International Journal of Pharmaceutics最新文献_第2页

Current approaches to overcome the limit of TRAIL-based treatment in colorectal cancer: From fusion protein to nano-delivery platform. 目前的方法克服了基于trail的结直肠癌治疗的局限性：从融合蛋白到纳米递送平台。

IF 5.2 2区医学

International Journal of Pharmaceutics Pub Date : 2025-10-15 Epub Date: 2025-08-05 DOI: 10.1016/j.ijpharm.2025.126031

Xiaorong Chen, Xi Yang, Xianyan Chen, Cheng Yi, Zhaojun Li

{"title":"Current approaches to overcome the limit of TRAIL-based treatment in colorectal cancer: From fusion protein to nano-delivery platform.","authors":"Xiaorong Chen, Xi Yang, Xianyan Chen, Cheng Yi, Zhaojun Li","doi":"10.1016/j.ijpharm.2025.126031","DOIUrl":"10.1016/j.ijpharm.2025.126031","url":null,"abstract":"Colorectal cancer (CRC), one of common malignancies, ranks second in cancer-related mortality worldwide. Despite advances in targeted therapy and immune therapy, patients with metastatic CRC have poor 5-year survival, which is approximately 14%. Multiple investigations are underway with the aim to improve outcome of this cohort. The tumor necrosis factor (TNF)-related apoptosis-inducing ligand (TRAIL) has been considered as an ideal candidate in the field of cancer treatment because it is able to selectively induce apoptosis of cancer or transformed cells while sparing normal cells or tissues. TRAIL or TRAIL-based therapies have shown significant tumoricidal effects in multiple cancer xenograft models, and phase I clinical trials have demonstrated its safety. However, most phase II or III trials fail to show robust efficacy, which may be related to their poor pharmacokinetic characteristics, such as short half-life and inadequate accumulation in tumor sites, and TRAIL resistance. Recently, several studies have developed novel methods to improve efficacy of TRAIL, by fusing molecules with diverse functions to TRAIL, by utilizing nanoparticles or cellular vehicles to deliver TRAIL, and by combining TRAIL with other agents. In this review, we emphasize the existing approaches to overcome the aforementioned issues with the aim to enhance efficacy of TRAIL for the treatment of CRC.","PeriodicalId":14187,"journal":{"name":"International Journal of Pharmaceutics","volume":" ","pages":"126031"},"PeriodicalIF":5.2,"publicationDate":"2025-10-15","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144784271","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":2,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0

Technical and regulatory perspective on acid stage dissolution assessed via optical coherence tomography (Part 1: Release Scenario). 通过光学相干断层扫描评估酸阶段溶解的技术和监管观点（第1部分：释放情景）。

IF 5.2 2区医学

International Journal of Pharmaceutics Pub Date : 2025-10-15 Epub Date: 2025-08-05 DOI: 10.1016/j.ijpharm.2025.126044

Jesús Alberto Afonso Urich, Matthias Wolfgang, Raymar Andreina Lara Garcia, Heli West, Johannes Khinast

{"title":"Technical and regulatory perspective on acid stage dissolution assessed via optical coherence tomography (Part 1: Release Scenario).","authors":"Jesús Alberto Afonso Urich, Matthias Wolfgang, Raymar Andreina Lara Garcia, Heli West, Johannes Khinast","doi":"10.1016/j.ijpharm.2025.126044","DOIUrl":"10.1016/j.ijpharm.2025.126044","url":null,"abstract":"Enteric coating ensures a targeted release of active pharmaceutical ingredients (APIs) by protecting them from premature dissolution in the stomach. The effectiveness of such coating depends on its thickness and integrity, which are critical for achieving the desired acid protection. This study explores the use of Optical Coherence Tomography (OCT) as an innovative and non-destructive alternative to traditional acid stage dissolution testing performed by directly measuring the coating thickness. Three enteric coating materials (Acryl-Eze®, Aquarius™ Control ENA, and Nutrateric®) were tested in two manufacturing batches to evaluate operator variability. OCT was used to measure the coating thickness, which was correlated with the acid stage dissolution testing and established critical thicknesses of 68 µm for Acryl-Eze®, 69 µm for Aquarius™ Control ENA, and 65 µm for Nutrateric®. These specifications ensure compliance with the pharmacopeial performance criteria for acid protection and can be implemented into regulatory frameworks as part of product release protocols in the dossier. By demonstrating the agreement between the results of OCT-based thickness measurements and the pharmacopeial dissolution testing, this work underscores the potential of OCT to be recognized in regulatory contexts as a tool for enhanced production efficiency and quality assurance in manufacturing enteric-coated oral dosage forms.","PeriodicalId":14187,"journal":{"name":"International Journal of Pharmaceutics","volume":" ","pages":"126044"},"PeriodicalIF":5.2,"publicationDate":"2025-10-15","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144784284","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":2,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0

