Assay and drug development technologies最新文献_第3页

Protective Effects of Schizochytrium Microalgal Fatty Acids on Alcoholic Liver Disease: A Network Pharmacology and In Vivo Study. 分裂藻微藻脂肪酸对酒精性肝病的保护作用：网络药理学和体内研究

IF 1.6 4区医学

Assay and drug development technologies Pub Date : 2025-04-01 Epub Date: 2025-01-16 DOI: 10.1089/adt.2024.106

Cailin Luo, Li Tian, Yangmin Wen, Zhihua Zheng

{"title":"Protective Effects of Schizochytrium Microalgal Fatty Acids on Alcoholic Liver Disease: A Network Pharmacology and In Vivo Study.","authors":"Cailin Luo, Li Tian, Yangmin Wen, Zhihua Zheng","doi":"10.1089/adt.2024.106","DOIUrl":"10.1089/adt.2024.106","url":null,"abstract":"\u0000 This study aimed to elucidate the hepatoprotective mechanisms of microalgal fatty acids (MFA) from Schizochytrium against alcoholic liver disease (ALD) through network pharmacology and in vivo analysis. Network pharmacology and molecular docking methodologies were employed to predict the potential mechanisms of MFA against ALD. To substantiate these predictions, an acute alcoholic liver injury mouse model was utilized to assess the impact of MFA on serum levels of alanine aminotransferase (ALT), alkaline phosphatase (ALP), aspartate aminotransferase (AST), total protein (TP), and albumin (ALB). Additionally, liver histopathology and the expression levels of phosphatidylinositol 3 kinase (PI3K) and protein kinase B (AKT) protein were evaluated. Seven active ingredients and 53 potential targets (including 7 core targets) for ALD treatment were identified in MFA. Kyoto Encyclopedia of Genes and Genomes pathway analyses indicated that these seven core targets are implicated in various biological pathways, notably those associated with cancer, viral infections, and the PI3K/AKT signaling pathway. Furthermore, molecular docking studies demonstrated that docosahexaenoic acid and docosapentaenoic acid in MFA exhibited strong binding affinity for these seven crucial targets. Animal experiments demonstrated that administration of MFA significantly decreased the levels of AST, ALT, and ALP, while increasing the levels of ALB and TP in mice with acute alcoholic liver injury. Moreover, MFA ameliorated liver tissue pathology and markedly down-regulated the expression of PI3K and AKT proteins in the liver. These results suggest that MFA may possess therapeutic potential for ALD by targeting multiple pathways, with its mechanisms likely involving the inhibition of the PI3K/AKT signaling pathway.\u0000 ","PeriodicalId":8586,"journal":{"name":"Assay and drug development technologies","volume":" ","pages":"151-163"},"PeriodicalIF":1.6,"publicationDate":"2025-04-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142999183","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

Glycerosomes: Versatile Carriers for Multi-Route Drug Delivery Systems. 甘油小体：多途径给药系统的多功能载体。

IF 1.6 4区医学

Assay and drug development technologies Pub Date : 2025-04-01 Epub Date: 2025-02-12 DOI: 10.1089/adt.2024.098

Kunal Banode, Omkar Patharkar, Vaishnavi Jadhav, Neha Mundhe, Uddhav Mhatre, Madhur Kulkarni

{"title":"Glycerosomes: Versatile Carriers for Multi-Route Drug Delivery Systems.","authors":"Kunal Banode, Omkar Patharkar, Vaishnavi Jadhav, Neha Mundhe, Uddhav Mhatre, Madhur Kulkarni","doi":"10.1089/adt.2024.098","DOIUrl":"10.1089/adt.2024.098","url":null,"abstract":"\u0000 Glycerosomes signify a groundbreaking advancement in drug delivery technology. Comprising glycerol, phospholipids, and water, glycerosomes offer superior drug stability, penetration, entrapment efficiency, fluidity, and viscosity compared with conventional liposomes. Their formation process eliminates the need for specific transition temperatures, streamlining production. Glycerol's plasticizing properties enhance vesicle elasticity and flexibility, enabling enhanced skin penetration. These vesicles demonstrate immense promise across a range of drug delivery pathways. In dermal and transdermal applications, glycerosomes augment drug permeation by moisturizing the stratum corneum and improving membrane fluidity. For oral delivery, they shield drugs from the harsh gastrointestinal environment and boost intestinal absorption. Pulmonary delivery benefits from glycerosomes' capacity to stabilize and disperse aerosolized vesicles, facilitating deep penetration into lung tissues. Ophthalmic applications profit from increased corneal penetration and extended retention. Intranasal use of glycerosomes enhances mucosal penetration and enables direct drug delivery to the central nervous system by circumventing the blood-brain barrier. Ongoing advancements in glycerosome technology concentrate on integrating diverse functional ingredients like essential oils, β-sitosterol, sodium hyaluronate, and trimethyl chitosan to develop specialized formulations. These variants include STO-glycerosomes, S-glycerosomes, PO-S-glycerosomes, HY-glycerosomes, TMC-glycerosomes, glycethosomes, and glycerospanlastics, all offering enhanced stability, permeability, and therapeutic efficacy. This review delves into the mechanisms of drug transport within glycerosomes, their applications in various delivery routes, and the latest technological developments, highlighting their substantial potential as versatile carriers in contemporary drug delivery systems.\u0000 ","PeriodicalId":8586,"journal":{"name":"Assay and drug development technologies","volume":" ","pages":"136-150"},"PeriodicalIF":1.6,"publicationDate":"2025-04-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143397930","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

