水溶性 Calixarene 的设计、开发和体外评估:用于紫杉醇给药的超分子纳米载体

IF 0.8 4区 医学 Q4 CHEMISTRY, MEDICINAL Pharmaceutical Chemistry Journal Pub Date : 2024-08-03 DOI:10.1007/s11094-024-03182-2
Jigar Raval, Riddhi Trivedi, Prajesh Prajapati
{"title":"水溶性 Calixarene 的设计、开发和体外评估:用于紫杉醇给药的超分子纳米载体","authors":"Jigar Raval, Riddhi Trivedi, Prajesh Prajapati","doi":"10.1007/s11094-024-03182-2","DOIUrl":null,"url":null,"abstract":"<p>In the area of drug development the solubility of an active ingredient plays a very crucial and vital part and is of the highest significance. Increasing importance is being placed on the research into active ingredient solubilization. The designing of a host guest complex with a compound that has a higher dissolubility profile can work with the solubilization of lipophilic drugs. In this research work optimized nano-carriers were effectively synthesized utilizing thin-film hydration strategies. The drug sulfonated calix[4]resorcinarene blend (1:10) containing ethanol was dispersed and sonicated with an estimated three cycles, at an amplitude 70 with a 20-s interval for an optimized time. The synthesized nanovesicles have an average diameter of 477.7 nm, a higher mono dispersity (PDI-0.282), and a greater loading capacity of the drugs is 95%. Atomic force microscopy in accordance with dynamic light-scattering spectra confirmed the spherical shape of paclitaxel-loaded sulfonated calix[4]resorcinarene nanovesicles<i>.</i> In vitro release of medication from nanovesicles affirmed the extended discharge pattern of drugs with r<sup>2</sup> of 0.9902 compared with the commercial formulation available on the market. MTT assay is performed to access the toxicity of the sufonated calix[4]resorcinarene <i>in vitro</i>. IC<sub>50</sub> values indicate that synthesized sufonated calix[4]resorcinarene shows better IC<sub>50</sub> values than paclitaxel and taxol. The formulated nanovesicles from sulfonated calix[4]resorcinarene showed an ideal size with higher capacity for binding drug and provide better patient compliance, which are positive for their expected application as a modular drug delivery platform for anti-cancer drugs.</p>","PeriodicalId":19990,"journal":{"name":"Pharmaceutical Chemistry Journal","volume":null,"pages":null},"PeriodicalIF":0.8000,"publicationDate":"2024-08-03","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"0","resultStr":"{\"title\":\"Design, Development and In Vitro Assessment of Water-Soluble Calixarene: A Supramolecular-Based Nano-Carrier for Paclitaxel Drug Delivery\",\"authors\":\"Jigar Raval, Riddhi Trivedi, Prajesh Prajapati\",\"doi\":\"10.1007/s11094-024-03182-2\",\"DOIUrl\":null,\"url\":null,\"abstract\":\"<p>In the area of drug development the solubility of an active ingredient plays a very crucial and vital part and is of the highest significance. Increasing importance is being placed on the research into active ingredient solubilization. The designing of a host guest complex with a compound that has a higher dissolubility profile can work with the solubilization of lipophilic drugs. In this research work optimized nano-carriers were effectively synthesized utilizing thin-film hydration strategies. The drug sulfonated calix[4]resorcinarene blend (1:10) containing ethanol was dispersed and sonicated with an estimated three cycles, at an amplitude 70 with a 20-s interval for an optimized time. The synthesized nanovesicles have an average diameter of 477.7 nm, a higher mono dispersity (PDI-0.282), and a greater loading capacity of the drugs is 95%. Atomic force microscopy in accordance with dynamic light-scattering spectra confirmed the spherical shape of paclitaxel-loaded sulfonated calix[4]resorcinarene nanovesicles<i>.</i> In vitro release of medication from nanovesicles affirmed the extended discharge pattern of drugs with r<sup>2</sup> of 0.9902 compared with the commercial formulation available on the market. MTT assay is performed to access the toxicity of the sufonated calix[4]resorcinarene <i>in vitro</i>. IC<sub>50</sub> values indicate that synthesized sufonated calix[4]resorcinarene shows better IC<sub>50</sub> values than paclitaxel and taxol. The formulated nanovesicles from sulfonated calix[4]resorcinarene showed an ideal size with higher capacity for binding drug and provide better patient compliance, which are positive for their expected application as a modular drug delivery platform for anti-cancer drugs.</p>\",\"PeriodicalId\":19990,\"journal\":{\"name\":\"Pharmaceutical Chemistry Journal\",\"volume\":null,\"pages\":null},\"PeriodicalIF\":0.8000,\"publicationDate\":\"2024-08-03\",\"publicationTypes\":\"Journal Article\",\"fieldsOfStudy\":null,\"isOpenAccess\":false,\"openAccessPdf\":\"\",\"citationCount\":\"0\",\"resultStr\":null,\"platform\":\"Semanticscholar\",\"paperid\":null,\"PeriodicalName\":\"Pharmaceutical Chemistry Journal\",\"FirstCategoryId\":\"3\",\"ListUrlMain\":\"https://doi.org/10.1007/s11094-024-03182-2\",\"RegionNum\":4,\"RegionCategory\":\"医学\",\"ArticlePicture\":[],\"TitleCN\":null,\"AbstractTextCN\":null,\"PMCID\":null,\"EPubDate\":\"\",\"PubModel\":\"\",\"JCR\":\"Q4\",\"JCRName\":\"CHEMISTRY, MEDICINAL\",\"Score\":null,\"Total\":0}","platform":"Semanticscholar","paperid":null,"PeriodicalName":"Pharmaceutical Chemistry Journal","FirstCategoryId":"3","ListUrlMain":"https://doi.org/10.1007/s11094-024-03182-2","RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"Q4","JCRName":"CHEMISTRY, MEDICINAL","Score":null,"Total":0}
引用次数: 0