Novel multi-nozzle spray coating technology for the continuous production and isolation of drug nanoparticles. 用于药物纳米颗粒连续生产和分离的新型多喷嘴喷涂技术。

IF 5.2 2区医学

International Journal of Pharmaceutics Pub Date : 2025-10-15 Epub Date: 2025-08-05 DOI: 10.1016/j.ijpharm.2025.126016

Aaron O'Sullivan, Vivek Verma, Mohamad Baassiri, Clarinda Costa, Mohsen H Moghimi, Kevin M Ryan, Orest Shardt, Luis Padrela

{"title":"Novel multi-nozzle spray coating technology for the continuous production and isolation of drug nanoparticles.","authors":"Aaron O'Sullivan, Vivek Verma, Mohamad Baassiri, Clarinda Costa, Mohsen H Moghimi, Kevin M Ryan, Orest Shardt, Luis Padrela","doi":"10.1016/j.ijpharm.2025.126016","DOIUrl":"10.1016/j.ijpharm.2025.126016","url":null,"abstract":"Different strategies have been employed to improve the bioavailability of poorly soluble drug candidates, including nanomaterials like polymeric and raw-drug nanoparticles. A multitude of top-down and bottom-up approaches have been reported in the literature to date to produce such products, but the adoption of bottom-up methods in industry is still limited due to technical challenges like low yields, particle aggregation, and inadequate rheological properties. This work presents a novel technology termed multi-nozzle supercritical enhanced nano-coating (MUSENC) for the simultaneous production and isolation of drug nanoparticles. Using multiple spraying nozzles, nanoparticles of celecoxib (263 ± 59 nm) were coated onto micron-sized carrier particles, enhancing yield (61 ± 4 %) and isolation efficiency (drug loading of 6.1 ± 0.4 %). Computational fluid dynamics simulations provided insights into the interactions of the spraying jets, aiding in process optimization. All formulations exhibited good flowability and mechanical strength, demonstrating the effectiveness of this continuous single-step manufacturing process.","PeriodicalId":14187,"journal":{"name":"International Journal of Pharmaceutics","volume":" ","pages":"126016"},"PeriodicalIF":5.2,"publicationDate":"2025-10-15","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144784283","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":2,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0

Impact of skin model and dissolvable microneedle design on efficiency of cutaneous protein delivery. 皮肤模型及可溶微针设计对皮肤蛋白质递送效率的影响。

IF 5.2 2区医学

International Journal of Pharmaceutics Pub Date : 2025-10-15 Epub Date: 2025-07-30 DOI: 10.1016/j.ijpharm.2025.126022

Lyndsey E Moore, Isabella A van Hulst, Koen van der Maaden, Sonja Vucen, Anne C Moore