Deep Learning Accelerates the Development of Antimicrobial Peptides Comprising 15 Amino Acids. 深度学习加速了包含15个氨基酸的抗菌肽的开发。

IF 1.6 4区医学

Assay and drug development technologies Pub Date : 2025-03-27 DOI: 10.1089/adt.2025.011

Yuchen Hu, Junchao Zhou, Yuhang Gao, Ban Chen, Jiangtao Su, Hong Li

{"title":"Deep Learning Accelerates the Development of Antimicrobial Peptides Comprising 15 Amino Acids.","authors":"Yuchen Hu, Junchao Zhou, Yuhang Gao, Ban Chen, Jiangtao Su, Hong Li","doi":"10.1089/adt.2025.011","DOIUrl":"https://doi.org/10.1089/adt.2025.011","url":null,"abstract":"\u0000 The emergence of multidrug-resistant bacteria has led to an urgent need for novel antimicrobial agents. Antimicrobial peptides (AMPs) exhibit broad-spectrum and highly effective antibacterial activity and are less prone to resistance, making them potential candidates for the next generation of antimicrobial drugs. However, screening for AMPs from a vast library of peptides through wet lab experiments is a slow and laborious process. By leveraging large datasets of labeled peptides, researchers utilize deep learning algorithms to train models that capture complex patterns and features associated with antimicrobial activity, which advance the discovery and development of novel AMPs. Since the discovery of certain lengths of AMPs has been rarely reported, we applied deep learning to accelerate the discovery of AMPs consisting of 15 amino acids and developed a model named AMPPRED15 in this article. Wet lab experiments were also conducted to evaluate the performance of the model. Fortunately, we successfully identified two AMPs, one of which demonstrated antibacterial activities comparable to the marketed antibiotic cefoperazone sodium.\u0000 ","PeriodicalId":8586,"journal":{"name":"Assay and drug development technologies","volume":" ","pages":""},"PeriodicalIF":1.6,"publicationDate":"2025-03-27","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143727615","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

Pharmacological Evaluation of Aescin for Neuroprotection in Intracerebroventricular Streptozotocin Model of Alzheimer's Disease in Experimental Rats. 七叶皂苷对实验性阿尔茨海默病大鼠脑室内链脲佐菌素模型神经保护作用的药理评价。

IF 1.6 4区医学

Assay and drug development technologies Pub Date : 2025-03-17 DOI: 10.1089/adt.2024.130

Shaveta Bhardwaj, Anu Jindal, Shamsher Singh, Romanpreet Kaur, Amarjot Kaur Grewal

