Drug Delivery最新文献

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Merging konjac glucomannan with other copolymeric hydrogels as a cutting-edge liquid raft system for dual delivery of etoricoxib and famotidine. 将魔芋葡甘露聚糖与其他共聚水凝胶合并,作为一种尖端的液体筏系统,用于双重递送依托昔布和法莫替丁。
IF 6.5 2区 医学
Drug Delivery Pub Date : 2023-12-01 DOI: 10.1080/10717544.2023.2189630
Nabil A Shoman, Marwa Saady, Mahmoud Teaima, Rehab Abdelmonem, Mohamed A El-Nabarawi, Sammar Fathy Elhabal
{"title":"Merging konjac glucomannan with other copolymeric hydrogels as a cutting-edge liquid raft system for dual delivery of etoricoxib and famotidine.","authors":"Nabil A Shoman, Marwa Saady, Mahmoud Teaima, Rehab Abdelmonem, Mohamed A El-Nabarawi, Sammar Fathy Elhabal","doi":"10.1080/10717544.2023.2189630","DOIUrl":"10.1080/10717544.2023.2189630","url":null,"abstract":"<p><p>This study aimed to formulate and evaluate a floating raft system for the co-delivery of etoricoxib (ETO) and famotidine (FAM) using a combination of glucomannan with natural/semi-synthetic polysaccharides. Formulation variables affect gelation lag time (GLT), floating lag time (FLT), and release percentage of drugs after 1-8 h, Stability, and viscosity parameters were evaluated. In vivo X-ray studies, followed by the pharmacokinetic study, were performed on human volunteers. Formulations exhibited pseudoplastic behavior for ease of swallowing. The optimum raft system (ORS) comprised 1% Na alginate, 0.1% Low Methoxyl (LM) pectin, 0.8% Konjac glucomannan (KGL), 1% Precirol, and 1% CaCO<sub>3</sub>. ORS exhibited rapid GLT and FLT (around 42 and 8 sec respectively) in 0.1 N HCl as well as controlled release of ETO (15% in 1 h and 82% in 8 h) and FAM (29% in 1 h and 85% in 8 h). Formulation stability with the absence of any drug-excipient interactions was observed. The X-ray imaging showed a promising buoyancy ability for approximately 8 h. Compared with marketed products, ORS showed superior relative bioavailability for both drugs. These findings revealed the successful preparation of a promising raft system with improved dual drug delivery.</p>","PeriodicalId":11679,"journal":{"name":"Drug Delivery","volume":"30 1","pages":"2189630"},"PeriodicalIF":6.5,"publicationDate":"2023-12-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC10184610/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"9527845","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":2,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Spray-dried nanocrystal-loaded polymer microparticles for long-term release local therapies: an opportunity for poorly soluble drugs. 喷雾干燥纳米晶体负载聚合物微粒长期释放局部治疗:一个机会,难溶性药物。
IF 6 2区 医学
Drug Delivery Pub Date : 2023-12-01 Epub Date: 2023-11-22 DOI: 10.1080/10717544.2023.2284683
Carlos Rodríguez-Nogales, Joke Meeus, Gaby Thonus, Sam Corveleyn, Eric Allémann, Olivier Jordan
{"title":"Spray-dried nanocrystal-loaded polymer microparticles for long-term release local therapies: an opportunity for poorly soluble drugs.","authors":"Carlos Rodríguez-Nogales, Joke Meeus, Gaby Thonus, Sam Corveleyn, Eric Allémann, Olivier Jordan","doi":"10.1080/10717544.2023.2284683","DOIUrl":"10.1080/10717544.2023.2284683","url":null,"abstract":"<p><p>Nano- and micro-technologies can salvage drugs with very low solubility that were doomed to pre-clinical and clinical failure. A unique design approach to develop drug nanocrystals (NCs) loaded in extended release polymeric microparticles (MPs) for local treatments is presented here through the case of a potential osteoarthritis (OA) drug candidate for intra-articular (IA) administration. Optimizing a low-shear wet milling process allowed the production of NCs that can be subsequently freeze-dried (FD) and redispersed in a hydrophobic polymer-organic solvent solution to form spray-dried MPs. Results demonstrated a successful development of a ready-to-upscale formulation containing PLGA MPs with high drug NC encapsulation rates that showed a continuous and controlled drug release profile over four months. The screenings and procedures described allowed for identifying and overcoming common difficulties and challenges raised along the drug reduction to nano-size and spray-drying process. Above all, the technical knowledge acquired is intended for formulation scientists aiming to improve the therapeutic perspectives of poorly soluble drugs.