{"title":"Impact of skin model and dissolvable microneedle design on efficiency of cutaneous protein delivery.","authors":"Lyndsey E Moore, Isabella A van Hulst, Koen van der Maaden, Sonja Vucen, Anne C Moore","doi":"10.1016/j.ijpharm.2025.126022","DOIUrl":"10.1016/j.ijpharm.2025.126022","url":null,"abstract":"Dissolvable microneedle (DMN) patches, or microarray patches (MAP), are drug and vaccine delivery technologies that demonstrate clinical potential due to their ability to enhance thermostability and to permit injection-free, easy administration into the skin. A key attribute for MAP-mediated delivery is maximum delivery efficiency of the vaccine subsequent to administration. Despite an acceptance that not all of the vaccine is delivered, few studies have quantified the delivery efficiency and how the microneedle design impacts on this function. Importantly, there has been no comparative investigation to determine how the source of skin impacts on ex vivo dose delivery. Here, we investigated the amount of protein antigen delivered and microneedle insertion efficiencies to three commonly used skin types: mouse, pig, and human. Pig and human skin performed similarly in skin delivery and insertion efficiency studies. Insertion efficiency in mouse skin was significantly more variable. We also describe how a two-layer DMN patch delivers increased protein delivery to pig skin (88 % ± 8 %) compared to single layer designs (48 % ± 20 %). Overall, our findings indicate that pig skin is a suitable surrogate skin model for human skin, while mouse skin is less representative. These findings will help the development and harmonisation of assays that assess the quality of protein-containing DMN patches.","PeriodicalId":14187,"journal":{"name":"International Journal of Pharmaceutics","volume":" ","pages":"126022"},"PeriodicalIF":5.2,"publicationDate":"2025-10-15","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144764823","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":2,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0

Artificial intelligence: a new era in prostate cancer diagnosis and treatment. 人工智能：前列腺癌诊断和治疗的新时代

IF 5.2 2区医学

International Journal of Pharmaceutics Pub Date : 2025-10-15 Epub Date: 2025-08-05 DOI: 10.1016/j.ijpharm.2025.126024

Nithin Vidiyala, Prashanth Parupathi, Pavani Sunkishala, Chetan Sree Muppavarapu, Aditya Gujja, Praneeth Kanagala, Sai Krishna Meduri, Dinesh Nyavanandi

{"title":"Artificial intelligence: a new era in prostate cancer diagnosis and treatment.","authors":"Nithin Vidiyala, Prashanth Parupathi, Pavani Sunkishala, Chetan Sree Muppavarapu, Aditya Gujja, Praneeth Kanagala, Sai Krishna Meduri, Dinesh Nyavanandi","doi":"10.1016/j.ijpharm.2025.126024","DOIUrl":"10.1016/j.ijpharm.2025.126024","url":null,"abstract":"Prostate cancer (PCa) represents one of the most prevalent cancers among men, with substantial challenges in timely and accurate diagnosis and subsequent treatment. Traditional diagnosis and treatment methods for PCa, such as prostate-specific antigen (PSA) biomarker detection, digital rectal examination, imaging (CT/MRI) analysis, and biopsy histopathological examination, suffer from limitations such as a lack of specificity, generation of false positives or negatives, and difficulty in handling large data, leading to overdiagnosis and overtreatment. The integration of artificial intelligence (AI) in PCa diagnosis and treatment is revolutionizing traditional approaches by offering advanced tools for early detection, personalized treatment planning, and patient management. AI technologies, especially machine learning and deep learning, improve diagnostic accuracy and treatment planning. The AI algorithms analyze imaging data, like MRI and ultrasound, to identify cancerous lesions effectively with great precision. In addition, AI algorithms enhance risk assessment and prognosis by combining clinical, genomic, and imaging data. This leads to more tailored treatment strategies, enabling informed decisions about active surveillance, surgery, or new therapies, thereby improving quality of life while reducing unnecessary diagnoses and treatments. This review examines current AI applications in PCa care, focusing on their transformative impact on diagnosis and treatment planning while recognizing potential challenges. It also outlines expected improvements in diagnosis through AI-integrated systems and decision support tools for healthcare teams. The findings highlight AI's potential to enhance clinical outcomes, operational efficiency, and patient-centred care in managing PCa.","PeriodicalId":14187,"journal":{"name":"International Journal of Pharmaceutics","volume":" ","pages":"126024"},"PeriodicalIF":5.2,"publicationDate":"2025-10-15","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144794394","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":2,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0

