Journal of Drug Targeting最新文献

Development of an Effective Drug Carrier for Targeted Therapy in Lung Adenocarcinoma Using ROS-responsive Micelles. 利用ros反应胶束靶向治疗肺腺癌的有效药物载体的开发。

IF 3.9 4区医学

Journal of Drug Targeting Pub Date : 2025-10-09 DOI: 10.1080/1061186X.2025.2571547

Yuan Liu, Lu Zhang, Liang Kong, Ying Bi, Yu Zhang, Lingling Han, Wuri Ouen, Tianye Yu, Zhuang Ma

{"title":"Development of an Effective Drug Carrier for Targeted Therapy in Lung Adenocarcinoma Using ROS-responsive Micelles.","authors":"Yuan Liu, Lu Zhang, Liang Kong, Ying Bi, Yu Zhang, Lingling Han, Wuri Ouen, Tianye Yu, Zhuang Ma","doi":"10.1080/1061186X.2025.2571547","DOIUrl":"https://doi.org/10.1080/1061186X.2025.2571547","url":null,"abstract":"Lung cancer is the malignant tumor with the highest growing morbidity and mortality rates worldwide. Lung adenocarcinoma is the most prevalent type of non-small cell lung cancer (NSCLC). It is highly malignant and may lead to distant metastasis at an early stage. The standard treatment for lung adenocarcinoma involves a combination of surgery and chemotherapy, which is frequently associated with severe side effects. In response to this challenge, a safe and effective drug carrier has been designed to facilitate drug delivery. The surface of this polymer micelle is modified with reactive oxygen species (ROS)-responsive targeting ligands and cell-penetrating ligands. Pemetrexed (PMX) and baicalein (BAI) are encapsulated within the micelle. The micelles exploit the high expression of ROS in the tumor microenvironment and cell-penetrating peptides to deliver drugs safely and efficiently into tumor cells, thereby inhibiting the invasion and metastasis of these cells and ultimately suppressing tumor growth. This carrier holds significant potential for guiding clinical treatment strategies for lung adenocarcinoma.","PeriodicalId":15573,"journal":{"name":"Journal of Drug Targeting","volume":" ","pages":"1-40"},"PeriodicalIF":3.9,"publicationDate":"2025-10-09","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145251156","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0

Improving the Therapeutic Efficacy and Bioavailability of Carvedilol for Control of Diabetes-Associated Heart Failure: In Vitro and In Vivo Characterization. 提高卡维地洛控制糖尿病相关性心力衰竭的疗效和生物利用度：体外和体内表征

IF 3.9 4区医学

Journal of Drug Targeting Pub Date : 2025-10-09 DOI: 10.1080/1061186X.2025.2573051

Tamer Mohamed Mahmoud, Mohammed Ayad Alboreadi, Amr Gamal Fouad, Nada H Mohammed, Amany Belal, Fahad H Baali, Nisreen Khalid Aref Albezrah, Mohammed S Alharthi, Sherif Faysal Abdelfattah Khalil, Fatma I Abo El-Ela

{"title":"Improving the Therapeutic Efficacy and Bioavailability of Carvedilol for Control of Diabetes-Associated Heart Failure: In Vitro and In Vivo Characterization.","authors":"Tamer Mohamed Mahmoud, Mohammed Ayad Alboreadi, Amr Gamal Fouad, Nada H Mohammed, Amany Belal, Fahad H Baali, Nisreen Khalid Aref Albezrah, Mohammed S Alharthi, Sherif Faysal Abdelfattah Khalil, Fatma I Abo El-Ela","doi":"10.1080/1061186X.2025.2573051","DOIUrl":"https://doi.org/10.1080/1061186X.2025.2573051","url":null,"abstract":"Carvedilol (CRD) is an oral beta-adrenergic antagonist approved for treating heart failure (HF). However, due to its short half-life and poor solubility, CRD has limited bioavailability and effectiveness. This study aimed to develop a nasal spray of CRD-novasomes (CLN) to enhance CRD's sustainability, targeting, bioavailability, and efficacy as a therapy for diabetes mellitus-associated HF (DMHF). Several CLN formulations were created using Box-Behnken design and characterized in vitro to identify the optimized formulation, which was later evaluated in vivo using an experimental DMHF rat model. The selected optimized CLN formulation consists of 30.079 mg of oleic acid, 56.897 mg of Span 60, and 60 mg of cholesterol. The optimized CLN demonstrated significant improvements over free CRD, enhancing CRD's sustainability and permeability by 71.39% and 6.08-fold, respectively. When compared to oral free CRD, the nasal CLN increased the bioavailability and target efficiency of CRD by 5.74-fold and 4.24-fold, respectively. In relation to DMHF positive control, the nasal CLN significantly lowered glucose, LDH, and CK-MB levels by 93.68%, 94.29%, and 96.50%, respectively, showcasing its efficacy. Histopathological and toxicity studies further validated the activity and safety of the optimized CLN. These findings indicate that the nasal CLN spray shows potential as a therapy for DMHF.","PeriodicalId":15573,"journal":{"name":"Journal of Drug Targeting","volume":" ","pages":"1-42"},"PeriodicalIF":3.9,"publicationDate":"2025-10-09","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145251315","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0

