ADMET and DMPK最新文献_第7页

Antimalarial evaluation of alkyl-linked bis-thiadiazine derivatives in murine model infected with two Plasmodium strains 在感染两种疟原虫菌株的小鼠模型中评估烷基连接双噻二嗪衍生物的抗疟效果

IF 2.5

ADMET and DMPK Pub Date : 2023-11-30 DOI: 10.5599/admet.2105

Katherine Stefania Loachamin Gualotuña, Lilian M. Spencer, Hortensia M. Rodríguez Cabrera, Renata Abigail Montero Calderón, Beatríz Pernía, J. Coro, Margarita Suarez, Francisco Javier Tingo Jacome, Zully J. Rodriguez Parra, Jose Manuel Lozano, Jesús A Cortés Vecino

{"title":"Antimalarial evaluation of alkyl-linked bis-thiadiazine derivatives in murine model infected with two Plasmodium strains","authors":"Katherine Stefania Loachamin Gualotuña, Lilian M. Spencer, Hortensia M. Rodríguez Cabrera, Renata Abigail Montero Calderón, Beatríz Pernía, J. Coro, Margarita Suarez, Francisco Javier Tingo Jacome, Zully J. Rodriguez Parra, Jose Manuel Lozano, Jesús A Cortés Vecino","doi":"10.5599/admet.2105","DOIUrl":"https://doi.org/10.5599/admet.2105","url":null,"abstract":"Background and Purpose: Plasmodium falciparum and P. vivax are responsible for most malaria cases in humans in the African Region and the Americas; these parasites have developed resistance to classic antimalarial drugs. On the other hand, previous investigations of the alkyl-linked bis tetrahydro-(2H)-1,3,5-thiadiazine-2-thione (bis-THTT) derivatives compounds show satisfactory results against protozoan parasites such as Trypanosoma cruzi, Trypanosoma vaginalis, Trypanosoma brucei rhodesiense and Leishmania donovani. Therefore, it is possible to see some effect of bis-THTT derivatives on other protozoan parasites, such as Plasmodium. Experimental Approach: This study aimed to perform an in vivo biological evaluation of bis-THTT (JH1 to JH6) derivatives compounds as possible anti-malaria drugs in BALB/c mice infected with Plasmodium berghei ANKA and Plasmodium yoelii 17XL strains. In this work, we evaluated the compounds as potential antimalarial drugs in BALB/c mice infected with Plasmodium strains. Key Results: For each compound, we assess the percentages of parasitemia by smears from tail blood and the humoral response by indirect ELISA test using each compound as an antigen. We also evaluated the B lymphocyte response and the cytotoxicity of the bis-THTT derivatives compounds with MTT cell proliferation assays. Conclusions: Our results show that the bis-THTT derivatives JH2 and JH4 presented effective parasitemia control in mice infected with P. berghei; JH5 and JH6 compounds have similar infection control results as chloroquine in mice infected P. yoelii strain. The evaluation of bis-THTT derivatives compounds in a model of BALB/c mice infected with P. berghei and P. yoelii allowed us to conclude that some of them have an antimalarial effect; however, none of the tested compounds exceeded the efficiency of chloroquine.","PeriodicalId":7259,"journal":{"name":"ADMET and DMPK","volume":"38 1","pages":""},"PeriodicalIF":2.5,"publicationDate":"2023-11-30","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"139199219","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0

Pharmacokinetics evaluation of newly formulated beads alginate/gum acacia loaded ketoconazole in rabbit plasma by oral administration 口服新配制的海藻酸珠/刺槐胶负载酮康唑在兔血浆中的药代动力学评价

