{"title":"4-甲基伞伞花缓释PVA-GO给药体系的合成。","authors":"Somayeh Hashamdar, Niloofar Haeri Moghaddam, Setareh Ebrahimnasab, Majid Momeny, Fatemeh Ramezani","doi":"10.1080/03639045.2024.2436530","DOIUrl":null,"url":null,"abstract":"<p><strong>Introduction: </strong>4-methyl umbelliferon (4MU) is a coumarin with anti-inflammatory, anti-thrombotic, enzyme-inhibiting, and antioxidant properties. Despite the benefits of the compound, it is eliminated very quickly from the blood circulation through the liver, kidney, and digestive system due to its hydrophobic properties. In this study we proposed to improve the durability of 4MU by binding of 4MU to poly vinyl alcohol (PVA) and graphene oxide (GO).</p><p><strong>Methods: </strong>The PVA-4MU-GO complex was synthesized and characterized. Release of 4MU from the complex was investigated. H9C2 cells viability was investigated and the entry of complex to the cell was analyzed using flow cytometry.</p><p><strong>Result: </strong>UV-Vis and FTIR studies confirmed the interaction of 4MU with PVA and GO. SEM measurement also revealed a particle size around 101 nm for PVA-4MU-GO complexes. The obtained results confirmed the assembly of PVA-4MU-GO. A continuous drug release for 8 d (160 h) was achieved. Cytotoxic studies on H9C2 cell showed that PVA-4MU-GO complex is dependent to the concentration of GO and also the relation of 4MU to GO. Sustained release and penetration of PVA-4MU-GO complex into the H9C2 cell were observed.</p><p><strong>Conclusion: </strong>PVA-4MU-GO complex is recommended as an alternative for 4MU. Synthesis the complex of PVA-4MU-GO, verifying the correct binding, showing the <i>in vitro</i> release of the 4MU, as well as checking its toxicity and its gradual entry into the H9C2 cell, were performed in this study.</p>","PeriodicalId":11263,"journal":{"name":"Drug Development and Industrial Pharmacy","volume":" ","pages":"1021-1030"},"PeriodicalIF":2.4000,"publicationDate":"2024-12-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"0","resultStr":"{\"title\":\"Synthesis of a PVA-GO drug delivery system for sustained release of 4-methyl umbelliferon.\",\"authors\":\"Somayeh Hashamdar, Niloofar Haeri Moghaddam, Setareh Ebrahimnasab, Majid Momeny, Fatemeh Ramezani\",\"doi\":\"10.1080/03639045.2024.2436530\",\"DOIUrl\":null,\"url\":null,\"abstract\":\"<p><strong>Introduction: </strong>4-methyl umbelliferon (4MU) is a coumarin with anti-inflammatory, anti-thrombotic, enzyme-inhibiting, and antioxidant properties. Despite the benefits of the compound, it is eliminated very quickly from the blood circulation through the liver, kidney, and digestive system due to its hydrophobic properties. In this study we proposed to improve the durability of 4MU by binding of 4MU to poly vinyl alcohol (PVA) and graphene oxide (GO).</p><p><strong>Methods: </strong>The PVA-4MU-GO complex was synthesized and characterized. Release of 4MU from the complex was investigated. H9C2 cells viability was investigated and the entry of complex to the cell was analyzed using flow cytometry.</p><p><strong>Result: </strong>UV-Vis and FTIR studies confirmed the interaction of 4MU with PVA and GO. SEM measurement also revealed a particle size around 101 nm for PVA-4MU-GO complexes. The obtained results confirmed the assembly of PVA-4MU-GO. A continuous drug release for 8 d (160 h) was achieved. Cytotoxic studies on H9C2 cell showed that PVA-4MU-GO complex is dependent to the concentration of GO and also the relation of 4MU to GO. Sustained release and penetration of PVA-4MU-GO complex into the H9C2 cell were observed.</p><p><strong>Conclusion: </strong>PVA-4MU-GO complex is recommended as an alternative for 4MU. Synthesis the complex of PVA-4MU-GO, verifying the correct binding, showing the <i>in vitro</i> release of the 4MU, as well as checking its toxicity and its gradual entry into the H9C2 cell, were performed in this study.