Effectiveness of glucosamine hydrochloride and eperisone with exercise therapy on inflammatory factors and knee joint function in patients with knee osteoarthritis. 盐酸氨基葡萄糖、依培力松联合运动疗法对膝关节骨性关节炎患者炎症因子及膝关节功能的影响。

IF 3.9 4区医学

Journal of Drug Targeting Pub Date : 2025-10-09 DOI: 10.1080/1061186X.2025.2573055

Jun Ruan, Xuanying Li

{"title":"Effectiveness of glucosamine hydrochloride and eperisone with exercise therapy on inflammatory factors and knee joint function in patients with knee osteoarthritis.","authors":"Jun Ruan, Xuanying Li","doi":"10.1080/1061186X.2025.2573055","DOIUrl":"https://doi.org/10.1080/1061186X.2025.2573055","url":null,"abstract":"Objective: This study aimed to unveil the effect of glucosamine hydrochloride (GAH) and eperisone combined with exercise therapy on inflammatory markers and knee joint function in patients with knee osteoarthritis (KOA).Methods: Sixty KOA patients were randomly assigned into two groups. Group A (n = 30) received GAH plus exercise therapy, while Group B (n = 30) received GAH combined with eperisone and exercise therapy. Serum inflammatory factors, knee symptom scores (pain, stiffness, daily function), and functional measures [knee flexion range of motion (ROM), Lysholm score, five-time sit-to-stand test, and 15-meter walking time] were assessed before and after treatment. Clinical efficacy was also evaluated.Results: Post-treatment, both groups showed decreased serum MMP-3, TNF-α, and IL-6 levels, with significantly greater reductions in Group B (P < 0.001). Group B had lower symptom scores (P < 0.05), greater ROM and Lysholm improvements (P < 0.001), and better functional performance (P < 0.001). The effective rate was higher in Group B (100.00%) than in Group A (86.67%) (P = 0.038).Conclusion: GAH combined with eperisone and exercise therapy is more effective than GAH alone in patients with KOA. It significantly reduces inflammatory markers and symptoms, and enhances knee joint function.","PeriodicalId":15573,"journal":{"name":"Journal of Drug Targeting","volume":" ","pages":"1-41"},"PeriodicalIF":3.9,"publicationDate":"2025-10-09","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145251285","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0

Design and in vivo evaluation of a multi-epitope vaccine that suppresses tumor growth in a murine colorectal cancer model. 抑制小鼠结直肠癌模型肿瘤生长的多表位疫苗的设计和体内评价

IF 3.9 4区医学

Journal of Drug Targeting Pub Date : 2025-10-09 DOI: 10.1080/1061186X.2025.2573054

Alisa Khodadadi, Saeid Afshar, Rezvan Najafi, Alireza Zamani, Razieh Dalirfardouei, Meysam Soleimani

{"title":"Design and in vivo evaluation of a multi-epitope vaccine that suppresses tumor growth in a murine colorectal cancer model.","authors":"Alisa Khodadadi, Saeid Afshar, Rezvan Najafi, Alireza Zamani, Razieh Dalirfardouei, Meysam Soleimani","doi":"10.1080/1061186X.2025.2573054","DOIUrl":"https://doi.org/10.1080/1061186X.2025.2573054","url":null,"abstract":"Harnessing the immune system through cancer vaccines offers a promising strategy to overcome tumor heterogeneity, which remains one of the most significant challenges in achieving effective treatment for colorectal cancer (CRC). In this study, we designed and validated a novel multi-epitope vaccine against CRC using integrated computational and experimental approaches. The final construct was developed through in silico prediction and optimization, followed by recombinant expression and in vivo testing in a CRC mouse model. Mice receiving the multi-dose vaccine exhibited a mean tumor volume approximately 80% lower than that of the untreated cancer group. Additionally, IL-4 levels were significantly elevated (p < 0.0001), consistent with activation of humoral immune responses. Histopathological assessment showed largely preserved tissue architecture in the spleen, kidney, and liver. The multi-dose vaccine group achieved 100% survival, compared with 60% survival in the untreated cancer group. These results suggest the vaccine can suppress tumor progression, enhance immune responses, and provide systemic protection, supporting further preclinical development.","PeriodicalId":15573,"journal":{"name":"Journal of Drug Targeting","volume":" ","pages":"1-22"},"PeriodicalIF":3.9,"publicationDate":"2025-10-09","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145251192","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0