摘要

在药物研发领域,活性成分的溶解度起着至关重要的作用,具有极其重要的意义。活性成分的溶解性研究越来越受到重视。设计一种具有较高溶解度的化合物的主客复合物,可以提高亲脂性药物的溶解度。在这项研究工作中,利用薄膜水合策略有效合成了优化的纳米载体。将含有乙醇的药物磺化钙[4]间苯二酚混合物(1:10)分散,并在优化的时间内,以 70 的振幅和 20 秒的间隔进行了估计三个循环的超声处理。合成的纳米微粒平均直径为 477.7 nm,单分散度(PDI-0.282)较高,载药量为 95%。原子力显微镜和动态光散射光谱证实,磺化钙[4]间苯二酚纳米粒子呈球形。体外药物释放证实,与市场上的商业制剂相比,纳米颗粒的药物释放模式更长,r2 为 0.9902。MTT 试验用于体外检测磺化钙[4]间苯二酚的毒性。IC50 值表明,合成的磺化卡利克[4]间苯二酚的 IC50 值优于紫杉醇和紫杉醇。磺化钙[4]间苯二酚配制的纳米微粒具有理想的尺寸和更高的药物结合能力,能更好地满足患者的需求,有望成为抗癌药物的模块化给药平台。
本文章由计算机程序翻译,如有差异,请以英文原文为准。

摘要图片

查看原文
分享 分享
微信好友 朋友圈 QQ好友 复制链接
本刊更多论文
Design, Development and In Vitro Assessment of Water-Soluble Calixarene: A Supramolecular-Based Nano-Carrier for Paclitaxel Drug Delivery

