Journal of Drug Delivery Science and Technology最新文献

{"title":"Formulation of folic acid-decorated β-cyclodextrin-based magnetic nanoparticles hybrid nanotherapeutic for targeted delivery of chlorogenic acid","authors":"Shagufta Juber Pathan ,&nbsp;Somnath Devidas Bhinge ,&nbsp;Shrinivas Krishna Mohite ,&nbsp;Sopan Namdev Nangare ,&nbsp;Mangesh Anil Bhutkar ,&nbsp;Namdeo Ramhari Jadhav ,&nbsp;Shubhangi Patil ,&nbsp;Smita Kumbhar ,&nbsp;Shailendra Shivaji Gurav","doi":"10.1016/j.jddst.2025.107536","DOIUrl":"10.1016/j.jddst.2025.107536","url":null,"abstract":"<div><div>Neuroblastoma, the most common extracranial pediatric tumor, has attracted considerable attention owing to the promising anticancer potential of chlorogenic acid (ChA). However, the utility of ChA is restricted by off-target effects. To overcome this limitation, we developed chlorogenic acid-loaded folic acid-conjugated β-cyclodextrin magnetic nanoparticles (Fe₃O₄-<em>β</em>-CD-FA@ChA) as a novel targeted delivery system. This study aimed to design, synthesize, and evaluate Fe₃O₄-<em>β</em>-CD-FA nanoparticles for the customized release, tumor-specific targeting, anticancer activity, and potential diagnostic application of ChA against neuroblastoma. In brief, the Fe₃O₄ core was synthesized by co-precipitation using Fe²⁺/Fe³⁺ salts and functionalized with <em>β</em>-cyclodextrin (<em>β</em>-CD) and FA through carbodiimide coupling. Here, ChA was loaded via an incubation diffusion method, enabling efficient encapsulation through non-covalent interactions. The resulting nanohybrids exhibited a mean size of 688.1 nm, carried a negative surface charge (−16 mV), and displayed irregular morphology. Customized drug release was achieved, with 34.38 % and 58.34 % ChA released over 48 h at pH 6.8 and 5.5, respectively. <em>In vitro</em> studies on SH-SY5Y neuroblastoma cells demonstrated significantly enhanced cytotoxicity (71.20 ± 0.92 %) compared to free ChA (40.95 ± 0.60 %), attributable to FA-mediated receptor targeting. Magnetic resonance imaging (MRI) confirmed superior intracellular accumulation and enhanced contrast in targeted cells. In conclusion, these findings highlight the potential of <em>β</em>-CD to design the Fe₃O₄-<em>β</em>-CD-FA@ChA nanohybrids in achieving targeted delivery, improved therapeutic efficacy, pH-responsive drug release, and theranostic capability. This <em>β</em>-CD-mediated nanoplatform offers a promising strategy for neuroblastoma treatment and warrants further investigation with other bioactive compounds.</div></div>","PeriodicalId":15600,"journal":{"name":"Journal of Drug Delivery Science and Technology","volume":"114 ","pages":"Article 107536"},"PeriodicalIF":4.9,"publicationDate":"2025-09-17","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145109530","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 in thermo-responsive hydrogels for ocular drug delivery: Materials, mechanisms, and clinical potential","authors":"Irfan Pathan ,&nbsp;Mohammed Adnan Raza ,&nbsp;Ayushmaan Roy ,&nbsp;Hemant Badwaik ,&nbsp;Kalyani Sakure ,&nbsp;Ajaz uddin","doi":"10.1016/j.jddst.2025.107537","DOIUrl":"10.1016/j.jddst.2025.107537","url":null,"abstract":"<div><div>Recent advancements in thermo-responsive hydrogels have revolutionized ocular drug delivery by offering a smart, non-invasive, and patient-compliant platform for sustained and targeted therapy. This review comprehensively discusses the development and application of thermo-responsive hydrogels in the treatment of prevalent ocular diseases such as dry eye syndrome, glaucoma, and uveitis. These hydrogels undergo sol-to-gel transitions at physiological temperatures, enabling in situ gelation upon ocular administration. The underlying mechanism enhances drug residence time and enables controlled drug release at the site of action. Formulations leverage both natural polymers such as chitosan, gelatin, and hyaluronic acid and synthetic polymers like poloxamers, PNIPAM, and PEG-based systems, each contributing to biocompatibility, biodegradability, and responsiveness to temperature stimuli. Key properties such as temperature-sensitive phase transition, controlled drug release, and high biocompatibility position these hydrogels as superior alternatives to conventional eye drops. The benefits include reduced dosing frequency, minimized systemic absorption, and enhanced drug bioavailability. Recent innovations focus on sustainable hydrogel synthesis, incorporation of novel polymer composites, and improved drug encapsulation techniques. Despite significant progress, challenges remain, including potential cytotoxicity of synthetic components, scalability of production, and achieving precise drug release kinetics. Future directions aim to optimize formulation stability, explore stimuli-combination responsive systems, and integrate nanotechnology for precision medicine. This review underscores the transformative potential of thermo-responsive hydrogels in ocular therapeutics and highlights their promise as a cornerstone in the next generation of smart ophthalmic drug delivery systems.