</p>","PeriodicalId":11679,"journal":{"name":"Drug Delivery","volume":"30 1","pages":"2284683"},"PeriodicalIF":6.0,"publicationDate":"2023-12-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC10987046/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"138294946","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":2,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
The direct transfer approach for transcellular drug delivery. 跨细胞药物传递的直接转移方法。
IF 6 2区 医学
Drug Delivery Pub Date : 2023-12-01 Epub Date: 2023-11-30 DOI: 10.1080/10717544.2023.2288799
Yi-Fan Wang, Ze-Fan Shen, Fang-Yue Xiang, Heng Wang, Pu Zhang, Qi Zhang
{"title":"The direct transfer approach for transcellular drug delivery.","authors":"Yi-Fan Wang, Ze-Fan Shen, Fang-Yue Xiang, Heng Wang, Pu Zhang, Qi Zhang","doi":"10.1080/10717544.2023.2288799","DOIUrl":"10.1080/10717544.2023.2288799","url":null,"abstract":"<p><p>A promising paradigm for drug administration that has garnered increasing attention in recent years is the direct transfer (DT) of nanoparticles for transcellular drug delivery. DT requires direct cell-cell contact and facilitates unidirectional and bidirectional matter exchange between neighboring cells. Consequently, DT enables fast and deep penetration of drugs into the targeted tissues. This comprehensive review discusses the direct transfer concept, which can be delineated into the following three distinct modalities: membrane contact-direct transfer, gap junction-mediated direct transfer (GJ-DT), and tunneling nanotubes-mediated direct transfer (TNTs-DT). Further, the intercellular structures for each modality of direct transfer and their respective merits and demerits are summarized. The review also discusses the recent progress on the drugs or drug delivery systems that could activate DT.</p>","PeriodicalId":11679,"journal":{"name":"Drug Delivery","volume":"30 1","pages":"2288799"},"PeriodicalIF":6.0,"publicationDate":"2023-12-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC10987047/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"138458594","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":2,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
A comprehensive review on recent nanosystems for enhancing antifungal activity of fenticonazole nitrate from different routes of administration. 综述了近年来不同给药途径纳米系统增强硝酸非替康唑抗真菌活性的研究进展。
IF 6.5 2区 医学
Drug Delivery Pub Date : 2023-12-01 DOI: 10.1080/10717544.2023.2179129
Sadek Ahmed, Maha M Amin, Sinar Sayed
{"title":"A comprehensive review on recent nanosystems for enhancing antifungal activity of fenticonazole nitrate from different routes of administration.","authors":"Sadek Ahmed, Maha M Amin, Sinar Sayed","doi":"10.1080/10717544.2023.2179129","DOIUrl":"10.1080/10717544.2023.2179129","url":null,"abstract":"<p><p>This review aims to comprehensively highlight the recent nanosystems enclosing Fenticonazole nitrate (FTN) and to compare between them regarding preparation techniques, studied factors and responses. Moreover, the optimum formulae were compared in terms of <i>in vitro, ex vivo</i> and <i>in vivo</i> studies in order to detect the best formula. FTN is a potent antifungal imidazole compound that had been used for treatment of many dangerous fungal infections affecting eye, skin or vagina. FTN had been incorporated in various innovative nanosystems in the recent years in order to achieve significant recovery such as olaminosomes, novasomes, cerosomes, terpesomes and trans-novasomes. These nanosystems were formulated by various techniques (ethanol injection or thin film hydration) utilizing different statistical designs (Box-Behnken, central composite, full factorial and