IF 2.5

ADMET and DMPK Pub Date : 2023-11-30 DOI: 10.5599/admet.2042

Viviane Annisa, T. Sulai̇man, A. Nugroho, A. Nugroho

{"title":"Pharmacokinetics evaluation of newly formulated beads alginate/gum acacia loaded ketoconazole in rabbit plasma by oral administration","authors":"Viviane Annisa, T. Sulai̇man, A. Nugroho, A. Nugroho","doi":"10.5599/admet.2042","DOIUrl":"https://doi.org/10.5599/admet.2042","url":null,"abstract":"Background and purporse: The combination of alginate and gum acacia in previous studies showed good results in inhibiting ketoconazole precipitation due to the supersaturation phenomenon. Ketoconazole-loaded alginate and gum acacia can produce hydrogel beads through cross-linking with Ca2+ using ionotropic gelation techniques. However, the pharmacokinetic study of the ketoconazole beads loaded to alginate and gum acacia needs further investigation. This study aimed to evaluate pharmacokinetic parameters using rabbits via oral administration. Experimental approach: The drug was administered orally to 2 groups of rabbits: pure ketoconazole (KTZ) and formulation of ketoconazole (AG75) groups. Blood samples were obtained from the ear marginal vein at various time points: 0 (before administration), 15, 30, 45, 60, 90, 120, 150, 180, 240, 300, 360, and 420 minutes after oral dosage. The pharmacokinetic study employed a non-compartment analysis to calculate the area under the curve (AUC), the volume of distribution (Vd F-1), clearance (Cl F-1), maximum concentration (Cmax), and time to reach maximum concentration (tmax). The data obtained from the parameter result was analyzed using the independent-sample T-test. Key result: The results of the KTZ group include AUC of 15.83±0.62 h µg mL-1, VdF-1 of 8.95±1.17 mL, ClF-1 of 3.45±0.3 mL h-1, Cmax of 4.7±0.69 µg mL-1, and tmax of 1.67±0.17 h. The results of the AG75 group include AUC of 27.8±1.01 h µg mL-1, VdF-1 of 11.5±2.4 mL, ClF-1 of 2.15±0.11 mL h-1, Cmax of 4.49±0.52 µg mL-1, and tmax of 2.5±0.5 h. Conclusion: The formulation incorporating ketoconazole beads resulted in a higher AUC0-∞ than the pure ketoconazole. This finding suggests that the created formulation has enhanced the bioavailability of ketoconazole.","PeriodicalId":7259,"journal":{"name":"ADMET and DMPK","volume":"451 ","pages":""},"PeriodicalIF":2.5,"publicationDate":"2023-11-30","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"139203189","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0

Enhancing encapsulation of filarial antigen Brugia malayi thioredoxin in nano-liposomes: The role of lecithin composition 提高丝虫抗原 Brugia malayi 硫氧还蛋白在纳米脂质体中的包裹性：卵磷脂成分的作用

IF 2.5

ADMET and DMPK Pub Date : 2023-11-30 DOI: 10.5599/admet.2089

Malathi Balasubramaniyan, V. Vinayagam, Moni Philip Jacob Kizhakedathil, Kaliraj Perumal

{"title":"Enhancing encapsulation of filarial antigen Brugia malayi thioredoxin in nano-liposomes: The role of lecithin composition","authors":"Malathi Balasubramaniyan, V. Vinayagam, Moni Philip Jacob Kizhakedathil, Kaliraj Perumal","doi":"10.5599/admet.2089","DOIUrl":"https://doi.org/10.5599/admet.2089","url":null,"abstract":"Background and purpose: Lymphatic filariasis is a debilitating infectious disease prevalent in endemic areas, necessitating the development of an effective vaccine for eradication. Although recombinant vaccine candidates have been deemed safe, they often fail to provide sufficient protection, which can be overcome by encapsulating them in nano-liposomes. In this study, we have optimised the liposomal composition for enhanced stability and encapsulation of filarial antigen Brugia malayi thioredoxin (Bm-TRX). Experimental approach: Nano-liposomes were prepared using egg phosphatidylcholine (EPC) and cholesterol via thin-film hydration, followed by sonication and characterizing. Encapsulation efficiency was optimised using different weight ratios of EPC to cholesterol (8:2, 7:3, and 6:4) and total lipid (EPC+Cholesterol) concentration to antigen Bm-TRX (10:1, 10:2, and 10:3) followed by release kinetics study. Key results: Optimised parameters yielded spherical liposomes measuring 209 nm in diameter with narrow polydispersity. Our findings demonstrated the highest encapsulation efficiency of 70.685 % and stability of 10 hours for an EPC to cholesterol weight ratio of 7:3. The in silico study proved the antigenic nature of TRX. Conclusion: The liposomal formulations loaded with TRX, as optimized in this study, hold promise for improving antigen efficiency by enhancing stability, bioavailability, and prophylactic effects by acting as immune potentiators.","PeriodicalId":7259,"journal":{"name":"ADMET and DMPK","volume":"57 4 1","pages":""},"PeriodicalIF":2.5,"publicationDate":"2023-11-30","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"139198127","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0