</div></div>","PeriodicalId":15600,"journal":{"name":"Journal of Drug Delivery Science and Technology","volume":"114 ","pages":"Article 107537"},"PeriodicalIF":4.9,"publicationDate":"2025-09-17","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145096016","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":"Revolutionizing cancer treatment with oncolytic viruses: From tumor targeting and metabolic reprogramming to immune activation and precision delivery","authors":"Alia Uzma ,&nbsp;Adiba Adiba ,&nbsp;Muhammad Armaghan Khalid ,&nbsp;Muhammad Tariq Navid ,&nbsp;Munazza Fatima ,&nbsp;Uzma Azeem Awan ,&nbsp;Deeba Amraiz","doi":"10.1016/j.jddst.2025.107543","DOIUrl":"10.1016/j.jddst.2025.107543","url":null,"abstract":"<div><div>Oncolytic viruses (OVs) have emerged as promising immunotherapeutic agents capable of selectively killing tumor cells while saving healthy tissues. Advances in genetic engineering have enhanced OV efficacy by embracing immune-stimulating molecules, like GM-CSF and combining them with other treatments such as checkpoint inhibitors. Beyond direct oncolysis, OVs induce immunogenic cell death and release tumor-associated antigens that activate dendritic cells and cytotoxic T lymphocytes, thus boosting antitumor immunity. Despite their potential, challenges such as limited intra-tumoral penetration, immune evasion and rapid clearance remain significant barriers. New delivery strategies including nanoparticle encapsulation, mesenchymal stem cell carriers and vesicle-based systems are under observation to improve stability and targeting. Personalized approaches that align OV therapy with unique tumor profiles may further enhance therapeutic success. Overcoming these hurdles could strongly establish oncolytic virotherapy as an evolutionary approach in cancer immunotherapy and underscoring the need for continued research and well-designed clinical trials to fully recognize its potential.</div></div>","PeriodicalId":15600,"journal":{"name":"Journal of Drug Delivery Science and Technology","volume":"114 ","pages":"Article 107543"},"PeriodicalIF":4.9,"publicationDate":"2025-09-17","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145096013","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":"Grape pomace and quercetin: a synergistic approach using PG-PEVs for Psoriasis treatment","authors":"Matteo Perra ,&nbsp;Rita Abi Rached ,&nbsp;Laura Fancello ,&nbsp;Amparo Nacher ,&nbsp;Octavio Diez-Sales ,&nbsp;Amparo Ruiz-Sauri ,&nbsp;Carmen Duque-Soto ,&nbsp;Jesus Lozano-Sanchez ,&nbsp;Carmen Escobedo-Lucea ,&nbsp;Pietro Matricardi ,&nbsp;Alessandra Del Giudice ,&nbsp;Ines Castangia ,&nbsp;Maria Manconi ,&nbsp;Maria Letizia Manca","doi":"10.1016/j.jddst.2025.107544","DOIUrl":"10.1016/j.jddst.2025.107544","url":null,"abstract":"<div><div>Psoriasis is a chronic inflammatory skin disorder that affects millions worldwide and poses significant therapeutic challenges due to the adverse effects of conventional treatments. In this</div><div>study we explored a sustainable approach based on Cannonau grape pomace extract, a winemaking side-stream rich in antioxidant polyphenols, combined with quercetin, to develop effective treatments for psoriasis. The extract was obtained using an eco-friendly extraction process and incorporated into phospholipid vesicles containing propylene glycol (PG-PEVs), which exhibited favourable physicochemical features: small size (∼77–172nm), homogeneously dispersed (PDI ∼0.29), highly negative zeta potential (∼−45 mV), high entrapment efficiency (≥82 %), and long-term stability over 18 months. Biological evaluations revealed the high biocompatibility of the formulations (≥80 %), and their ability to protect keratinocytes from oxidative stress and hyperproliferation, hallmarks of psoriasis.