An inhalable composite particulate system for targeted delivery of therapeutics deep into small airways: in vitro and in vivo evaluation. 一种可吸入的复合颗粒系统，用于靶向递送治疗药物深入小气道：体外和体内评估。

IF 5.2 2区医学

International Journal of Pharmaceutics Pub Date : 2025-10-15 Epub Date: 2025-08-06 DOI: 10.1016/j.ijpharm.2025.126053

Nan Li, Xu Li, Songwen Tan, Di Hao, Zi Wang, Shu Fang, Peng Quan

{"title":"An inhalable composite particulate system for targeted delivery of therapeutics deep into small airways: in vitro and in vivo evaluation.","authors":"Nan Li, Xu Li, Songwen Tan, Di Hao, Zi Wang, Shu Fang, Peng Quan","doi":"10.1016/j.ijpharm.2025.126053","DOIUrl":"10.1016/j.ijpharm.2025.126053","url":null,"abstract":"Chronic obstructive pulmonary disease (COPD) is characterized by the airflow limitation due to chronic inflammation and excessive airway mucus secretion. Targeted delivery of therapeutics deep into small airways is the key step in treatment of COPD. In this study, we designed an inhalable composite particulate system with nano in micro structure for targeted delivery of therapeutics deep into small airways. Curcumin was incorporated into solid lipid nanoparticles modified with PEG2000 to improve the retention time and reduce the immune recognition and clearance in small airways. Then, flower-like lactose with rapid dissolution rate was used as an inhalable carrier to deliver the nanoparticles deep into the small airways. The inhalable composite particles showed a mass median aerodynamic diameter suitable for deep lung deposition (approximately 2.5 μm), high fine particle fraction (approximately 58 %) and rapid dissolution rate in simulated lung fluid. The in vivo pharmacokinetic study indicated that intratracheal administration of the inhalable composite particles significantly improved the concentration and retention time of curcumin in the lung and decreased the systemic exposure of the therapeutics. The inhalable composite particles also showed good safety in the in vitro cell viability study and the in vivo acute inhalation toxicity study. In the in vivo pharmacodynamic study, intratracheal administration of the inhalable composite particles delayed the progression of COPD by reducing the inflammation and inhibiting the excessive collagen production in the lung. The inhalable composite particulate system demonstrated a great potential for targeting delivery of therapeutics into small airways.","PeriodicalId":14187,"journal":{"name":"International Journal of Pharmaceutics","volume":" ","pages":"126053"},"PeriodicalIF":5.2,"publicationDate":"2025-10-15","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144803987","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":2,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0

Enhanced follicular penetration of antiseptics using nanocrystals - investigated via novel hair follicle content removal method. 利用纳米晶体增强杀菌剂在毛囊中的渗透作用——通过新型毛囊内容物去除方法进行研究。

IF 5.2 2区医学

International Journal of Pharmaceutics Pub Date : 2025-10-12 DOI: 10.1016/j.ijpharm.2025.126274

Lalita Roscetti, Cornelia M Keck, Muzn Alkhaldi, Anam S Khan, Em-On Chaiprateep, Tehseen Sehra, Soma Sengupta, Loris Busch, Burkhard Kleuser, Martina C Meinke, Anna Lena Klein