{"title":"Pharmacological Evaluation of Aescin for Neuroprotection in Intracerebroventricular Streptozotocin Model of Alzheimer's Disease in Experimental Rats.","authors":"Shaveta Bhardwaj, Anu Jindal, Shamsher Singh, Romanpreet Kaur, Amarjot Kaur Grewal","doi":"10.1089/adt.2024.130","DOIUrl":"https://doi.org/10.1089/adt.2024.130","url":null,"abstract":"\u0000 Alzheimer's disease (AD) is a neurological disorder that results in the loss of memory and cognitive functions linked to redox disbalance, neuroinflammation, neurotransmitters changes, and the accumulation of amyloid-beta (1-42) plaques in AD. In this study, rats were administered with intracerebroventricular (ICV) streptozotocin (STZ) to produce AD-like symptoms in rats. ICV-STZ bilaterally, 3 mg/kg, was infused on days 1 and 3 with the help of Hamilton syringe by fixing cannula at the target position of rat brain using coordinates -2 mm (anteriposterior), 1.6 mm Mediolateral (ML), and 1.5 mm (dorsoventral). Learning and spatial memory were checked using Morris water maze and elevated plus maze apparatus. In ICV-STZ, rats lost their spatial and learning memory, increased level of prooxidant like Lipid peroxidation (LPO), nitrite and reduced glutathione (GSH), catalase, and superoxide dismutase (SOD) level. The increased level acetylcholinesterase (AChE) catalyzed acetylcholine (ACh) concentration indicates cholinergic neuron degeneration. Furthermore, we found raised inflammatory markers and altered neurotransmitters level after ICV-STZ. Administration of aescin (10, 20, and 30 mg/kg, p.o.) dose-dependently ameliorated the behavioral alteration and inhibited inflammatory markers like tumor necrosis factor-alpha, interleukin-6 (IL-6), and IL-1β. Furthermore, aescin restored antioxidants like GSH, SOD, and catalase and reduced the nitrite and lipid peroxidation level. AChE enzyme causes degradation of ACh, and its level was declined after treatment with aescin. Aescin also restored GABA, norepinephrine, and serotonin level in the brain with prevention of raised glutamate level. Moreover, the histopathological study confirmed neuronal pathogenesis, and aescin significantly achieved neuroprotective effect via preventing neuroinflammation, balancing redox potential, and inhibiting AChE enzyme.\u0000 ","PeriodicalId":8586,"journal":{"name":"Assay and drug development technologies","volume":" ","pages":""},"PeriodicalIF":1.6,"publicationDate":"2025-03-17","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143647074","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

Next-Gen Cancer Treatment: Nanotechnology-Driven siRNA Delivery Solutions. 新一代癌症治疗：纳米技术驱动的 siRNA 递送解决方案。

IF 1.6 4区医学

Assay and drug development technologies Pub Date : 2025-03-13 DOI: 10.1089/adt.2024.121

Harshita, Vancha Harish, Sakshi Lad Upendra, Sharfuddin Mohd, Sachin Kumar Singh, Pooja Agrawal, Sukriti Vishwas, Kamal Dua

{"title":"Next-Gen Cancer Treatment: Nanotechnology-Driven siRNA Delivery Solutions.","authors":"Harshita, Vancha Harish, Sakshi Lad Upendra, Sharfuddin Mohd, Sachin Kumar Singh, Pooja Agrawal, Sukriti Vishwas, Kamal Dua","doi":"10.1089/adt.2024.121","DOIUrl":"https://doi.org/10.1089/adt.2024.121","url":null,"abstract":"\u0000 RNA interference through small interfering RNA (siRNA) has shown great promise as a potential cancer treatment strategy in recent years. However, the delivery of siRNA to target cancer cells efficiently remains a significant challenge. This review aims to highlight the recent advances in nanotechnology-enabled siRNA delivery for cancer treatment, bridging the gap between bench research and clinical application. A comprehensive literature search was conducted to identify recent studies focused on the utilization of nanotechnology for siRNA delivery in cancer treatment. Key databases, including PubMed, Scopus, and Web of Science, were used, and relevant articles were screened. Several nanotechnology-based platforms for siRNA delivery have emerged in recent years, providing enhanced selectivity, improved stability, and controlled release profiles. The primary types of nanocarriers discussed include lipid-based nanoparticles, inorganic nanoparticles, polymeric nanoparticles, and exosomes. Nanotechnology-based siRNA delivery systems represent a promising avenue for cancer treatment. Although significant progress has been made in preclinical studies, translating these findings to clinical applications poses several challenges, including scale-up production, safety, and targeted delivery. Nevertheless, the recent developments in this field hold great promise in revolutionizing cancer therapy, providing hope for more effective and personalized treatment options in the future.\u0000 ","PeriodicalId":8586,"journal":{"name":"Assay and drug development technologies","volume":" ","pages":""},"PeriodicalIF":1.6,"publicationDate":"2025-03-13","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143623260","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

A Pioneer Review on Lactoferrin-Conjugated Extracellular Nanovesicles for Targeting Cellular Melanoma: Recent Advancements and Future Prospects. 乳铁蛋白结合的细胞外纳米囊泡靶向细胞黑色素瘤的先驱综述：最新进展和未来展望。

IF 1.6 4区医学

Assay and drug development technologies Pub Date : 2025-02-01 Epub Date: 2024-12-10 DOI: 10.1089/adt.2024.045