D-optimal). Different factors were studied in each nanosystem regarding its composition as surfactant concentrations, surfactant type, amount of oleic acid, cholesterol, oleylamine, ceramide, sodium deoxycholate, terpene concentration and ethanol concentration. Numerous responses were studied such as percent entrapment efficiency (EE%), particle size (PS), poly-dispersity index (PDI), zeta potential (ZP), and <i>in vitro</i> drug release. Selection of the optimum formula was based on numerical optimization accomplished by Design-Expert® software taking in consideration the largest EE %, ZP (as absolute value) and <i>in vitro</i> drug release and lowest PS and PDI. <i>In vitro</i> comparisons were done employing different techniques such as Transmission electron microscopy, pH determination, effect of gamma sterilization, elasticity evaluation and docking study. In addition to, <i>ex vivo</i> permeation, <i>in vivo</i> irritancy test, histopathological, antifungal activity and Kinetic study.</p>","PeriodicalId":11679,"journal":{"name":"Drug Delivery","volume":"30 1","pages":"2179129"},"PeriodicalIF":6.5,"publicationDate":"2023-12-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9930819/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"9302772","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":2,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Kartogenin delivery systems for biomedical therapeutics and regenerative medicine. 用于生物医学治疗和再生医学的Kartogenin递送系统。
IF 6.5 2区 医学
Drug Delivery Pub Date : 2023-12-01 DOI: 10.1080/10717544.2023.2254519
Peixing Chen, Xiaoling Liao
{"title":"Kartogenin delivery systems for biomedical therapeutics and regenerative medicine.","authors":"Peixing Chen, Xiaoling Liao","doi":"10.1080/10717544.2023.2254519","DOIUrl":"10.1080/10717544.2023.2254519","url":null,"abstract":"<p><p>Kartogenin, a small and heterocyclic molecule, has emerged as a promising therapeutic agent for incorporation into biomaterials, owing to its unique physicochemical and biological properties. It holds potential for the regeneration of cartilage-related tissues in various common conditions and injuries. Achieving sustained release of kartogenin through appropriate formulation and efficient delivery systems is crucial for modulating cell behavior and tissue function. This review provides an overview of cutting-edge kartogenin-functionalized biomaterials, with a primarily focus on their design, structure, functions, and applications in regenerative medicine. Initially, we discuss the physicochemical properties and biological functions of kartogenin, summarizing the underlying molecular mechanisms. Subsequently, we delve into recent advancements in nanoscale and macroscopic materials for the carriage and delivery of kartogenin. Lastly, we address the opportunities and challenges presented by current biomaterial developments and explore the prospects for their application in tissue regeneration. We aim to enhance the generation of insightful ideas for the development of kartogenin delivery materials in the field of biomedical therapeutics and regenerative medicine by providing a comprehensive understanding of common preparation methods.</p>","PeriodicalId":11679,"journal":{"name":"Drug Delivery","volume":"30 1","pages":"2254519"},"PeriodicalIF":6.5,"publicationDate":"2023-12-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://ftp.ncbi.nlm.nih.gov/pub/pmc/oa_pdf/cb/e4/IDRD_30_2254519.PMC10478613.pdf","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"10171189","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":2,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Stability of polymeric cationic niosomes and their plasmid DNA-based complexes as gene delivery carriers. 作为基因递送载体的聚合物阳离子阴离子体及其基于质粒DNA的复合物的稳定性。
IF 6.5 2区 医学
Drug Delivery Pub Date : 2023-12-01 DOI: 10.1080/10717544.2023.2219420
Mohamed Mashal, Noha Attia, Santiago Grijalvo, Ramón Eritja, Gustavo Puras, José Luis Pedraz