DNAJA1 as a Modulator of CD8⁺ T-Cell Function and Prognosis in Lung Cancer: Implications for Immune Regulation and Therapeutic Targeting. DNAJA1作为CD8+ t细胞功能和肺癌预后的调节剂：免疫调节和治疗靶向的意义

IF 3.9 4区医学

Journal of Drug Targeting Pub Date : 2025-10-08 DOI: 10.1080/1061186X.2025.2571546

Shengkai Yang, Lian Liu, Yubiao Guo, Luqi Dai

{"title":"DNAJA1 as a Modulator of CD8+ T-Cell Function and Prognosis in Lung Cancer: Implications for Immune Regulation and Therapeutic Targeting.","authors":"Shengkai Yang, Lian Liu, Yubiao Guo, Luqi Dai","doi":"10.1080/1061186X.2025.2571546","DOIUrl":"https://doi.org/10.1080/1061186X.2025.2571546","url":null,"abstract":"In lung adenocarcinoma (LUAD), dysfunctional CD8+ T-cells and an immunosuppressive tumour microenvironment (TME) are major barriers to effective immunotherapy, yet the molecular regulators coordinating T cell exhaustion and macrophage polarization remain undefined. To address this, we integrated single-cell RNA sequencing, TCGA transcriptome and methylation data, co-culture assays, chromatin profiling, functional assays, and xenograft models to investigate the role of DNAJA1 in immune regulation and tumor progression. Our results demonstrated that DNAJA1 was upregulated in exhausted CD8+ T-cells in lung cancer tissues and correlated positively with exhaustion markers including PD-1, TIM-3, and LAG-3. Notably, exhausted CD8+ T-cells exhibited DNAJA1 promoter hypomethylation and enrichment of activating histone modifications H3K4me3 and H3K27ac, while inhibiting the activation of H3K4me3 and H3K27ac reduced DNAJA1 expression. Additionally, DNAJA1 overexpression upregulated M2-associated genes (CD206 and IL-10), while its knockdown enhanced the expression of M1-associated genes (CD86 and IL-12). Furthermore, DNAJA1 promoted tumour cell proliferation, and its expression level showed a moderate positive correlation with PD-L1. Collectively, these findings establish DNAJA1 as an epigenetically activated regulator that drives CD8+ T-cell exhaustion and protumor macrophage polarization, highlighting its dual role as a functional immunomodulator and potential biomarker for stratifying LUAD patients with immune-dysregulated TME.","PeriodicalId":15573,"journal":{"name":"Journal of Drug Targeting","volume":" ","pages":"1-25"},"PeriodicalIF":3.9,"publicationDate":"2025-10-08","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145251180","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0

SUPRADES: unlocking the versatility of cyclodextrin-based deep eutectic solvents. SUPRADES：解锁环糊精基深共晶溶剂的多功能性。

IF 3.9 4区医学

Journal of Drug Targeting Pub Date : 2025-09-29 DOI: 10.1080/1061186X.2025.2563606

Nikita V Pawar, Maheshkumar R Borkar

{"title":"SUPRADES: unlocking the versatility of cyclodextrin-based deep eutectic solvents.","authors":"Nikita V Pawar, Maheshkumar R Borkar","doi":"10.1080/1061186X.2025.2563606","DOIUrl":"10.1080/1061186X.2025.2563606","url":null,"abstract":"Green and sustainable technologies have emerged in recent years as a result of increased public awareness of the damaging effects that chemicals have on the environment. To replace ionic liquids (ILs) and traditional organic solvents, deep eutectic solvents (DESs) have been created as environmentally friendly solvents in various fields. In recent years researchers have looked at creating deep eutectic supramolecular polymers (DESPs) by combining DESs with macrocyclic host molecules, such as cyclodextrins (CDs), cucurbiturils and crown ethers. The Supramolecular Deep Eutectic Solvents (SUPRADES), Cyclodextrin-based DES (CycloDES) and Low Melting Mixtures (LMMs) are examples of DESPs. This article provides a comprehensive review on SUPRADES and its applications in various areas like drug solubility enhancement, extraction of different compounds, chiral separation, absorption of volatile organic compounds etc. Compared to traditional DESs and ILs, SUPRADES offer advantages like improved selectivity, tuneability, and biocompatibility. Notably, the review highlights the key differences between traditional DESs/ILs and new SUPRADES, including their increased molecular recognition power and designed host-guest interactions. Through the integration of dispersed results, this review sheds fresh light on how SUPRADES can surpass deficiencies of previous systems and proposes future applications for their practical utilisation.","PeriodicalId":15573,"journal":{"name":"Journal of Drug Targeting","volume":" ","pages":"1-18"},"PeriodicalIF":3.9,"publicationDate":"2025-09-29","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145102781","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0

