Hongshuai Lv, Weiping Jia, Peng Dong, Jiaojiao Liu, Si Wang, Xiaohai Li, Jinghua Hu, Ling Zhao, Yikang Shi
{"title":"Improved Antitumor Efficacy of a Dextran-based Docetaxel-coupled Conjugate against Triple-Negative Breast Cancer.","authors":"Hongshuai Lv, Weiping Jia, Peng Dong, Jiaojiao Liu, Si Wang, Xiaohai Li, Jinghua Hu, Ling Zhao, Yikang Shi","doi":"10.2174/1567201820666230622105503","DOIUrl":"10.2174/1567201820666230622105503","url":null,"abstract":"<p><strong>Background: </strong>Most chemotherapeutic agents are characterized by poor water solubility and non-specific distribution. Polymer-based conjugates are promising strategies for overcoming these limitations.</p><p><strong>Objective: </strong>This study aims to fabricate a polysaccharide, dextran-based, dual-drug conjugate by covalently grafting docetaxel (DTX) and docosahexaenoic acid (DHA) onto the bifunctionalized dextran through a long linker, and to investigate the antitumor efficacy of this conjugate against breast cancer.</p><p><strong>Methods: </strong>DTX was firstly coupled with DHA and covalently bounded with the bifunctionalized dextran (100 kDa) through a long linker to produce a conjugate dextran-DHA-DTX (termed C-DDD). Cytotoxicity and cellular uptake of this conjugate were measured <i>in vitro</i>. Drug biodistribution and pharmacokinetics were investigated through liquid chromatography/mass spectrometry analysis. The inhibitory effects on tumor growth were evaluated in MCF-7- and 4T1-tumor-bearing mice.</p><p><strong>Results: </strong>The loading capacity of the C-DDD for DTX was 15.90 (weight/weight). The C-DDD possessed good water solubility and was able to self-assemble into nanoparticles measuring 76.8 ± 5.5 nm. The maximum plasma concentration and area under the curve (0-∞) for the released DTX and total DTX from the C-DDD were significantly enhanced compared with the conventional DTX formulation. The C-DDD selectively accumulated in the tumor, with limited distribution was observed in normal tissues. The C-DDD exhibited greater antitumor activity than the conventional DTX in the triplenegative breast cancer model. Furthermore, the C-DDD nearly eliminated all MCF-7 tumors in nude mice without leading to systemic adverse effects.</p><p><strong>Conclusion: </strong>This dual-drug C-DDD has the potential to become a candidate for clinical application through the optimization of the linker.</p>","PeriodicalId":10842,"journal":{"name":"Current drug delivery","volume":" ","pages":"775-784"},"PeriodicalIF":2.4,"publicationDate":"2024-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"10050822","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}
Yachana Mishra, Vijay Mishra, Alaa A A Aljabali, Mohamed El-Tanani, Gowhar A Naikoo, Nitin Charbe, Sai Raghuveer Chava, Murtaza M Tambuwala
{"title":"3D Printed Personalized Colon-targeted Tablets: A Novel Approach in Ulcerative Colitis Management.","authors":"Yachana Mishra, Vijay Mishra, Alaa A A Aljabali, Mohamed El-Tanani, Gowhar A Naikoo, Nitin Charbe, Sai Raghuveer Chava, Murtaza M Tambuwala","doi":"10.2174/1567201821666230915150544","DOIUrl":"10.2174/1567201821666230915150544","url":null,"abstract":"<p><p>Ulcerative colitis (UC) and Crohn's disease (CD) are two types of idiopathic inflammatory bowel disease (IBD) that are increasing in frequency and incidence worldwide, particularly in highly industrialized countries. Conventional tablets struggle to effectively deliver anti-inflammatory drugs since the inflammation is localized in different areas of the colon in each patient. The goal of 3D printing technology in pharmaceutics is to create personalized drug delivery systems (DDS) that are tailored to each individual's specific needs. This review provides an overview of existing 3D printing processes, with a focus on extrusion-based technologies, which have received the most attention. Personalized pharmaceutical products offer numerous benefits to patients worldwide, and 3D printing technology is becoming more affordable every day. Custom manufacturing of 3D printed tablets provides innovative ideas for developing a tailored colon DDS. In the future, 3D printing could be used to manufacture personalized tablets for UC patients based on the location of inflammation in the colon, resulting in improved therapeutic outcomes and a better quality of life.</p>","PeriodicalId":10842,"journal":{"name":"Current drug delivery","volume":" ","pages":"1211-1225"},"PeriodicalIF":2.8,"publicationDate":"2024-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"10634609","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}