Dilpreet Singh, Sonima Prasad

{"title":"A Pioneer Review on Lactoferrin-Conjugated Extracellular Nanovesicles for Targeting Cellular Melanoma: Recent Advancements and Future Prospects.","authors":"Dilpreet Singh, Sonima Prasad","doi":"10.1089/adt.2024.045","DOIUrl":"10.1089/adt.2024.045","url":null,"abstract":"\u0000 Melanoma, a highly aggressive form of skin cancer, presents a formidable challenge in terms of treatment due to its propensity for metastasis and resistance to conventional therapies. The development of innovative nanocarriers for targeted drug delivery has opened new avenues in cancer therapy. Lactoferrin-conjugated extracellular nanovesicles (LF-EVs) have emerged as a promising vehicle in the targeted treatment of cellular melanoma, owing to their natural biocompatibility, enhanced bioavailability, and ability to traverse biological barriers effectively. This review synthesizes recent advancements in the use of LF-EVs as a novel drug delivery system for melanoma, emphasizing their unique capacity to enhance cellular uptake through LF's receptor-mediated endocytosis pathways. Key studies demonstrate that LF conjugation significantly increases the specificity of extracellular nanovesicles for melanoma cells, minimizes off-target effects, and promotes efficient intracellular drug release. Furthermore, we explore how LF-EVs interact with the tumor microenvironment, potentially inhibiting melanoma progression and metastasis while supporting antitumor immune responses. Future prospects in this field include optimizing LF conjugation techniques, improving the scalability of LF-EV production, and integrating multifunctional payloads to target drug resistance mechanisms. This review highlights the potential of LF-EVs to transform melanoma treatment strategies, bridging current gaps in therapeutic delivery and paving the way for personalized and less invasive melanoma therapies.\u0000 ","PeriodicalId":8586,"journal":{"name":"Assay and drug development technologies","volume":" ","pages":"55-69"},"PeriodicalIF":1.6,"publicationDate":"2025-02-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142799337","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

In Silico Screening of Phytochemicals as Potential Inhibitors of the JAK/STATs Pathway in Psoriasis. 银屑病JAK/STATs通路潜在抑制剂植物化学物质的硅筛选

IF 1.6 4区医学

Assay and drug development technologies Pub Date : 2025-02-01 Epub Date: 2025-01-08 DOI: 10.1089/adt.2024.087

Lokendra Singh Rathor, Divya Sahu, Manju Singh, Deependra Singh

{"title":"In Silico Screening of Phytochemicals as Potential Inhibitors of the JAK/STATs Pathway in Psoriasis.","authors":"Lokendra Singh Rathor, Divya Sahu, Manju Singh, Deependra Singh","doi":"10.1089/adt.2024.087","DOIUrl":"10.1089/adt.2024.087","url":null,"abstract":"\u0000 The skin is a dynamic tissue that consists of different layers such as stratum corneum, the site for keratinocyte development and maturation for the natural changeover of skin. In psoriasis, this natural development of keratinocytes gets disturbed and aggregation of nucleated keratinocytes takes place in the epidermis of the skin, leading to the presence of scaly skin, which makes the patient physically, socially, and psychologically ill. Various natural, semisynthetic, and synthetic treatments are available. Still, semisynthetic or synthetic are mainly used to treat psoriasis with side effects on different parts of the body, which is life threatening. Various molecular target sites are getting upregulated such as Janus kinase/Signal transducer and activator of transcription (JAK/STATs), phosphodiesterase 4 (PDE4), mitogen-activated protein kinase (MAPK), platelet selectin (Pan Selectin), Tumor Necrosis Factor Alpha (TNF-α), Interleukin-23 (IL-23), Interleukin-17 (IL-17), and Tyrosine Kinase 2 (Tyk2) in psoriasis. Plants and their bioactive compounds of flavonoids, alkaloids, resins, tannins, glycosides, and terpenoids category are used in the treatment of psoriasis as topical, oral, and biological forms. Using a computational approach, the inhibition of these molecular targets can be studied and potential molecules can be identified. This research article aims to find out the potential molecules that can inhibit the molecular sites and are effective than synthetic ones.\u0000 ","PeriodicalId":8586,"journal":{"name":"Assay and drug development technologies","volume":" ","pages":"100-113"},"PeriodicalIF":1.6,"publicationDate":"2025-02-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142943381","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

Golden Therapeutic Approach to Combat Viral Diseases Using Gold Nanomaterials. 利用金纳米材料对抗病毒性疾病的黄金治疗方法。

IF 1.6 4区医学

Assay and drug development technologies Pub Date : 2025-02-01 Epub Date: 2024-12-11 DOI: 10.1089/adt.2024.071