{"title":"Enhanced follicular penetration of antiseptics using nanocrystals - investigated via novel hair follicle content removal method.","authors":"Lalita Roscetti, Cornelia M Keck, Muzn Alkhaldi, Anam S Khan, Em-On Chaiprateep, Tehseen Sehra, Soma Sengupta, Loris Busch, Burkhard Kleuser, Martina C Meinke, Anna Lena Klein","doi":"10.1016/j.ijpharm.2025.126274","DOIUrl":"https://doi.org/10.1016/j.ijpharm.2025.126274","url":null,"abstract":"Effective skin disinfection is critical in preventing surgical-site infections (SSIs), particularly during long surgical procedures where bacteria from hair follicles can continuously emerge onto the skin surface and recolonize it. To enhance follicular disinfection, this study investigates the intrafollicular delivery of isopropanol, an antiseptic agent, dissolved in the outer phase of a suspension of specifically-engineered hesperetin nanocrystals. To accurately quantify follicular penetration, we analyzed both intrafollicular concentration and penetration depth. For the former, we developed the 'hair plucking method', a novel technique that extracts whole hair follicles, comprising the hairs and their associated follicular epidermis. Using porcine ear skin as an ex vivo model, we applied two formulations: an isopropanol-based hesperetin nanocrystals suspension, and an isopropanol-based particle-free control, while a third skin area remained untreated and served as a baseline. Rhodamine 6G, a fluorescent dye, was incorporated into both formulations to track penetration. Fluorescence spectroscopy analysis of fully plucked hair follicles was employed to measure the intrafollicular concentration of the dyed antiseptic, while laser scanning microscopy of cryohistological hair follicle sections was employed to measure its penetration depth. The results showed that the nanocrystals increased intrafollicular concentration of the antiseptic formulation by over 85 % (p < 0.05) and its penetration depth by approximately 38 % (p < 0.001), demonstrating enhanced follicular delivery and validating the efficacy of the hair plucking method. These findings highlight the potential of nanoparticle-based formulations to improve surgical antisepsis and reduce SSI risks, contributing to safer and more effective preoperative disinfection strategies.","PeriodicalId":14187,"journal":{"name":"International Journal of Pharmaceutics","volume":" ","pages":"126274"},"PeriodicalIF":5.2,"publicationDate":"2025-10-12","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145292156","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":2,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0

Enhanced corneal permeation of diclofenac through an ophthalmic nanocrystal suspension. 双氯芬酸通过眼用纳米晶体悬浮液增强角膜渗透。

IF 5.2 2区医学

International Journal of Pharmaceutics Pub Date : 2025-10-12 DOI: 10.1016/j.ijpharm.2025.126272

Elena Loi, Victoria Díaz-Tomé, Selene Cuello-Rodríguez, Maria Cristina Cardia, Víctor Álvarez-González, Joana Moreira, Francesco Lai, Francisco J Otero-Espinar

{"title":"Enhanced corneal permeation of diclofenac through an ophthalmic nanocrystal suspension.","authors":"Elena Loi, Victoria Díaz-Tomé, Selene Cuello-Rodríguez, Maria Cristina Cardia, Víctor Álvarez-González, Joana Moreira, Francesco Lai, Francisco J Otero-Espinar","doi":"10.1016/j.ijpharm.2025.126272","DOIUrl":"https://doi.org/10.1016/j.ijpharm.2025.126272","url":null,"abstract":"Diclofenac (DCF) is a non-steroidal anti-inflammatory drug (NSAID) with analgesic, anti-inflammatory and antipyretic effects, commonly used to treat painful and chronic inflammatory conditions linked to angiogenesis. It works by inhibiting cyclooxygenase (COX) enzymes and leukocyte migration, reducing prostaglandin synthesis and inflammation. Topically, DCF is used to manage ocular inflammation such as uveitis and keratitis, prevent cystoid macular edema post-surgery, and maintain mydriasis during operations. Clinical studies show it provides anti-inflammatory benefits comparable to dexamethasone but with a lower risk of increasing intraocular pressure. DCF may also help prevent posterior capsule opacification after cataract surgery. This study aimed to enhance DCF ocular delivery using nanocrystals. Stabilized with Poloxamer 188, the nanosuspensions produced monodisperse nanocrystals (∼450 nm) with a negative ζ-potential (-38 mV), significantly improving corneal permeation versus standard formulations. Ex vivo bovine cornea studies confirmed faster and more efficient drug penetration from the nanosuspension compared to a commercial solution. Safety was supported by BCOP, HET-CAM and cell viability assays, all showing no irritation. Corneal hydration remained stable, indicating low irritation potential. In summary, the developed nanosuspensions offer a promising strategy for improving DCF ocular delivery and therapeutic efficacy. Further clinical studies are needed to confirm long-term safety and effectiveness in humans.","PeriodicalId":14187,"journal":{"name":"International Journal of Pharmaceutics","volume":" ","pages":"126272"},"PeriodicalIF":5.2,"publicationDate":"2025-10-12","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145292115","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":2,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0