{"title":"Engineered Exosomes for Drug Delivery in Cancer Therapy: A Promising Approach and Application.","authors":"Peiwen Fu, Siqi Yin, Huiying Cheng, Wenrong Xu, Jiajia Jiang","doi":"10.2174/1567201820666230712103942","DOIUrl":"10.2174/1567201820666230712103942","url":null,"abstract":"<p><p>A significant amount of research effort is currently focused on investigating the role of exosomes in various cancers. These tiny vesicles, apart from acting as biomarkers, also play a crucial role in tumor formation and development. Several studies have demonstrated that exosomes can be a drug delivery vehicle for cancer therapy. In this paper, we highlight the key advantages of exosomes as a drug delivery candidate, with a particular focus on their low immunogenicity, natural targeting ability and suitable mechanical properties. Furthermore, we propose that the selection of appropriate exosomes and drug loading methods based on therapeutic goals and product heterogeneity is essential for preparing engineered exosomes. We comprehensively analyzed the superiorities of current drug-loading methods to improve the creation of designed exosomes. Moreover, we systematically review the applications of engineered exosomes in various therapies such as immunotherapy, gene therapy, protein therapy, chemotherapy, indicating that engineered exosomes have the potential to be reliable and, safe drug carriers that can address the unmet needs in cancer clinical practice.</p>","PeriodicalId":10842,"journal":{"name":"Current drug delivery","volume":" ","pages":"817-827"},"PeriodicalIF":2.4,"publicationDate":"2024-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"10150216","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}
Neslihan Üstündağ Okur, Emre Şefik Çağlar, Mustafa Sinan Kaynak, Mine Diril, Saniye Özcan, Hatice Yeşim Karasulu
{"title":"Enhancing Oral Bioavailability of Domperidone Maleate: Formulation, <i>In vitro</i> Permeability Evaluation In-caco-2 Cell Monolayers and <i>In situ</i> Rat Intestinal Permeability Studies.","authors":"Neslihan Üstündağ Okur, Emre Şefik Çağlar, Mustafa Sinan Kaynak, Mine Diril, Saniye Özcan, Hatice Yeşim Karasulu","doi":"10.2174/1567201820666230214091509","DOIUrl":"10.2174/1567201820666230214091509","url":null,"abstract":"<p><strong>Background: </strong>The domperidone maleate, a lipophilic agent classified as a Biopharmaceutical Classification System Class II substance with weak water solubility. Self- Emulsifying Drug Delivery System is a novel approach to improve water solubility and, ultimately bioavailability of drugs.</p><p><strong>Objective: </strong>This study aimed to develop and characterize new domperidone-loaded self-emulsifying drug delivery systems as an alternative formulation and to evaluate the permeability of domperidone-loaded self-emulsifying drug delivery systems by using Caco-2 cells and <i>via</i> single-pass intestinal perfusion method.</p><p><strong>Methods: </strong>Three self-emulsifying drug delivery systems were prepared and characterized in terms of pH, viscosity, droplet size, zeta potential, polydispersity index, conductivity, <i>etc</i>. Each formulation underwent 10, 100, 200, and 500 times dilution in intestinal buffer pH 6.8 and stomach buffer pH 1.2, respectively. Female Sprague Dawley rats were employed for <i>in situ</i> single-pass intestinal perfusion investigations.</p><p><strong>Results: </strong>Results of the study revealed that the ideal self-emulsifying drug delivery systems formulation showed narrow droplet size, ideal zeta potential, and no conductivity. Additionally, as compared to the control groups, the optimum formulation had better apparent permeability (12.74 ± 0.02×10-4) from Caco-2 cell monolayer permeability experiments. The study also revealed greater Peff values (2.122 ± 0.892×10-4 cm/s) for the optimal formulation from <i>in situ</i> intestinal perfusion analyses in comparison to control groups (Domperidone; 0.802 ± 0.418×10-4 cm/s).</p><p><strong>Conclusion: </strong>To conclude, prepared formulations can be a promising way of oral administration of Biopharmaceutical Classification System Class II drugs.</p>","PeriodicalId":10842,"journal":{"name":"Current drug delivery","volume":" ","pages":"1010-1023"},"PeriodicalIF":2.4,"publicationDate":"2024-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC11092562/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"10767561","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Na Yang, Xinyi Ai, Kang Cheng, Yihan Wu, Zhi Lu, Zhenda Liu, Teng Guo, Nianping Feng