Improving the bioavailability and therapeutic efficacy of valsartan for the control of cardiotoxicity-associated breast cancer. 提高缬沙坦控制心脏毒性相关乳腺癌的生物利用度和疗效。

IF 3.9 4区医学

Journal of Drug Targeting Pub Date : 2025-09-29 DOI: 10.1080/1061186X.2025.2564352

Mary Eskander Attia, Fatma I Abo El-Ela, Saad M Wali, Amr Gamal Fouad, Amany Belal, Fahad H Baali, Nisreen Khalid Aref Albezrah, Mohammed S Alharthi, Marwa M Nagib

{"title":"Improving the bioavailability and therapeutic efficacy of valsartan for the control of cardiotoxicity-associated breast cancer.","authors":"Mary Eskander Attia, Fatma I Abo El-Ela, Saad M Wali, Amr Gamal Fouad, Amany Belal, Fahad H Baali, Nisreen Khalid Aref Albezrah, Mohammed S Alharthi, Marwa M Nagib","doi":"10.1080/1061186X.2025.2564352","DOIUrl":"10.1080/1061186X.2025.2564352","url":null,"abstract":"Cardiotoxicity remains the most severe side effect of breast cancer (BC) treatments. Valsartan, an angiotensin II receptor blocker, has antioxidant properties that can mitigate cardiotoxicity-associated BC (CABC). However, valsartan's limited solubility and low bioavailability result in reduced effectiveness. Therefore, this study developed an in-situ nasal pH-responsive valsartan-loaded novasome (ISVLN) to enhance valsartan's sustainability, bioavailability, targeting and efficacy when used alongside chemotherapy to prevent CABC. Various VLN formulations were created and optimised using the Box-Behnken design. The optimal formulation was mixed with chitosan and glyceryl monooleate to develop ISVLN, which was further assessed in vivo using a DMBA-induced breast cancer (DIBC) rat model to evaluate its bioavailability and efficacy. The optimal VLN formulation comprises oleic acid (26 mg), Span 60 (65 mg) and cholesterol (52 mg). The ISVLN formulation improved valsartan's sustainability, permeability and bioavailability compared to free valsartan by 66.40%, 7.46-fold and 4.57-fold, respectively. The ISVLN formulation enhanced valsartan's targeting in both the tumour and heart by 2.30-fold and 1.96-fold, respectively. Compared with the DIBC-positive group, the ISVLN group reduced the tumour volume and mortality rate by 86.20% and 23.53%, respectively. Furthermore, the ISVLN group reduced the LDH and CK-MB levels by 96.11% and 95.97%, respectively. Histopathological analysis confirmed the efficacy of the ISVLN formulation. These findings suggest that a nasal ISVLN could serve as an adjuvant therapy to prevent CABC.","PeriodicalId":15573,"journal":{"name":"Journal of Drug Targeting","volume":" ","pages":"1-20"},"PeriodicalIF":3.9,"publicationDate":"2025-09-29","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145102757","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0

Formulation and optimisation of nanoemulsions for enhancing topical delivery of methotrexate in CFA induced arthritis rat model. 增强甲氨蝶呤在CFA性关节炎大鼠模型中的局部递送的NEs的配方和优化。

IF 3.9 4区医学

Journal of Drug Targeting Pub Date : 2025-09-29 DOI: 10.1080/1061186X.2025.2565409