</p>\",\"PeriodicalId\":11263,\"journal\":{\"name\":\"Drug Development and Industrial Pharmacy\",\"volume\":\" \",\"pages\":\"1021-1030\"},\"PeriodicalIF\":2.4000,\"publicationDate\":\"2024-12-01\",\"publicationTypes\":\"Journal Article\",\"fieldsOfStudy\":null,\"isOpenAccess\":false,\"openAccessPdf\":\"\",\"citationCount\":\"0\",\"resultStr\":null,\"platform\":\"Semanticscholar\",\"paperid\":null,\"PeriodicalName\":\"Drug Development and Industrial Pharmacy\",\"FirstCategoryId\":\"3\",\"ListUrlMain\":\"https://doi.org/10.1080/03639045.2024.2436530\",\"RegionNum\":4,\"RegionCategory\":\"医学\",\"ArticlePicture\":[],\"TitleCN\":null,\"AbstractTextCN\":null,\"PMCID\":null,\"EPubDate\":\"2024/12/4 0:00:00\",\"PubModel\":\"Epub\",\"JCR\":\"Q3\",\"JCRName\":\"CHEMISTRY, MEDICINAL\",\"Score\":null,\"Total\":0}","platform":"Semanticscholar","paperid":null,"PeriodicalName":"Drug Development and Industrial Pharmacy","FirstCategoryId":"3","ListUrlMain":"https://doi.org/10.1080/03639045.2024.2436530","RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"2024/12/4 0:00:00","PubModel":"Epub","JCR":"Q3","JCRName":"CHEMISTRY, MEDICINAL","Score":null,"Total":0}
引用次数: 0
摘要
简介:4-甲基伞形花(4MU)是一种具有抗炎、抗血栓、抑制酶和抗氧化特性的香豆素。尽管这种化合物有好处,但由于它的疏水性,它很快就会通过肝脏、肾脏和消化系统从血液循环中消除。在这项研究中,我们提出通过将4MU与聚乙烯醇(PVA)和氧化石墨烯(GO)结合来提高4MU的耐久性。方法:合成PVA-4MU-GO配合物并进行表征。研究了该配合物中4MU的释放。流式细胞术检测H9C2细胞活力,分析复合物进入细胞的情况。结果:UV-Vis和FTIR研究证实了4MU与PVA和GO的相互作用。SEM测量还显示PVA-4MU-GO配合物的粒径约为101 nm。所得结果证实了PVA-4MU-GO的组装。药物连续释放8 d (160 h)。对H9C2细胞的细胞毒性研究表明,PVA-4MU-GO复合物依赖于GO的浓度以及4MU与GO的关系。观察PVA-4MU-GO复合物在H9C2细胞中的持续释放和渗透。结论:推荐PVA-4MU-GO配合物作为4MU的替代品。本研究合成了PVA-4MU-GO复合物,验证了其正确结合,显示了4MU的体外释放,并检查了其毒性和逐渐进入H9C2细胞。
Synthesis of a PVA-GO drug delivery system for sustained release of 4-methyl umbelliferon.
Introduction: 4-methyl umbelliferon (4MU) is a coumarin with anti-inflammatory, anti-thrombotic, enzyme-inhibiting, and antioxidant properties. Despite the benefits of the compound, it is eliminated very quickly from the blood circulation through the liver, kidney, and digestive system due to its hydrophobic properties. In this study we proposed to improve the durability of 4MU by binding of 4MU to poly vinyl alcohol (PVA) and graphene oxide (GO).
Methods: The PVA-4MU-GO complex was synthesized and characterized. Release of 4MU from the complex was investigated. H9C2 cells viability was investigated and the entry of complex to the cell was analyzed using flow cytometry.
Result: UV-Vis and FTIR studies confirmed the interaction of 4MU with PVA and GO. SEM measurement also revealed a particle size around 101 nm for PVA-4MU-GO complexes. The obtained results confirmed the assembly of PVA-4MU-GO. A continuous drug release for 8 d (160 h) was achieved. Cytotoxic studies on H9C2 cell showed that PVA-4MU-GO complex is dependent to the concentration of GO and also the relation of 4MU to GO. Sustained release and penetration of PVA-4MU-GO complex into the H9C2 cell were observed.
Conclusion: PVA-4MU-GO complex is recommended as an alternative for 4MU. Synthesis the complex of PVA-4MU-GO, verifying the correct binding, showing the in vitro release of the 4MU, as well as checking its toxicity and its gradual entry into the H9C2 cell, were performed in this study.
期刊介绍:
The aim of Drug Development and Industrial Pharmacy is to publish novel, original, peer-reviewed research manuscripts within relevant topics and research methods related to pharmaceutical research and development, and industrial pharmacy. Research papers must be hypothesis driven and emphasize innovative breakthrough topics in pharmaceutics and drug delivery. The journal will also consider timely critical review papers.