{"title":"A Compound Essential Oil Alters Stratum Corneum Structure, Potentially Promoting the Transdermal Permeation of Hydrophobic and Hydrophilic Ingredients.","authors":"Na Yang, Xinyi Ai, Kang Cheng, Yihan Wu, Zhi Lu, Zhenda Liu, Teng Guo, Nianping Feng","doi":"10.2174/1567201820666230120122206","DOIUrl":"10.2174/1567201820666230120122206","url":null,"abstract":"<p><strong>Background: </strong>The stratum corneum (SC) is the main barrier of the skin, and cosmeceuticals are different from ordinary cosmetics in that they need to deliver active ingredients targeting specific skin problems through the SC into the deeper layers of the skin. Thus, we designed a compound essential oil (CEO) extracted from <i>Salvia miltiorrhiza</i> Bge and <i>Cinnamomum cassia</i> Presl, supplemented with borneol to deliver active ingredients through the SC.</p><p><strong>Methods: </strong>The CEO was prepared by flash extraction combined with the microwave method. Moreover, the main components of the CEO were determined using gas chromatography-mass spectrometry (GCMS). Visualization techniques, such as scanning electron microscopy (SEM), haematoxylin-eosin (HE) staining, and confocal laser scanning microscopy (CLSM), were used to study the permeationpromoting mechanism of the CEO on the skin. Furthermore, the permeation-promoting effects of the CEO on both hydrophobic and hydrophilic ingredients were tested <i>via in vitro</i> skin penetration experiments and <i>in vivo</i> microdialysis experiments.</p><p><strong>Results: </strong>The results indicated the ability of the CEO to alter the structure of the SC, leading to enhanced transdermal permeation of hydrophobic and hydrophilic ingredients. The 1.5% CEO group demonstrated the best permeation-promoting effect compared to the other CEO groups and blank groups (P<0.05). Furthermore, the CEO displayed an expedited permeability-promoting effect on hydrophobic ingredients compared to hydrophilic ingredients.</p><p><strong>Conclusion: </strong>It is concluded that the prepared CEO can promote the transdermal permeation of hydrophobic and hydrophilic ingredients. This study will provide a reference for the application of the prepared CEO in the development of cosmeceuticals with natural efficacy.</p>","PeriodicalId":10842,"journal":{"name":"Current drug delivery","volume":" ","pages":"744-752"},"PeriodicalIF":2.4,"publicationDate":"2024-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"9126742","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}
Hong Shu, Wenhao Lv, Zhi-Jian Ren, Hui Li, Tiantian Dong, Yao Zhang, Fang Nie
{"title":"Ultrasound-mediated PLGA-PEI Nanobubbles Carrying STAT6 SiRNA Enhances NSCLC Treatment <i>via</i> Repolarizing Tumor-associated Macrophages from M2 to M1 Phenotypes.","authors":"Hong Shu, Wenhao Lv, Zhi-Jian Ren, Hui Li, Tiantian Dong, Yao Zhang, Fang Nie","doi":"10.2174/1567201820666230724151545","DOIUrl":"10.2174/1567201820666230724151545","url":null,"abstract":"<p><strong>Background: </strong>Tumor-associated macrophages (TAMs) are crucial for non-small cell lung cancer (NSCLC) development.</p><p><strong>Objective: </strong>In this study, polylactic acid-co-glycolic acid (PLGA)-polyethylenimine (PEI) nanobubbles (NBs) carrying STAT6 siRNA were prepared and combined with ultrasound-mediated nanobubbles destruction (UMND) to silence the STAT6 gene, ultimately repolarizing TAMs from the M2 to the M1 phenotype, treating NSCLC <i>in vitro</i>.</p><p><strong>Methods: </strong>PLGA-PEI NBs-siRNA were prepared and characterised, and their respective ultrasound imaging, biological stabilities and cytotoxicities were detected. Transfection efficiency was evaluated by fluorescence microscopy and flow cytometry. Repolarization of THP-1-derived M2-like macrophages was determined by qPCR and flow cytometry. NSCLC cells (A549) were co-cultured with transfected M2-like macrophages or their associated conditioned medium (CM). Western blotting was used to detect STAT6 gene silencing in M2-like macrophages and markers of epithelial and mesenchymal in A549 cells. The proliferation of A549 cells was detected using CCK-8 and cell colony formation assays. Transwell assays were used to detect the migration and invasion of A549 cells.