Amruta Parmar, Brijesh Sukumaran

{"title":"Formulation and optimisation of nanoemulsions for enhancing topical delivery of methotrexate in CFA induced arthritis rat model.","authors":"Amruta Parmar, Brijesh Sukumaran","doi":"10.1080/1061186X.2025.2565409","DOIUrl":"10.1080/1061186X.2025.2565409","url":null,"abstract":"Methotrexate (MTX) is widely used in treating cancers and inflammatory conditions like psoriasis and rheumatoid arthritis (RA), however is associated with side effects. Nanoemulsions (NEs) offer enhanced stability, protection and improved permeation via various delivery routes. MTX-loaded oil-in-water NEs (O/W NEs) were formulated to improve entrapment efficiency, permeation ability and efficacy in CFA-induced arthritis model. The area of NEs was identified by pseudoternary phase diagrams, optimisation of MTX-NEs was performed using I-optimal mixture design, and characterised for %entrapment efficiency, droplet size, polydispersity index, zeta potential, morphology and %transmittance. The MTX-NE gel was evaluated for rheology, in vitro drug release, ex vivo permeation and efficacy in a CFA-induced arthritic rats. The MTX-NEs were prepared using Smix ratio of 3:1 with 0.2 N sodium hydroxide as aqueous phase. It showed >90% entrapment efficiency, size of 161.4 ± 13.5 nm, and 94 ± 1.8% of %transmittance. MTX-NE gel showed sustained release of 86 ± 1.8% MTX, and cumulative permeation of 77.6 ± 1.4% with a flux of 0.184 µg/cm2·h. Efficacy studies in a CFA-induced rat model resulted in significant reduction of paw oedema, radiographic, histopathological and inflammatory biomarkers. The optimised MTX-NE gel showed enhanced delivery, sustained release and significant anti-arthritic effects, supporting its potential as an effective for RA therapy.","PeriodicalId":15573,"journal":{"name":"Journal of Drug Targeting","volume":" ","pages":"1-17"},"PeriodicalIF":3.9,"publicationDate":"2025-09-29","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145131185","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0

pH-targeted and time-released microparticles of quercetin and lycopene for ulcerative colitis treatment: DoE-based formulation development, pharmacokinetics, and in-vivo proof of concept studies. 用于溃疡性结肠炎治疗的ph靶向和时间释放的槲皮素和番茄红素微粒：基于doe的配方开发，药代动力学和体内概念验证研究。

IF 3.9 4区医学

Journal of Drug Targeting Pub Date : 2025-09-25 DOI: 10.1080/1061186X.2025.2561211

Syaiful Choiri, Nadia Risti Ikka Pertiwi, Diva Amanda Nur Saputri, Syahwa Agustin Rahmawati, Yuliana Sabella Widyasari, Nanang Wiyono, Ilham Kuncahyo

{"title":"pH-targeted and time-released microparticles of quercetin and lycopene for ulcerative colitis treatment: DoE-based formulation development, pharmacokinetics, and in-vivo proof of concept studies.","authors":"Syaiful Choiri, Nadia Risti Ikka Pertiwi, Diva Amanda Nur Saputri, Syahwa Agustin Rahmawati, Yuliana Sabella Widyasari, Nanang Wiyono, Ilham Kuncahyo","doi":"10.1080/1061186X.2025.2561211","DOIUrl":"10.1080/1061186X.2025.2561211","url":null,"abstract":"Lycopene (LYC) and quercetin (QRN) exhibit synergistic effects on ulcerative colitis (UC) treatment due to their anti-inflammatory and antioxidant properties. This study aimed to develop a microparticle formulation utilising pH-sensitive and time-release-based polymers, namely Eudragit L and Eudragit RS, respectively, to achieve colon-targeted and controlled-release delivery. Subsequently, pharmacokinetics and UC therapy proof-of-concept studies were conducted. The box-Behnken design was employed to develop and optimise the LYC-QRN microparticles, characterised by particle size and distribution, entrapment efficiency (EE), and drug loading, followed by morphology, molecular, thermal and crystallinity evaluations. The polymers primarily contributed to LYC-QRN encapsulation and loading, while the drug concentration influenced particle size behaviour. The optimised formulation was achieved using 4.10% Eudragit RS, 0.76% Eudragit L, and a drug concentration of 7.82%, resulting in an EE of >50%. QRN and LYC loading were approximately 50 and 25 mg/g, respectively, and the particle size was nearly 1 µm, exhibiting minimal variation. Characterisation demonstrated that the drug in the microparticle dispersed molecularly as an amorphous system, devoid of any chemical interactions. The drug was released at a specific pH-triggering system, enhancing its bioavailability by 3.5-fold. In-vivo evaluation demonstrated that LYC-QRN microparticles effectively cured chronic colon inflammation and protected the gastric mucus layers.","PeriodicalId":15573,"journal":{"name":"Journal of Drug Targeting","volume":" ","pages":"1-13"},"PeriodicalIF":3.9,"publicationDate":"2025-09-25","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145054215","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0

Nanotechnology-driven approaches for the early detection and targeted treatment of Alzheimer's disease. 纳米技术驱动的阿尔茨海默病早期检测和靶向治疗方法。

IF 3.9 4区医学

Journal of Drug Targeting Pub Date : 2025-09-19 DOI: 10.1080/1061186X.2025.2561788

Dinesh Kumar Sharma

引用次数: 0