url":null,"abstract":"<div><div>Lung cancer (LC) has the highest mortality rate worldwide and novel therapies are being sought. Among those are cell-product-based therapies such as extracellular vesicles (EVs). Recently, it has been discovered that artificial cell-derived vesicle by extrusion (EXT) could be a potential tool to lower barriers to clinical translation. In this study we propose a formulation of human natural killer (NK) EXT encapsulating docetaxel (DTX) for LC therapy. EXT-DTXs were generated from NK cells by cell extrusion. EXTs and DTX-EXTs, were characterized and compared to EVs secreted by NK cells. All vesicles displayed a cup-shaped morphology with a mean size of &lt;200 nm and stable composition, with zeta potentials between −26 and −33 mV. DTX-EXT contained 14 ± 9.1 p.m. DTX per μg of EXT protein. The proteome of EVs, EXT and DTX-EXT was analyzed and revealed a distinct protein enrichment pattern for each group. Uptake inhibition studies identified clathrin-mediated endocytosis as the primary internalization pathway for all vesicle types in A549 and H1975 LC cells. Cytotoxicity assays demonstrated that DTX-EXTs induced significantly higher apoptosis and reduced cell viability compared to EVs and EXTs, with higher efficacy in A549 cells. Notably, DTX-EXTs induced cytotoxic effects at picomolar docetaxel concentrations, 300–600 times lower than free DTX. This study provides the first comprehensive characterization of docetaxel-loaded NK artificially cell-derived vesicle by extrusion, highlighting their potential as a novel therapeutic delivery system with enhanced anti-tumor efficacy. Future studies are warranted to further explore the therapeutic potential and safety profile of DTX-EXTs in cancer treatment.</div></div>","PeriodicalId":15600,"journal":{"name":"Journal of Drug Delivery Science and Technology","volume":"106 ","pages":"Article 106693"},"PeriodicalIF":4.5,"publicationDate":"2025-02-06","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143395777","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":"Bioinspired PCL-based composite scaffolds produced via hot melt extrusion and fused filament fabrication: An integrated workflow for enhanced bone regeneration","authors":"Carmela Tommasino ,&nbsp;Carla Sardo ,&nbsp;Angiola Guidone ,&nbsp;Alessandra Soriente ,&nbsp;Maria Grazia Raucci ,&nbsp;Tania Ciaglia ,&nbsp;Giulia Auriemma ,&nbsp;Rita Patrizia Aquino","doi":"10.1016/j.jddst.2025.106679","DOIUrl":"10.1016/j.jddst.2025.106679","url":null,"abstract":"<div><div>This study presents a comprehensive and integrated workflow for fabricating bioinspired, macroporous 3D scaffolds tailored for bone tissue engineering. Poly-(ε-caprolactone) (PCL) served as the base polymer, enriched with nature-derived fillers such as sodium alginate and microcrystalline cellulose, along with bioactive nano-hydroxyapatite ceramics, to enhance hydrophilicity, bioactivity, and cellular interactions.</div><div>A combined manufacturing approach was implemented to ensure uniform filler distribution and optimized scaffold performance: hybrid pellets preparation and composite filament production through Hot Melt Extrusion (HME), followed by scaffold fabrication using Fused Filament Fabrication (FFF). This multistep process allowed precise control over material composition, ensuring compatibility and consistency across fabrication stages.</div><div>The 3D printed scaffolds were characterized for printability, architecture, surface topography, thermal and mechanical properties, degradation behavior, swelling capacity, and drug release profiles. Incorporating nature-derived fillers improved hydrophilicity, swelling behavior, and biodegradation kinetics, while nano-hydroxyapatite enhanced mechanical strength and sustained release of dexamethasone. In vitro tests using murine pre-osteoblasts confirmed scaffold biocompatibility and osteogenic potential, promoting cell proliferation and differentiation. The findings underscore the potential of this integrated workflow for advancing scaffold design and bone regeneration.