Optimizing cinnamophilin delivery via SNEDDS for enhanced anti-melanogenic activity: A comprehensive evaluation of skin safety, permeability, and tyrosinase inhibition. 通过SNEDDS优化肉桂素递送以增强抗黑素活性：皮肤安全性，渗透性和酪氨酸酶抑制的综合评估。

IF 5.2 2区医学

International Journal of Pharmaceutics Pub Date : 2025-10-11 DOI: 10.1016/j.ijpharm.2025.126260

Yu-Chen Chen, Yih-Fung Chen, Hsin-Ya Yu, Chia-Hsuan Lin, Wan-Yi Liu, Hsun-Shuo Chang, Yu-Tse Wu, Horng-Huey Ko

{"title":"Optimizing cinnamophilin delivery via SNEDDS for enhanced anti-melanogenic activity: A comprehensive evaluation of skin safety, permeability, and tyrosinase inhibition.","authors":"Yu-Chen Chen, Yih-Fung Chen, Hsin-Ya Yu, Chia-Hsuan Lin, Wan-Yi Liu, Hsun-Shuo Chang, Yu-Tse Wu, Horng-Huey Ko","doi":"10.1016/j.ijpharm.2025.126260","DOIUrl":"https://doi.org/10.1016/j.ijpharm.2025.126260","url":null,"abstract":"Skin hyperpigmentation disorders, such as melasma and age spots, result from abnormal melanin overproduction and remain a significant dermatological concern. Tyrosinase, a key enzyme in melanogenesis, represents a critical target for depigmenting therapies. Cinnamophilin (CINN), a lignan isolated from Machilus species, exhibits strong antioxidant properties and potential tyrosinase inhibitory activity. However, its poor water solubility and limited skin permeability restrict its topical application. In this study, a self-nanoemulsifying drug delivery system (SNEDDS) was developed to enhance the dermal delivery and efficacy of CINN. Molecular docking revealed the binding of CINN at the tyrosinase catalytic site through hydrogen bonding and π-π interactions, without direct coordination to catalytic copper ions. CINN also exhibited concentration-dependent tyrosinase inhibition in vitro, with an IC50 value of 39.4 ± 0.1  μM. Enzyme kinetics indicated a mixed-type inhibition mechanism. The optimized CINN-loaded SNEDDS formulation exhibited a mean droplet size of 266.8  nm with a polydispersity index of 0.295 and enhanced skin permeability by approximately threefold in a PAMPA model. In α-MSH-stimulated B16F10 cells, CINN-loaded SNEDDS significantly reduced both melanin secretion and intracellular tyrosinase activity. These findings identify CINN as a natural tyrosinase inhibitor and demonstrate the potential of SNEDDS to improve its solubility, skin permeability, and anti-melanogenic efficacy for topical application.","PeriodicalId":14187,"journal":{"name":"International Journal of Pharmaceutics","volume":" ","pages":"126260"},"PeriodicalIF":5.2,"publicationDate":"2025-10-11","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145286137","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":2,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0

Corrigendum to “Complementary approaches and advanced technologies in ameliorating rate of wound healing” [Int. J. Pharm. 682 (2025) 125910] “提高伤口愈合速度的补充方法和先进技术”的勘误表[Int.]中华医学杂志。682 (2025)125910 [j]

IF 5.2 2区医学

International Journal of Pharmaceutics Pub Date : 2025-10-11 DOI: 10.1016/j.ijpharm.2025.126261

Smitakshi Talukdar , Jharna Medhi , Pervej Alom Barbhuiya , Srijita Chakrabarti

引用次数: 0