</div><div>In a psoriasis-like murine model, PG-PEVs significantly reduced inflammation, neutrophil infiltration, and epidermal hyperplasia, as confirmed by decreased MPO levels (from ∼353 to ∼179 ng/mL) and improved skin architecture observed through histological analysis, which outperformed the effects of the natural chemicals in dispersion. These findings highlight the therapeutic potential of Cannonau pomace extract-loaded PG-PEVs as a promising, sustainable dermatological strategy. Moreover, this study supports the valorisation of agricultural side-streams into high-value cosmeceuticals, aligning with circular economy principles.</div></div>","PeriodicalId":15600,"journal":{"name":"Journal of Drug Delivery Science and Technology","volume":"114 ","pages":"Article 107544"},"PeriodicalIF":4.9,"publicationDate":"2025-09-17","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145095510","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":"Thermosensitive in situ gel containing alpha-lipoic acid and rutin for the treatment of corneal neovascularization: formulation, characterization, and in vivo evaluation","authors":"Heybet Kerem Polat ,&nbsp;Nasıf Fatih Karakuyu ,&nbsp;Sedat Ünal ,&nbsp;Yasin Turanlı ,&nbsp;Esra Pezik ,&nbsp;Gülşah Usta Sofu ,&nbsp;Emine Sarman","doi":"10.1016/j.jddst.2025.107538","DOIUrl":"10.1016/j.jddst.2025.107538","url":null,"abstract":"<div><div>Corneal neovascularization (CnV) is a significant ophthalmological condition often leading to discomfort and vision impairment. Due to the limitations and side effects associated with conventional drug therapies for CnV, innovative treatment strategies are being explored. In this study, the potential of alpha-lipoic acid and rutin-loaded thermosensitive in situ gels for the treatment of CnV was evaluated. The ocular in situ gel was formulated using the cold method and included chitosan, poloxamer 407, and poloxamer 188 as polymers. A design of experiments (DoE) approach was employed to investigate the effects of formulation variables on critical quality attributes, including pH, gelation temperature, and viscosity. The optimized drug-loaded gel exhibited a pH of 5.05 ± 0.1, pseudo-plastic flow behavior with a viscosity of 341 ± 26 cP at 25 °C, and gelation at 34 ± 0.4 °C. Drug release followed Weibull and first-order kinetics. Ocular safety was confirmed through in vitro cytotoxicity studies using L929 and ARPE-19 cell lines. In vivo studies in rats and histochemical analyses of the cornea demonstrated that the optimized formulation (Formulation K) was as effective as dexamethasone, a standard treatment for CnV, and further promoted epithelial cell regeneration. Histological evaluations of ocular tissues revealed reduced inflammation and neovascularization in the Formulation K group, supporting its therapeutic potential. Overall, our findings suggest that the developed in situ gel system offers sustained drug release and enhanced therapeutic efficacy for the treatment of corneal neovascularization.</div></div>","PeriodicalId":15600,"journal":{"name":"Journal of Drug Delivery Science and Technology","volume":"114 ","pages":"Article 107538"},"PeriodicalIF":4.9,"publicationDate":"2025-09-16","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145096019","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 evaluation of pomegranate seed oil nanoemulsions for delivery of fingolimod hydrochloride in multiple sclerosis treatment","authors":"Zahra Yeganeh ,&nbsp;Farnoush Oveissi ,&nbsp;Ladan Dayani ,&nbsp;Mehdi Aliomrani ,&nbsp;Azade Taheri","doi":"10.1016/j.jddst.2025.107541","DOIUrl":"10.1016/j.jddst.2025.107541","url":null,"abstract":"<div><div>Fingolimod hydrochloride is one of the available treatments for managing multiple sclerosis (MS), a leading cause of neurological disability among young adults. However, it may exhibit several side effects. This study aimed to develop a pomegranate seed oil nanoemulsion as a delivery system for fingolimod to enhance its therapeutic efficacy. A Box-Behnken experimental design was applied for optimization, with the oil proportion, poloxamer 188 concentration, and lecithin concentration selected as independent variables. Female C57BL/6 mice with experimental autoimmune encephalomyelitis (EAE) were treated intraperitoneally with fingolimod-loaded pomegranate seed oil nanoemulsion (FIN-PSO NE) containing 1 mg/kg of fingolimod daily for up to 28 days and subsequently evaluated. The optimized formulation, containing 30 % oil, 5 % poloxamer, and 2 % lecithin, showed a particle size of 231.26 ± 38.80 nm, a polydispersity index of 0.19 ± 0.06, and an entrapment efficiency of 99.57 ± 0.21 %. It also displayed a sustained drug release profile. SEM images revealed a smooth morphology and uniform size distribution. FTIR spectra indicated no interactions between the drug and other ingredients in the nanoemulsion. Additionally, this formulation alleviated neurological scores and reduced demyelination in EAE-induced mice. Consequently, it could be a promising candidate for MS treatment.