</p><p><strong>Results: </strong>PLGA-PEI NBs-siRNA had an average size of 223.13 ± 0.92 nm and a zeta potential of about -5.59 ± 0.97 mV. PLGA-PEI NBs showed excellent ultrasonic imaging capability in addition to biological stability to protect siRNA from degradation. UMND enhanced PLGA-PEI NBs-STAT6 siRNA transfection in M2-like macrophages, which made M2-like macrophages repolarize to M1-like macrophages and prevented proliferation, migration, invasion and epithelial-mesenchymal transition (EMT) in A549 cells.</p><p><strong>Conclusion: </strong>UMND enhanced PLGA-PEI NBs-STAT6 siRNA to repolarize TAMs from the M2 to the M1 phenotype, thus treating NSCLC. These findings provide a promising therapeutic approach for enhancing NSCLC immunotherapy.</p>","PeriodicalId":10842,"journal":{"name":"Current drug delivery","volume":" ","pages":"1114-1127"},"PeriodicalIF":2.4,"publicationDate":"2024-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"10247880","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}
{"title":"Role of Artificial Intelligence in Drug Discovery and Target Identification in Cancer.","authors":"Vishal Sharma, Amit Singh, Sanjana Chauhan, Pramod Kumar Sharma, Shubham Chaudhary, Astha Sharma, Omji Porwal, Neeraj Kumar Fuloria","doi":"10.2174/1567201821666230905090621","DOIUrl":"10.2174/1567201821666230905090621","url":null,"abstract":"<p><p>Drug discovery and development (DDD) is a highly complex process that necessitates precise monitoring and extensive data analysis at each stage. Furthermore, the DDD process is both timeconsuming and costly. To tackle these concerns, artificial intelligence (AI) technology can be used, which facilitates rapid and precise analysis of extensive datasets within a limited timeframe. The pathophysiology of cancer disease is complicated and requires extensive research for novel drug discovery and development. The first stage in the process of drug discovery and development involves identifying targets. Cell structure and molecular functioning are complex due to the vast number of molecules that function constantly, performing various roles. Furthermore, scientists are continually discovering novel cellular mechanisms and molecules, expanding the range of potential targets. Accurately identifying the correct target is a crucial step in the preparation of a treatment strategy. Various forms of AI, such as machine learning, neural-based learning, deep learning, and network-based learning, are currently being utilised in applications, online services, and databases. These technologies facilitate the identification and validation of targets, ultimately contributing to the success of projects. This review focuses on the different types and subcategories of AI databases utilised in the field of drug discovery and target identification for cancer.</p>","PeriodicalId":10842,"journal":{"name":"Current drug delivery","volume":" ","pages":"870-886"},"PeriodicalIF":2.4,"publicationDate":"2024-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"10164900","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}
{"title":"Current Landscape of Therapeutics for the Management of Hypertension - A Review.","authors":"Neda Fatima, Sumel Ashique, Aakash Upadhyay, Shubneesh Kumar, Himanshu Kumar, Nitish Kumar, Prashant Kumar","doi":"10.2174/1567201820666230623121433","DOIUrl":"10.2174/1567201820666230623121433","url":null,"abstract":"<p><p>Hypertension is a critical health problem. It is also the primary reason for coronary heart disease, stroke, and renal vascular disease. The use of herbal drugs in the management of any disease is increasing. They are considered the best immune booster to fight against several types of diseases. To date, the demand for herbal drugs has been increasing because of their excellent properties. This review highlights antihypertensive drugs, polyphenols, and synbiotics for managing hypertension. Evidence is mounting in favour of more aggressive blood pressure control with reduced adverse effects, especially for specific patient populations. This review aimed to present contemporary viewpoints and novel treatment options, including cutting-edge technological applications and emerging interventional and pharmaceutical therapies, as well as key concerns arising from several years of research and epidemiological observations related to the management of hypertension.</p>","PeriodicalId":10842,"journal":{"name":"Current drug delivery","volume":" ","pages":"662-682"},"PeriodicalIF":2.4,"publicationDate":"2024-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"10121748","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}