Metal-organic frameworks: Drug delivery applications and future prospects 金属有机框架：药物输送应用与未来前景

IF 2.5

ADMET and DMPK Pub Date : 2023-11-17 DOI: 10.5599/admet.2057

Prachi Mhettar, Niraj Kale, Jidnyasa Pantwalawalkar, S. Nangare, Namdeo Jadhav

{"title":"Metal-organic frameworks: Drug delivery applications and future prospects","authors":"Prachi Mhettar, Niraj Kale, Jidnyasa Pantwalawalkar, S. Nangare, Namdeo Jadhav","doi":"10.5599/admet.2057","DOIUrl":"https://doi.org/10.5599/admet.2057","url":null,"abstract":"Background and purpose: Metal-organic frameworks (MOFs) have gained incredible consideration in the biomedical field due to their flexible structural configuration, tunable pore size and tailorable surface modification. These inherent characteristics of MOFs portray numerous merits as potential drug carriers, depicting improved drug loading, site-specific drug delivery, biocompatibility, biodegradability, etc. Review approach: The current review article sheds light on the synthesis and use of MOFs in drug delivery applications. In the beginning, a brief overview of the key components and efficient fabrication techniques for MOF synthesis, along with its characterization methods, have been presented. The MOFs-based formulations have been critically discussed. The application of the design of experiments (DoE) approach to optimize MOFs has been elucidated. The MOFs-based formulations, especially the application of stimuli-responsive MOFs for site-specific drug delivery, have been deciphered. Along with drug release kinetic models, several administration methods for MOFs have also been enunciated. Subsequently, MOFs as future potential drug carriers have been elaborated. Key results and conclusion: Recently, MOFs have emerged as versatile drug delivery carriers possessing customization potential and meeting the needs of spatio-temporal drug delivery. Researchers have devised several environment-friendly approaches for MOF construction and surface modification. Owing to stimuli-responsive potential, MOFs have demonstrated their prominent therapeutic efficacy via several routes of administration. The numerous benefits of MOFs would certainly open up a new vista for its novel drug delivery applications.","PeriodicalId":7259,"journal":{"name":"ADMET and DMPK","volume":"66 5","pages":""},"PeriodicalIF":2.5,"publicationDate":"2023-11-17","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"139266685","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0

Nanomaterials as catalysts for the sensitive and selective determination of diclofenac 纳米材料作为催化剂灵敏、选择性地测定双氯芬酸

IF 2.5

ADMET and DMPK Pub Date : 2023-11-16 DOI: 10.5599/admet.2116

T. Dodevska, I. Shterev

{"title":"Nanomaterials as catalysts for the sensitive and selective determination of diclofenac","authors":"T. Dodevska, I. Shterev","doi":"10.5599/admet.2116","DOIUrl":"https://doi.org/10.5599/admet.2116","url":null,"abstract":"Background and purpose: Diclofenac (DCF) is a non-steroidal anti-inflammatory drug possessing analgesic and antipyretic properties. It is used for the treatment of rheumatoid arthritis pain, osteoarthritis, and acute muscle pain conditions and can be administrated orally, topically or intravenously. Because of its widespread use, hydrophilicity, stability and poor degradation (bioaccumulation in the food chain), DCF is an emerging chemical contaminant that can cause adverse effects in the ecosystems. Taking into account the consumption of DCF in pharmaceutical formulations and its negative impact on the environment, the development of new sensitive, selective, cheap, fast, and online capable analytical devices is needed for on-site applications. Experimental approach: This brief review attempts to cover the recent developments related to the use of nanomaterials as catalysts for electrochemical determination of DCF in pharmaceutical formulations, biological fluids and environmental samples. Key results: The article aims to prove how electrochemical sensors represent reliable alternatives to conventional methods for DCF analysis. Conclusion: The manuscript highlights the progress in the development of electrochemical sensors for DCF detection. We have analyzed numerous recent papers (mainly since 2019) on sensors developed for the quantitative determination of DCF, indicating the limit of detection, linear range, stability, reproducibility, and analytical applications. Current challenges related to the sensor design and future perspectives are outlined.","PeriodicalId":7259,"journal":{"name":"ADMET and DMPK","volume":"34 12","pages":""},"PeriodicalIF":2.5,"publicationDate":"2023-11-16","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"139266767","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0