</div></div>","PeriodicalId":15600,"journal":{"name":"Journal of Drug Delivery Science and Technology","volume":"106 ","pages":"Article 106679"},"PeriodicalIF":4.5,"publicationDate":"2025-02-06","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143379273","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":"Dry granulation by roller compaction of paracetamol with different grades of mannitol","authors":"Luca Palugan ,&nbsp;Saliha Moutaharrik ,&nbsp;Anastasia Foppoli ,&nbsp;Giuseppe Buratti ,&nbsp;Alessandra Buscarini ,&nbsp;Alessandra Maroni ,&nbsp;Andrea Gazzaniga ,&nbsp;Matteo Cerea","doi":"10.1016/j.jddst.2025.106689","DOIUrl":"10.1016/j.jddst.2025.106689","url":null,"abstract":"<div><div>Roller compaction dry granulation is a manufacturing technology that has been increasingly used in the pharmaceutical industry for improving the flowability and bulk density of powder mixtures or to prevent segregation problems of high-potency drugs before tableting. To compare the potential of four different commercial grades of mannitol, powder (PO), spray-dried (XL and EZ) and granular (GR), in addressing the formulation of drugs with poor flowability and compaction properties, this work evaluated the performance of binary mixtures of these grades with varying contents (20–80%) of paracetamol powder, a material considered a model for having shown critical issues in this respect. Granules obtained with these mixtures by roller compaction at different pressures were characterized in terms of particle size distribution, bulk density, flow properties and tableting ability. Particles with the desired size (500–1300 μm), increased bulk density and appropriate flow properties could be achieved. Regarding tableting ability of granules, mixture prepared with mannitol spray-dried (XL and EZ) allowed to obtain the most resistant tablets at 20% drug content and an important reduction of tableting properties was observed at 40% and tableting with higher paracetamol content was not feasible. Mannitol GR allowed to prepare tablets only with granules containing 20% of drug, while granules prepared with mannitol PO permitted to achieve tablets up to 80% paracetamol, even if high roller compaction pressures were required and low mechanical resistant tablets were gained.</div></div>","PeriodicalId":15600,"journal":{"name":"Journal of Drug Delivery Science and Technology","volume":"106 ","pages":"Article 106689"},"PeriodicalIF":4.5,"publicationDate":"2025-02-05","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143395776","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":"Optimized delivery of Enalapril Maleate via polymeric Invasomal in-situ gel for glaucoma treatment: In vitro, in vivo, and histological studies","authors":"Asmaa M. Baiomy ,&nbsp;Mona K. Younis ,&nbsp;Rasha M. Kharshoum ,&nbsp;Alyaa Alsalhi ,&nbsp;Randa Mohammed Zaki ,&nbsp;Obaid Afzal ,&nbsp;Amira H. Hassan","doi":"10.1016/j.jddst.2025.106685","DOIUrl":"10.1016/j.jddst.2025.106685","url":null,"abstract":"<div><div>Glaucoma is a prevalent ocular condition requiring effective drug delivery systems to overcome the challenges of poor ocular bioavailability and rapid clearance. This study aimed to develop an innovative ophthalmic delivery system utilizing invasomes loaded with Enalapril Maleate to enhance therapeutic outcomes. Enalapril Maleate-loaded invasomes were prepared via a thin-film hydration method, with eight formulae containing varying amounts of terpenes, and evaluated for particle size, surface charge, drug loading efficiency, and in vitro release profile. The optimal formula (F6) was selected using Design Expert software and incorporated into in-situ gel preparations with polymers such as HPMC E15 and Carbopol 940. Compatibility studies of the optimized formulae were conducted using Raman spectroscopy. Among the prepared gels, G3 (containing 1.5 % w/v HPMC E15 and 14 % w/v Pluronic F127) exhibited superior physicochemical characteristics. In vitro and in vivo studies demonstrated that G3, derived from F6, significantly enhanced corneal penetration and prolonged drug release for up to 12 h, effectively reducing intraocular pressure. Histological evaluations revealed improved corneal cell structure in rabbits treated with G3 compared to other groups. The study successfully formulated an in-situ gel containing Enalapril Maleate-loaded invasomes, demonstrating enhanced drug retention, sustained release, and effective intraocular pressure reduction, highlighting its potential as a novel approach to glaucoma management.