{"title":"Monoclonal Antibodies and Antibody-drug Conjugates as Emerging Therapeutics for Breast Cancer Treatment.","authors":"Swati Saini, Nisha Gulati, Rajendra Awasthi, Vimal Arora, Sachin Kumar Singh, Shobhit Kumar, Gaurav Gupta, Kamal Dua, Rakesh Pahwa, Harish Dureja","doi":"10.2174/1567201820666230731094258","DOIUrl":"10.2174/1567201820666230731094258","url":null,"abstract":"<p><p>When breast cells divide and multiply out of control, it is called breast cancer. Symptoms include lump formation in the breast, a change in the texture or color of the breast, or a discharge from the nipple. Local or systemic therapy is frequently used to treat breast cancer. Surgical and radiation procedures limited to the affected area are examples of local management. There has been significant worldwide progress in the development of monoclonal antibodies (mAbs) since 1986, when the first therapeutic mAb, Orthoclone OKT3, became commercially available. mAbs can resist the expansion of cancer cells by inducing the destruction of cellular membranes, blocking immune system inhibitors, and preventing the formation of new blood vessels. mAbs can also target growth factor receptors. Understanding the molecular pathways involved in tumor growth and its microenvironment is crucial for developing effective targeted cancer therapeutics. Due to their unique properties, mAbs have a wide range of clinical applications. Antibody-drug conjugates (ADCs) are drugs that improve the therapeutic index by combining an antigen-specific antibody with a payload. This review focuses on the therapeutic applications, mechanistic insights, characteristics, safety aspects, and adverse events of mAbs like trastuzumab, bevacizumab, pertuzumab, ertumaxomab, and atezolizumab in breast cancer treatment. The creation of novel technologies utilizing modified antibodies, such as fragments, conjugates, and multi-specific antibodies, must be a central focus of future studies. This review will help scientists working on developing mAbs to treat cancers more effectively.</p>","PeriodicalId":10842,"journal":{"name":"Current drug delivery","volume":" ","pages":"993-1009"},"PeriodicalIF":2.4,"publicationDate":"2024-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"9898276","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}
{"title":"Chitosan Oligosaccharide Modified Bovine Serum Albumin Nanoparticles for Improving Oral Bioavailability of Naringenin.","authors":"Ruiyue Fang, Yiqi Liao, Huishuang Qiu, Yuxin Liu, Shiyuan Lin, Hui Chen","doi":"10.2174/1567201820666230718143726","DOIUrl":"10.2174/1567201820666230718143726","url":null,"abstract":"<p><strong>Introduction: </strong>With the rapid development of nanotechnology, the research and development of nano-drugs have become one of the development directions of drug innovation. The encapsulation of the nanoparticles can change the biological distribution of the drug <i>in vivo</i> and improve the bioavailability of the drug <i> in vivo</i>. Naringenin is poorly soluble in water and has a low bioavailability, thus limiting its clinical application. The main purpose of this study was to develop a nano-sized preparation that could improve the oral bioavailability of naringenin.</p><p><strong>Methods: </strong>Chitosan oligosaccharide modified naringenin-loaded bovine serum albumin nanoparticles (BSA-COS@Nar NPs) were prepared by emulsification solvent evaporation and electrostatic interaction. The nanoparticles were characterized by HPLC, laser particle size analyzer, transmission electron microscope and X-ray diffraction analysis. The release <i>in vitro</i> was investigated, and the behavior of nanoparticles in rats was also studied. The caco-2 cell model was established <i>in vitro</i> to investigate the cytotoxicity and cellular uptake of nanoparticles.</p><p><strong>Results: </strong>BSA-COS@Nar NPs were successfully prepared, and the first-order release model was confirmed <i>in vitro</i> release. <i>In vivo</i> pharmacokinetic results indicated that the area under the drug concentration- time curve (AUC) of BSA-COS@Nar NPs was 2.37 times more than free naringenin. Cytotoxicity and cellular uptake results showed that BSA-COS@Nar NPs had no significant cytotoxic effect on Caco- 2 cells and promoted cellular uptake of the drug.</p><p><strong>Conclusion: </strong>BSA-COS@Nar NPs could improve the <i>in vivo</i> bioavailability of naringenin.</p>","PeriodicalId":10842,"journal":{"name":"Current drug delivery","volume":" ","pages":"1142-1150"},"PeriodicalIF":2.4,"publicationDate":"2024-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"9886818","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}