Oral bioavailability enhancement of doxazosin mesylate: Nanosuspension versus self-nanoemulsifying drug delivery systems 甲磺酸多沙唑嗪的口服生物利用度增强:纳米悬浮液与自纳米乳化给药系统

ADMET and DMPK Pub Date : 2023-11-03 DOI: 10.5599/admet.2022

Al Zahraa G. Al Ashmawy, Mohammad H. Alyami, Noura G. Eissa, Gehan F. Balata, Hanan M. El Nahas

{"title":"Oral bioavailability enhancement of doxazosin mesylate: Nanosuspension versus self-nanoemulsifying drug delivery systems","authors":"Al Zahraa G. Al Ashmawy, Mohammad H. Alyami, Noura G. Eissa, Gehan F. Balata, Hanan M. El Nahas","doi":"10.5599/admet.2022","DOIUrl":"https://doi.org/10.5599/admet.2022","url":null,"abstract":"Background and purpose: Doxazosin mesylate (DOX) is an antihypertensive drug that possesses poor water solubility and, hence, poor release properties. Both nanosuspensions and self-nanoemulsifying drug delivery systems (SNEDDS) are becoming nanotechnology techniques for the enhancement of water solubility of different drugs. Experimental approach: The study's goal was to identify the best drug delivery system able to enhance the release and antihypertensive effect of DOX by comparing the physical characteristics such as particle size, zeta potential, entrapment efficiency, release rate, and main arterial blood pressure of DOX-loaded nanosuspensions and SNEDDS in liquid and solid form. Key results: DOX nanosuspension preparation had a particle size of 385±13 nm, poly-dispersity index of 0.049±3, zeta potential of 50 ± 4 mV and drug release after 20 min (91±0.43 %). Liquid SNEDDS had a droplet size of 224±15 nm, poly-dispersity index of (0.470±0.01), zeta potential of -5±0.10 mV and DR20min of 93±4 %. Solid SEDDS showed particle size of 79±14 nm, poly-dispersity index of 1±0.00, a zeta potential of -18 ±0.26 mv and DR20min of 100 ±2.72 %. Conclusion: Finally, in terms of the mean arterial blood pressure lowering, solid SNEDDS performed better effect than both liquid SNEDDS and nanosuspension (P >0.05).","PeriodicalId":7259,"journal":{"name":"ADMET and DMPK","volume":"8 3","pages":"0"},"PeriodicalIF":0.0,"publicationDate":"2023-11-03","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"135872934","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0

Special issue devoted to the IAPC-10 Meeting: Joint World Conferences on Physico-Chemical Methods in Drug Discovery and Development and on ADMET and DMPK. IAPC-10 会议特刊：药物发现和开发中的物理化学方法世界联席会议》和《ADMET 和 DMPK》。

IF 3.4

ADMET and DMPK Pub Date : 2023-10-31 eCollection Date: 2024-01-01 DOI: 10.5599/admet.2541

Tatjana Verbić, Zoran Mandić

引用次数: 0

Nanomaterials as drug delivery agents for overcoming the blood-brain barrier: A comprehensive review 纳米材料作为克服血脑屏障的药物递送剂:综述

ADMET and DMPK Pub Date : 2023-10-31 DOI: 10.5599/admet.2043

Mangesh Kulkarni, Krishi Patel, Ayush Patel, Swayamprakash Patel, Jagruti Desai, Mehul Patel, Umang Shah, Ashish Patel, Nilay Solanki