</div></div>","PeriodicalId":15600,"journal":{"name":"Journal of Drug Delivery Science and Technology","volume":"106 ","pages":"Article 106685"},"PeriodicalIF":4.5,"publicationDate":"2025-02-05","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143378107","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":"Investigation of Moxifloxacin-loaded terpenes enriched cationic cerosomes (TECs) as an adjunct pulmonary therapy for COVID-19: In-silico study; D-optimal optimization; aerodynamic simulation assessment and cytotoxic evaluation","authors":"Rofida Albash ,&nbsp;Carol Yousry ,&nbsp;Mahmoud A. El Hassab ,&nbsp;Wagdy M. Eldehna ,&nbsp;Ahmed Adel Alaa-Eldin","doi":"10.1016/j.jddst.2025.106683","DOIUrl":"10.1016/j.jddst.2025.106683","url":null,"abstract":"<div><div>Fluoroquinolone; a class of broad-spectrum antibiotics, was investigated as a treatment for COVID-19 symptoms. The objective of this investigation was to load Moxifloxacin hydrochloride (MOX) into Terpenes-enriched cationic cerosomes (TECs) for pulmonary delivery and investigate its antiviral activity against hCoV-19. Firstly, molecular dynamic simulation (MD) was used to study MOX binding to SARS-CoV-2 enzymes' active site. After confirming MOX activity, MD simulation was further used to confirm MOX interaction with the TECs components and their stability. MOX-TECs were then fabricated utilizing thin film hydration. D-optimal statistical design was constructed to figure out the influence of various preparation variables on vesicles’ (TECs) features namely, entrapment efficiency (EE%), particle size (PS), and polydispersity index (PDI) and select the optimal formulation parameters. The optimum formula was further prepared utilizing dimethyldidodecylammonium bromide (DDAB) as cationic surfactant. The optimum formula (O-TEC) showed EE% of 89 ± 1.00 %, PS of 257.00 ± 2.00 nm, PDI of 0.427 ± 0.008, and ZP of 37.60 ± 1.44 mV. After that, O-TEC was lyophilized to obtain dry inhalable powder. The aerodynamic aspects of the lyophilized O-TECs using cascade impactor demonstrated better lung deposition compared with MOX powder. Finally, the <em>in vitro cytotoxic</em> study confirmed that loading MOX into TECs enhanced its antiviral effect (lower IC₅₀ against hCoV-19 infected cells) while promoting its safety against normal cells with a selectivity index of 9.39 compared to 4.44 for MOX powder. The acquired conclusions approved the competence of employing MOX-loaded TECs as adjunct pulmonary therapy for COVID-19.</div></div>","PeriodicalId":15600,"journal":{"name":"Journal of Drug Delivery Science and Technology","volume":"106 ","pages":"Article 106683"},"PeriodicalIF":4.5,"publicationDate":"2025-02-05","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143421487","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":"Pharmacokinetics and safety of glycopyrrolate: An open-label, single-dose study in Chinese adult patients after general anesthesia surgery","authors":"Ping Du ,&nbsp;Jiandong Gao ,&nbsp;Weiyue Yu ,&nbsp;Rui Zhao ,&nbsp;Hongchuan Liu ,&nbsp;Yun Yue ,&nbsp;Yingmin Ma ,&nbsp;Lihong Liu ,&nbsp;Pengfei Li","doi":"10.1016/j.jddst.2025.106692","DOIUrl":"10.1016/j.jddst.2025.106692","url":null,"abstract":"<div><h3>Background</h3><div>Glycopyrrolate injection is an anticholinergic drug. The pharmacoeconomic advantages of glycopyrrolate, approved for marketing under the current Chinese health insurance payment model, are significant. The aim of this research was to characterize its pharmacokinetic properties and safety in Chinese adult patients after general anesthesia surgery.