</div></div>","PeriodicalId":15600,"journal":{"name":"Journal of Drug Delivery Science and Technology","volume":"114 ","pages":"Article 107541"},"PeriodicalIF":4.9,"publicationDate":"2025-09-16","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145096048","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":"Fabrication and application of iron oxide-encapsulated PLGA nanoparticles with dual responsiveness to magnetic fields and light for nose-to-brain drug delivery","authors":"Kazuki Sato,&nbsp;Koki Ogawa,&nbsp;Sawaki Nabeshima,&nbsp;Susumu Suwabe,&nbsp;Tetsuya Ozeki","doi":"10.1016/j.jddst.2025.107535","DOIUrl":"10.1016/j.jddst.2025.107535","url":null,"abstract":"<div><div>Nose-to-brain delivery has been widely investigated as a potential strategy for glioma therapy. However, the nasal epithelial barrier remains a major obstacle to drug transport from the nasal cavity to the brain, particularly for macromolecular agents such as peptides, nucleic acids, and nanoparticles. Therefore, strategies to enhance epithelial permeability are required. In this study, we developed a drug delivery system to improve nose-to-brain transport through transcranial magnetic field application, with the aim of contributing to glioma treatment. Iron oxide nanoparticles (IONPs), which possess both superparamagnetic and photothermal properties, were utilized to enhance brain penetration and to enable photothermal therapy (PTT). IONPs were encapsulated in poly(lactic-co-glycolic acid) (PLGA) nanoparticles to form IONPs@PLGA, with an average size of approximately 200 nm. Transmission electron microscopy revealed that IONPs were located inside PLGA nanoparticles, and laser irradiation (660 nm) raised the temperature to 50 °C, suggesting that IONPs@PLGA generated sufficient heat to induce cancer cell death. Moreover, IONPs@PLGA were efficiently internalized by cells under a magnetic field, and laser irradiation induced strong cytotoxicity against C6 glioma cells. Notably, applying a magnetic field after intranasal administration increased brain accumulation by ∼2.5-fold, confirming enhanced delivery <em>via</em> magnetic targeting. In summary, we developed IONPs@PLGA, a dual magnetic- and light-responsive system, and demonstrated its potential to improve nose-to-brain delivery. Given their drug-loading capacity, IONPs@PLGA represent a promising platform for magnetically guided, non-invasive brain drug delivery.</div></div>","PeriodicalId":15600,"journal":{"name":"Journal of Drug Delivery Science and Technology","volume":"114 ","pages":"Article 107535"},"PeriodicalIF":4.9,"publicationDate":"2025-09-15","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145109539","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":"Phthalate angico gum nanoparticles-based microneedles: a long-acting transdermal delivery system for antiretroviral therapy","authors":"Thaisa Cardoso de Oliveira ,&nbsp;Antônia Carla de Jesus Oliveira ,&nbsp;Salete Reis ,&nbsp;Sofia Costa Lima ,&nbsp;Luíse Lopes Chaves ,&nbsp;Monica Felts de La Roca Soares ,&nbsp;José Lamartine Soares-Sobrinho","doi":"10.1016/j.jddst.2025.107527","DOIUrl":"10.1016/j.jddst.2025.107527","url":null,"abstract":"<div><div>Microneedles (MN) have gained attention as an alternative transdermal drug delivery system (TDDS) due to their ease of administration and painlessness, and the possibility of incorporating free drugs or nanoparticles to modulate drug release. This study aimed to develop TDDS for the antiretroviral drug nevirapine (NVP), using MN-containing phthalate angico gum (PAG) nanoparticles (NP). NVP-loaded NP were prepared as nanosuspensions (NPns) or lyophilized nanoparticles (NPfd) and incorporated into chitosan (CS) and polyvinylpyrrolidone (PVP) hydrogels to produce MN (M-NPns and M-NPfd). The MN were fabricated using a micro-molding method with a siloxane mold. The selected M-NPns and M-NPfd were characterized by scanning electron microscopy (SEM), permeation assays using Franz diffusion cells with porcine ear skin, and histological studies using MN containing 0.1 % rhodamine. Both M-NPns and M-NPfd showed significant drug permeation after 72 h, and histological assays demonstrated that MN promoted skin micropiercing. The incorporation of NP into CS: PVP-MN resulted in suitable mechanical properties and slow, progressive release of NVP. This study highlights the potential of MN containing PAG NP as an innovative long-acting TDDS for NVP delivery, by combining the technology of MN and NP, which may improve patient adherence and reduce the frequency of administration.