{"title":"Stability of polymeric cationic niosomes and their plasmid DNA-based complexes as gene delivery carriers.","authors":"Mohamed Mashal, Noha Attia, Santiago Grijalvo, Ramón Eritja, Gustavo Puras, José Luis Pedraz","doi":"10.1080/10717544.2023.2219420","DOIUrl":"10.1080/10717544.2023.2219420","url":null,"abstract":"<p><p>This study aims to explore the stability of lipo-polymeric niosomes/niosome-based pCMS-EGFP complexes under different storage temperatures (25 °C, 4 °C, and -20 °C). To date, the question of nucleic acid-complex stability is one of the most vital issues in gene delivery applications. The need for stable vaccines during the COVID-19 pandemic has merely highlighted it. In the case of niosomes as gene carriers, the scientific literature still lacks comprehensive stability studies. In this study, the physicochemical features of niosomes/nioplexes in terms of size, surface charge, and polydispersity index (PDI), along with transfection efficiency, and cytotoxicity in NT2 cells were evaluated for 8 weeks. Compared to day 0, the physicochemical features of the niosomes stored at 25 °C and -20 °C changed dramatically in terms of size, zeta potential, and PDI, while remaining in reasonable values when stored at 4 °C. However, niosomes and nioplexes stored at 4 °C and -20 °C showed nearly stable transfection efficiency values, yet an obvious decrease at 25 °C. This article provides a proof of concept into the stability of polymeric cationic niosomes and their nioplexes as promising gene delivery vehicles. Moreover, it highlights the practical possibility of storing nioplexes at 4 °C for up to 2 months, as an alternative to niosomes, for gene delivery purposes.</p>","PeriodicalId":11679,"journal":{"name":"Drug Delivery","volume":"30 1","pages":"2219420"},"PeriodicalIF":6.5,"publicationDate":"2023-12-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC10281300/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"9710986","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":2,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Platinum-based drugs and hydrogel: a promising anti-tumor combination. 铂类药物和水凝胶:一种前景广阔的抗肿瘤组合。
IF 6 2区 医学
Drug Delivery Pub Date : 2023-12-01 Epub Date: 2023-12-11 DOI: 10.1080/10717544.2023.2287966
Jiamin Yao, Shaojuan Song, Hang Zhao, Yao Yuan
{"title":"Platinum-based drugs and hydrogel: a promising anti-tumor combination.","authors":"Jiamin Yao, Shaojuan Song, Hang Zhao, Yao Yuan","doi":"10.1080/10717544.2023.2287966","DOIUrl":"10.1080/10717544.2023.2287966","url":null,"abstract":"<p><p>Platinum-based drugs are widely used as first-line anti-tumor chemotherapy agents. However, they also have nonnegligible side effects due to the free drugs in circulation. Therefore, it is necessary to develop efficient and safe delivery systems for better tumor cell targeting. Hydrogel is a promising anti-tumor drug carrier that can form a platinum/hydrogel combination system for drug release, which has shown better anti-tumor effects in some studies. However, there is a lack of systematic summary in this field. This review aims to provide a comprehensive overview of the platinum/hydrogel combination system with the following sections: firstly, an introduction of platinum-based drugs; secondly, an analysis of the platinum/hydrogel combination system; and thirdly, a discussion of the advantages of the hydrogel-based delivery system. We hope this review can offer some insights for the development of the platinum/hydrogel combination system for better cancer therapy.</p>","PeriodicalId":11679,"journal":{"name":"Drug Delivery","volume":"30 1","pages":"2287966"},"PeriodicalIF":6.0,"publicationDate":"2023-12-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC10987050/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"138797294","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":2,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
An update on the advances in the field of nanostructured drug delivery systems for a variety of orthopedic applications. 纳米结构药物输送系统在各种骨科应用领域的最新进展。