{"title":"Nanomaterials as drug delivery agents for overcoming the blood-brain barrier: A comprehensive review","authors":"Mangesh Kulkarni, Krishi Patel, Ayush Patel, Swayamprakash Patel, Jagruti Desai, Mehul Patel, Umang Shah, Ashish Patel, Nilay Solanki","doi":"10.5599/admet.2043","DOIUrl":"https://doi.org/10.5599/admet.2043","url":null,"abstract":"Background and Purpose: The blood-brain barrier (BBB), a critical interface of specialized endothelial cells, plays a pivotal role in regulating molecular and ion transport between the central nervous system (CNS) and systemic circulation. Experimental Approach: This review aims to delve into the intricate architecture and functions of the BBB while addressing challenges associated with delivering therapeutics to the brain. Historical milestones and contemporary insights underscore the BBB's significance in protecting the CNS. Key Results: Innovative approaches for enhanced drug transport include intranasal delivery exploiting olfactory and trigeminal pathways, as well as techniques like temporary BBB opening through chemicals, receptors, or focused ultrasound. These avenues hold the potential to reshape conventional drug delivery paradigms and address the limitations posed by the BBB's selectivity. Conclusion: This review underscores the vital role of the BBB in maintaining CNS health and emphasizes the importance of effective drug delivery through this barrier. Nanoparticles emerge as promising candidates to overcome BBB limitations and potentially revolutionize the treatment of CNS disorders. As research progresses, the application of nanomaterials shows immense potential for advancing neurological therapeutics, albeit with careful consideration of safety aspects.","PeriodicalId":7259,"journal":{"name":"ADMET and DMPK","volume":"21 1","pages":"0"},"PeriodicalIF":0.0,"publicationDate":"2023-10-31","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"135809267","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0

Recent advances in nanomaterial-based drug delivery systems for melanoma therapy 基于纳米材料的黑色素瘤药物递送系统的最新进展

ADMET and DMPK Pub Date : 2023-10-24 DOI: 10.5599/admet.2088

Rabinarayan Parhi, Partha Pratim Kaishap, Goutam Kumar Jena

{"title":"Recent advances in nanomaterial-based drug delivery systems for melanoma therapy","authors":"Rabinarayan Parhi, Partha Pratim Kaishap, Goutam Kumar Jena","doi":"10.5599/admet.2088","DOIUrl":"https://doi.org/10.5599/admet.2088","url":null,"abstract":"Background and Purpose: Safe and effective drug delivery is crucial for the treatment of cancer, which is quite impossible to achieve through traditional methods. Among all types of cancer, skin melanoma is known for its aggressive metastasizing ability and an unprecedented higher degree of lethalness, limiting the overall therapeutic efficacy. Here, we focus on the different types of nanomaterials (NMs) and their drug delivery applications against melanoma. Experimental Approach: All relevant publications, including research papers, reviews, chapters and patents, were assessed using search engines such as Scopus and PubMed, up to the end of August of 2023. The keywords used in the search were: nanomaterials, melanoma, drug delivery routes for melanoma, and nanomaterial-based drug delivery systems (DDS). Most of the publications out of 234 cited in this review are from the last five years. Key Results: The recent advancement and mechanism of action of various NMs against melanoma, including inorganic metallic and carbon-based NMs, organic polymeric and lipid-based NMs, and cell-derived vesicles are discussed. We also focus on the application of different NMs in the delivery of therapeutic agents for melanoma therapy. In addition, the skin and melanoma, genetic mutation and pathways for melanoma, conventional treatment options, and delivery routes for therapeutic agents are also discussed briefly. Conclusion: There are few NM-based DDS developed in the lab set up recently. The findings of this review will pave the path for the development of NM-based DDS on an industrial scale and help in the better management of skin melanoma.","PeriodicalId":7259,"journal":{"name":"ADMET and DMPK","volume":"32 7","pages":"0"},"PeriodicalIF":0.0,"publicationDate":"2023-10-24","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"135266651","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0

Nanomaterials in biomedicine, drug delivery and pharmaceutical analysis. 生物医学、药物输送和药物分析中的纳米材料。

IF 2.5

ADMET and DMPK Pub Date : 2023-10-16 eCollection Date: 2023-01-01 DOI: 10.5599/admet.2125

Hassan Karimi-Maleh, Afsaneh L Sanati, Rozhin Darabi

引用次数: 0