</div></div>","PeriodicalId":15600,"journal":{"name":"Journal of Drug Delivery Science and Technology","volume":"114 ","pages":"Article 107527"},"PeriodicalIF":4.9,"publicationDate":"2025-09-13","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145095514","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 probiotic microemulsion with antioxidant activity to promote wound healing","authors":"Yi-Xiao Shao ,&nbsp;Peng Wei ,&nbsp;Jia-wei Tu ,&nbsp;Bao-Jun Li ,&nbsp;Yong Li ,&nbsp;Ning-Li Xu ,&nbsp;Gui-Lan Xia ,&nbsp;Chen-Jian Liu ,&nbsp;Xiao-Ran Li ,&nbsp;Lei Zhang","doi":"10.1016/j.jddst.2025.107534","DOIUrl":"10.1016/j.jddst.2025.107534","url":null,"abstract":"<div><div>Wound healing is a complex and dynamic biological process, and the treatment of chronic wounds remains a major clinical challenge. In this study, a novel probiotic microemulsion (LTE) based on <em>Lactiplantibacillus plantarum</em>-fermented tea was developed for wound healing treatment. Using the tea leaves of the De'ang ethnic group in Yunnan Province as raw materials, they were fermented by <em>Lb. plantarum</em> 75-2m-2. The results of targeted metabolism and qRT-PCR showed that the antioxidant polyphenols increased significantly during the fermentation process, and the key degradation enzymes were upregulated. By optimizing the microemulsion formulation, a stable and biocompatible LTE was obtained. In a rat full-thickness skin injury model, LTE accelerated wound closure, promoted re-epithelialization and collagen deposition, regulated the skin microbiota, and reduced the levels of pro-inflammatory cytokines. This study integrated traditional fermentation technology with modern nanotechnology, providing a novel and effective method for wound healing treatment, and indicating that LTE is a promising candidate for clinical wound dressings.</div></div>","PeriodicalId":15600,"journal":{"name":"Journal of Drug Delivery Science and Technology","volume":"114 ","pages":"Article 107534"},"PeriodicalIF":4.9,"publicationDate":"2025-09-13","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145060164","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":"Optimization and evaluation of self-microemulsifying drug delivery systems for enzalutamide and N-desmethyl enzalutamide to enhance antitumor efficacy against prostate cancer","authors":"Guolian Ren ,&nbsp;Xiaohui Zhou ,&nbsp;Long Cao ,&nbsp;Xiaoning Li ,&nbsp;Fugui Guo ,&nbsp;Jingjing Han ,&nbsp;Xiaomin Niu ,&nbsp;Xiaozhou Dong ,&nbsp;Guoshun Zhang ,&nbsp;Ruili Wang ,&nbsp;Xihua Yang ,&nbsp;Shuqiu Zhang ,&nbsp;Shiping Yu ,&nbsp;Jixing Zhang","doi":"10.1016/j.jddst.2025.107532","DOIUrl":"10.1016/j.jddst.2025.107532","url":null,"abstract":"<div><div>Enzalutamide (ENZ) is clinically used primarily for the treatment of advanced prostate cancer. N-desmethyl-enzalutamide (NDE) is a primary and biologically active metabolite of ENZ. However, the poor water solubility and oral absorption of ENZ and NDE limit their clinical applications. To develop ENZ and its active metabolites into new formulations, a self-microemulsifying drug delivery system (SMEDDS) for ENZ and NDE was designed to enhance the solubility and antitumor efficacy of these two drugs during delivery. The results indicated that both ENZ- and NDE-SMEDDS exhibited favorable physicochemical properties and <em>in vitro</em> drug release characteristics. <em>In vivo</em> studies revealed that ENZ- and NDE-SMEDDS had higher AUC and half-lives in comparison with that of ENZ-suspensions (ENZ-sus) and NDE-suspensions (NDE-sus). The SMEDDS demonstrates superior antitumor activity compared to ENZ- and NDE-sus, with NDE-SMEDDS showing slightly better antitumor efficacy than ENZ-SMEDDS. The SMEDDS is a potentially novel oral drug delivery system that can enhance the solubility and antitumor effects of ENZ and NDE. Furthermore, as an active metabolite of ENZ, NDE can be developed into new formulations for antitumor application, offering new strategy for the clinical use of NDE.</div></div>","PeriodicalId":15600,"journal":{"name":"Journal of Drug Delivery Science and Technology","volume":"114 ","pages":"Article 107532"},"PeriodicalIF":4.9,"publicationDate":"2025-09-13","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145060165","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}