IF 6 2区 医学
Drug Delivery Pub Date : 2023-12-01 DOI: 10.1080/10717544.2023.2241667
Wenqing Liang, Chao Zhou, Songtao Jin, Lifeng Fu, Hengjian Zhang, Xiaogang Huang, Hengguo Long, Wenyi Ming, Jiayi Zhao
{"title":"An update on the advances in the field of nanostructured drug delivery systems for a variety of orthopedic applications.","authors":"Wenqing Liang, Chao Zhou, Songtao Jin, Lifeng Fu, Hengjian Zhang, Xiaogang Huang, Hengguo Long, Wenyi Ming, Jiayi Zhao","doi":"10.1080/10717544.2023.2241667","DOIUrl":"10.1080/10717544.2023.2241667","url":null,"abstract":"<p><p>Nanotechnology has made significant progress in various fields, including medicine, in recent times. The application of nanotechnology in drug delivery has sparked a lot of research interest, especially due to its potential to revolutionize the field. Researchers have been working on developing nanomaterials with distinctive characteristics that can be utilized in the improvement of drug delivery systems (DDS) for the local, targeted, and sustained release of drugs. This approach has shown great potential in managing diseases more effectively with reduced toxicity. In the medical field of orthopedics, the use of nanotechnology is also being explored, and there is extensive research being conducted to determine its potential benefits in treatment, diagnostics, and research. Specifically, nanophase drug delivery is a promising technique that has demonstrated the capability of delivering medications on a nanoscale for various orthopedic applications. In this article, we will explore current advancements in the area of nanostructured DDS for orthopedic use.</p>","PeriodicalId":11679,"journal":{"name":"Drug Delivery","volume":"30 1","pages":"2241667"},"PeriodicalIF":6.0,"publicationDate":"2023-12-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC10987052/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"138458593","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":2,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Quantitative analysis of therapeutic proteins in biological fluids: recent advancement in analytical techniques. 生物体液中治疗性蛋白的定量分析:分析技术的最新进展。
IF 6.5 2区 医学
Drug Delivery Pub Date : 2023-12-01 DOI: 10.1080/10717544.2023.2183816
Jae Geun Song, Kshitis Chandra Baral, Gyu-Lin Kim, Ji-Won Park, Soo-Hwa Seo, Da-Hyun Kim, Dong Hoon Jung, Nonye Linda Ifekpolugo, Hyo-Kyung Han
{"title":"Quantitative analysis of therapeutic proteins in biological fluids: recent advancement in analytical techniques.","authors":"Jae Geun Song, Kshitis Chandra Baral, Gyu-Lin Kim, Ji-Won Park, Soo-Hwa Seo, Da-Hyun Kim, Dong Hoon Jung, Nonye Linda Ifekpolugo, Hyo-Kyung Han","doi":"10.1080/10717544.2023.2183816","DOIUrl":"10.1080/10717544.2023.2183816","url":null,"abstract":"<p><p>Pharmaceutical application of therapeutic proteins has been continuously expanded for the treatment of various diseases. Efficient and reliable bioanalytical methods are essential to expedite the identification and successful clinical development of therapeutic proteins. In particular, selective quantitative assays in a high-throughput format are critical for the pharmacokinetic and pharmacodynamic evaluation of protein drugs and to meet the regulatory requirements for new drug approval. However, the inherent complexity of proteins and many interfering substances presented in biological matrices have a great impact on the specificity, sensitivity, accuracy, and robustness of analytical assays, thereby hindering the quantification of proteins. To overcome these issues, various protein assays and sample preparation methods are currently available in a medium- or high-throughput format. While there is no standard or universal approach suitable for all circumstances, a liquid chromatography-tandem mass spectrometry (LC-MS/MS) assay often becomes a method of choice for the identification and quantitative analysis of therapeutic proteins in complex biological samples, owing to its high sensitivity, specificity, and throughput. Accordingly, its application as an essential analytical tool is continuously expanded in pharmaceutical R&D processes. Proper sample preparation is also important since clean samples can minimize the interference from co-existing substances and improve the specificity and sensitivity of LC-MS/MS assays. A combination of different methods can be utilized to improve bioanalytical performance and ensure more accurate quantification. This review provides an overview of various protein assays and sample preparation methods, with particular emphasis on quantitative protein analysis by LC-MS/MS.