</div></div><div><h3>Methods</h3><div>An open-label, single-dose pharmacokinetics, safety and population pharmacokinetics of glycopyrrolate was performed in Chinese adult patients after general anesthesia surgery. Chinese adult patients after general anesthesia surgery were single intravenously administered by glycopyrrolate. Venous blood samples were drawn before and after administration and further quantified by a validated HPLC-MS/MS method. Safety was monitored during the whole stages. Population pharmacokinetics were performed by non-linear mixed-effects modelling.</div></div><div><h3>Results</h3><div>A total of 18 subjects were enrolled and evaluated. The principle pharmacokinetic parameters of C_max, t_1/2, AUC_0-t, AUC_0-∞, Vz and CL of glycopyrrolate were 45.8 ± 28.9 ng/mL, 1.7 ± 0.4 h, 10.3 ± 2.3 h∗ng/mL, 10.6 ± 2.4 h∗ng/mL, 1.9 ± 0.6 L/kg and 0.8 ± 0.2 L/h/kg, respectively. Safety was acceptable and no serious adverse events were detected. A three-compartment model and fitted concentration-time curve for glycopyrrolate were represented and validated, which was constant with published literatures.</div></div><div><h3>Conclusions</h3><div>Pharmacokinetics and safety of glycopyrrolate were investigated systemically with the help of this open-label, single-dose study in Chinese adult patients after general anesthesia surgery. Results of present study provide systemic data basis for improving the accessibility of the drug to Chinese patients and individualized and precise medication.</div></div><div><h3>Clinical trial registration</h3><div>No. CTR20170001 (Chinese Clinical Trial Registry, <span><span>https://db.yaozh.com/linchuangshiyan/bJaRbmNnaGljlWRilJaYmA.html</span><svg><path></path></svg></span>, Time of initial registration: 18 Feb 2017)</div></div>","PeriodicalId":15600,"journal":{"name":"Journal of Drug Delivery Science and Technology","volume":"105 ","pages":"Article 106692"},"PeriodicalIF":4.5,"publicationDate":"2025-02-05","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143377861","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":"Potential use of oral jelly formulations as supersaturable formulations: Acidified or alkalized jelly containing drugs with pH-dependent solubility","authors":"Junko Nakamura ,&nbsp;Yukari Kakino ,&nbsp;Takato Masada ,&nbsp;Makoto Kataoka ,&nbsp;Makoto Shuto ,&nbsp;Shinji Yamashita ,&nbsp;Yoshihiro Hishikawa ,&nbsp;Keiko Minami","doi":"10.1016/j.jddst.2025.106691","DOIUrl":"10.1016/j.jddst.2025.106691","url":null,"abstract":"<div><div>This study evaluates the potential of oral jelly formulations as supersaturable drug delivery systems for drugs with pH-dependent solubility, particularly in overcoming changes in gastric pH due to aging or medications. We prepared an oral jelly formulation of dipyridamole, a basic drug, by acidifying the jelly to pH 3. The stability of the acidified jelly was assessed over 28 days, with no precipitation. For comparison, a drug suspension and a neutral jelly were also tested. <em>In vitro</em> dissolution tests were conducted using 200 mL of Japanese Pharmacopoeia (JP) test fluids 2 (pH 6.8). Additionally, <em>in vivo</em> intestinal administration studies, bypassing gastric dissolution, were performed in rats to assess dipyridamole absorption. The acidified jelly showed a rapid, supersaturated dissolution profile <em>in vitro</em>. <em>In vivo</em>, the area under the curve (AUC) of dipyridamole from the acidified jelly was about 13 times higher than that of the suspension or neutral jelly. An alkalized jelly of telmisartan, an amphoteric drug, was also prepared at pH 10, showing a supersaturable dissolution profile <em>in vitro</em> and enhanced absorption <em>in vivo</em>. Acidified and alkalized jellies effectively serve as supersaturable formulations for basic and amphoteric drugs, with potential to improve oral absorption even under elevated gastric pH.</div></div>","PeriodicalId":15600,"journal":{"name":"Journal of Drug Delivery Science and Technology","volume":"106 ","pages":"Article 106691"},"PeriodicalIF":4.5,"publicationDate":"2025-02-05","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143378108","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}