Jasmine, Neelam Singh, Dheeraj Nagpal, Sanchit Puniani, Puneet Gupta

{"title":"Golden Therapeutic Approach to Combat Viral Diseases Using Gold Nanomaterials.","authors":"Jasmine, Neelam Singh, Dheeraj Nagpal, Sanchit Puniani, Puneet Gupta","doi":"10.1089/adt.2024.071","DOIUrl":"10.1089/adt.2024.071","url":null,"abstract":"\u0000 Gold nanoparticles (AuNPs), due to their unique properties and surface modification abilities, have become a promising carrier for a range of biomedical applications. AuNPs have intrinsic antiviral characteristics because of their capacity to enhance drug distribution by making antiviral medications more stable and soluble, which assures that higher quantities reach the intended site. Through surface changes, AuNPs can bind directly to viral particles or infected cells, increasing therapeutic efficiency and reducing side effects. AuNPs efficiently damage cell membranes and hinder viral reproduction within a host cell. Furthermore, because of their large surface area-to-volume ratio, which enables many functional groups to connect, improving interaction with virus particles and ceasing their multiplication. By altering dimensions and morphology or conjugating it with additional antiviral drugs, AuNPs can array their synergistic antiviral activity. Thus, the development of AuNP conjugated therapy presents a promising avenue to address the demand for novel anti-viral therapeutics against infections resistant to several drugs.\u0000 ","PeriodicalId":8586,"journal":{"name":"Assay and drug development technologies","volume":" ","pages":"70-83"},"PeriodicalIF":1.6,"publicationDate":"2025-02-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142806059","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

Development and Characterization of Oral Efavirenz-Loaded Nanostructured Lipid Carriers and Their Optimization with Box-Behnken Design Approach for the Neurological Disorder. 口服依非韦伦纳米结构脂质载体的开发和表征及其用于神经系统疾病的Box-Behnken设计方法优化

IF 1.6 4区医学

Assay and drug development technologies Pub Date : 2025-02-01 Epub Date: 2025-01-31 DOI: 10.1089/adt.2024.115

Ali Sartaj, Bushra Nabi, Ashif Iqubal, Nidhi Aggarwal, Kashif Haider, Sanjula Baboota, Javed Ali

{"title":"Development and Characterization of Oral Efavirenz-Loaded Nanostructured Lipid Carriers and Their Optimization with Box-Behnken Design Approach for the Neurological Disorder.","authors":"Ali Sartaj, Bushra Nabi, Ashif Iqubal, Nidhi Aggarwal, Kashif Haider, Sanjula Baboota, Javed Ali","doi":"10.1089/adt.2024.115","DOIUrl":"10.1089/adt.2024.115","url":null,"abstract":"To enhance brain delivery of efavirenz (EFV), optimized nanostructured lipid carriers (NLCs) were developed using a melt-emulsification technique and probe sonication. Box-Behnken design was chosen to systematically analyze the effects of variables on formulation outcomes, enabling efficient optimization with fewer experimental trials. This selection helped to improve the formulation by allowing us to refine key characteristics such as particle size, entrapment efficiency, and polydispersity index (PDI). The optimized EFV-NLCs had a mean particle size of 91.41 ± 7.90 nm, a PDI of 0.28 ± 0.04, a zeta potential of -17 mV, an entrapment efficiency of 85 ± 7%, and a drug loading of 14 ± 1%. Transmission electron microscopy confirmed that the EFV-NLCs were spherical with uniform size distribution. In vitro release tests showed prolonged drug release, with release rates ranging from 63.09 ± 2.76% to 84.43 ± 4.24% at pH 1.2 and 87.66 ± 6.31% to 92.56 ± 1.48% at pH 6.8. This was significantly better than the EFV suspension, which showed moderate and unsustainable release rates over 8 h. Furthermore, dissolution studies in both fasted and fed state simulated-intestinal-fluids (FaSSIF and FeSSIF) over 6 h revealed that % cumulative drug release was significantly higher in FeSSIF (94.06 ± 1.62%) compared with FaSSIF (65.21 ± 3.95%), indicating enhanced absorption in the presence of food. In vitro gut permeation studies revealed that EFV-NLCs had a 2.05-fold higher drug permeability than the suspension. These findings suggest that EFV-NLCs are promising for targeted brain delivery, are safe for oral administration, and could be instrumental in managing neuro-acquired immunodeficiency syndrome.","PeriodicalId":8586,"journal":{"name":"Assay and drug development technologies","volume":" ","pages":"84-99"},"PeriodicalIF":1.6,"publicationDate":"2025-02-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143063446","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

Drug Repurposing Patent Applications July-September 2024. 药物再利用专利申请2024年7月至9月。

IF 1.6 4区医学

Assay and drug development technologies Pub Date : 2025-01-01 Epub Date: 2024-11-29 DOI: 10.1089/adt.2024.126

Hermann A M Mucke

引用次数: 0