</p>","PeriodicalId":11679,"journal":{"name":"Drug Delivery","volume":"30 1","pages":"2183816"},"PeriodicalIF":6.5,"publicationDate":"2023-12-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC10003146/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"9442237","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":2,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Andrographolide nanophytosomes exhibit enhanced cellular delivery and pro-apoptotic activities in HepG2 liver cancer cells. 穿心莲内酯纳米植物体在HepG2肝癌癌症细胞中表现出增强的细胞递送和促凋亡活性。
IF 6.5 2区 医学
Drug Delivery Pub Date : 2023-12-01 DOI: 10.1080/10717544.2023.2174209
Thikryat Neamatallah, Azizah M Malebari, Abdulmohsin J Alamoudi, Syed Nazreen, Mohammad Mahboob Alam, Hawazen H Bin-Melaih, Osama A Abuzinadah, Shaimaa M Badr-Eldin, Gharam Alhassani, Lamar Makki, Mohammed Z Nasrullah
{"title":"Andrographolide nanophytosomes exhibit enhanced cellular delivery and pro-apoptotic activities in HepG2 liver cancer cells.","authors":"Thikryat Neamatallah, Azizah M Malebari, Abdulmohsin J Alamoudi, Syed Nazreen, Mohammad Mahboob Alam, Hawazen H Bin-Melaih, Osama A Abuzinadah, Shaimaa M Badr-Eldin, Gharam Alhassani, Lamar Makki, Mohammed Z Nasrullah","doi":"10.1080/10717544.2023.2174209","DOIUrl":"10.1080/10717544.2023.2174209","url":null,"abstract":"<p><p>Andrographolide (AG), a major active constituent of <i>Andrographis paniculata,</i> is known to hinder proliferation of several types of cancer cells. However, its poor solubility and cellular permeability restrict its use in clinical applications. In this study, AG-loaded phytosomes (AG-PTMs) were formulated and optimized with respect to particle size using l-α-phosphatidylcholine (PC):AG ratio and sonication time (ST) as independent variables. The optimized formula was prepared at 1:2.7 for AG:PC molar ratio and 4.9 min for ST and exhibited a particle size of 243.7 ± 7.3 nm, polydispersity index (PDI) of 0.310 and entrapment efficiency of 72.20 ± 4.53. Also, the prepared formula showed a slow release of AG over 24-h period. The antiproliferative activity of AG-PTMs was investigated against the liver cancer cell line HepG2. AG-PTMs significantly repressed the growth of HepG2 cells with an IC<sub>50</sub> value of 4.02 ± 0.14 µM. AG uptake by HepG2 cells was significantly enhanced in incubations containing the optimized formula. AG-PTMs also caused G2-M cell cycle phase arrest and increased the fraction of apoptotic cells in pre-G1 phase. These effects were associated with induction of oxidative stress and mitochondrial dysfunction. In addition, AG-PTMs significantly upregulated mRNA expression of <i>BAX</i> and downregulated that of <i>BCL2.</i> Furthermore, AG-PTMs significantly enhanced the concentration of caspase-3 in comparison to raw AG. These data indicate that the phytosomal delivery of AG significantly inhibited HepG2 cell proliferation through enhanced cellular uptake, arresting cell cycle at the G2-M phase and inducing mitochondrial-dependent apoptosis.</p>","PeriodicalId":11679,"journal":{"name":"Drug Delivery","volume":"30 1","pages":"2174209"},"PeriodicalIF":6.5,"publicationDate":"2023-12-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9930834/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"10733957","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":2,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
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