In the area of drug development the solubility of an active ingredient plays a very crucial and vital part and is of the highest significance. Increasing importance is being placed on the research into active ingredient solubilization. The designing of a host guest complex with a compound that has a higher dissolubility profile can work with the solubilization of lipophilic drugs. In this research work optimized nano-carriers were effectively synthesized utilizing thin-film hydration strategies. The drug sulfonated calix[4]resorcinarene blend (1:10) containing ethanol was dispersed and sonicated with an estimated three cycles, at an amplitude 70 with a 20-s interval for an optimized time. The synthesized nanovesicles have an average diameter of 477.7 nm, a higher mono dispersity (PDI-0.282), and a greater loading capacity of the drugs is 95%. Atomic force microscopy in accordance with dynamic light-scattering spectra confirmed the spherical shape of paclitaxel-loaded sulfonated calix[4]resorcinarene nanovesicles. In vitro release of medication from nanovesicles affirmed the extended discharge pattern of drugs with r2 of 0.9902 compared with the commercial formulation available on the market. MTT assay is performed to access the toxicity of the sufonated calix[4]resorcinarene in vitro. IC50 values indicate that synthesized sufonated calix[4]resorcinarene shows better IC50 values than paclitaxel and taxol. The formulated nanovesicles from sulfonated calix[4]resorcinarene showed an ideal size with higher capacity for binding drug and provide better patient compliance, which are positive for their expected application as a modular drug delivery platform for anti-cancer drugs.

求助全文
通过发布文献求助,成功后即可免费获取论文全文。 去求助
来源期刊
Pharmaceutical Chemistry Journal
Pharmaceutical Chemistry Journal CHEMISTRY, MEDICINAL-PHARMACOLOGY & PHARMACY
CiteScore
1.30
自引率
22.20%
发文量
226
审稿时长
3-8 weeks
期刊介绍: Pharmaceutical Chemistry Journal is a monthly publication devoted to scientific and technical research on the creation of new drugs and the improvement of manufacturing technology of drugs and intermediates. International contributors cover the entire spectrum of new drug research, including: methods of synthesis; results of pharmacological, toxicological, and biochemical studies; investigation of structure - activity relationships in prediction of new compounds; methods and technical facilities used; and problems associated with the development of ecologically safe and economically feasible methods of industrial production. In addition, analytical reviews of the international literature in the field provide coverage of the most recent developments around the world. Pharmaceutical Chemistry Journal is a translation of the Russian journal Khimiko-Farmatsevticheskii Zhurnal. The Russian Volume Year is published in English from April. All articles are peer-reviewed.
期刊最新文献
Synthesis, In Vitro Antimycobacterial Activity of Some 2-((5-Amino-1,3,4-Thiadiazol-2-YL)Methyl)-6-Aryl-Tetrahydropyridazin-3-One Derivatives Long-Acting Hydrogel Eye Drops Composite Sequentially Releases Basic Fibroblast Growth Factor and Carbomer for Synergistic Promotion of the Repair of Corneal Epithelium Study of Changes in Enterosgel Structure in Case of Violation of Drug Storage Conditions HPLC Determination of Myricitrin in Leaves of Common Myrtle (Myrtus communis L.) Preparation, Physicochemical Properties, and Antibacterial Activity of Hydrogel Films Based on Starch and Poly(Vinyl Alcohol) with Added Ethonium
×
引用
GB/T 7714-2015
复制
MLA
复制
APA
复制
导出至
BibTeX EndNote RefMan NoteFirst NoteExpress
×
×
提示
您的信息不完整,为了账户安全,请先补充。
现在去补充
×
提示
您因"违规操作"
具体请查看互助需知
我知道了
×
提示
现在去查看 取消
×
提示
确定
0
微信
客服QQ
Book学术公众号 扫码关注我们
反馈
×
意见反馈
请填写您的意见或建议
请填写您的手机或邮箱
已复制链接
已复制链接
快去分享给好友吧!
我知道了
×
扫码分享
扫码分享
Book学术官方微信
Book学术文献互助
Book学术文献互助群
群 号:481959085
Book学术
文献互助 智能选刊 最新文献 互助须知 联系我们:info@booksci.cn
Book学术提供免费学术资源搜索服务,方便国内外学者检索中英文文献。致力于提供最便捷和优质的服务体验。
Copyright © 2023 Book学术 All rights reserved.
ghs 京公网安备 11010802042870号 京ICP备2023020795号-1