三元固体分散体作为增强药理活性的替代方法。

IF 4.7 2区 医学 Q1 CHEMISTRY, MEDICINAL
Drug Design, Development and Therapy Pub Date : 2025-07-03 eCollection Date: 2025-01-01 DOI:10.2147/DDDT.S533359
Salma Amaliah, Diah Lia Aulifa, Amirah Mohd Gazzali, Arif Budiman
{"title":"三元固体分散体作为增强药理活性的替代方法。","authors":"Salma Amaliah, Diah Lia Aulifa, Amirah Mohd Gazzali, Arif Budiman","doi":"10.2147/DDDT.S533359","DOIUrl":null,"url":null,"abstract":"<p><p>Poor solubility and limited bioavailability remain significant challenges in developing oral drugs, affecting the clinical efficacy of many active pharmaceutical ingredients (APIs). Enhancing solubility has become a primary focus in improving API bioavailability. Among the most commonly employed strategies are amorphous solid dispersions (ASDs) and co-amorphous systems, collectively called binary systems. However, these systems often suffer from wettability and physicochemical limitations, which can hinder drug release. Adding a third component to form ternary solid dispersions (TSDs) significantly enhance drug release and bioavailability, ultimately improving therapeutic outcomes. While numerous studies have investigated the application of TSDs in enhancing API pharmacological activity, only limited studies have a comprehensive analysis of this approach. Therefore, this review aims to summarize and elucidate the mechanisms of TSD systems in improving pharmacological activity. The review includes available literature from Scopus, PubMed, and Google Scholar that utilizes the keywords \"ternary solid dispersion\" and \"pharmacological activity\", summarizing the importance of TSDs in therapeutic formulations for enhancing pharmacological activity. Various in vitro and in vivo studies consistently demonstrate that TSDs outperform binary systems by significantly enhancing the pharmacological effects of diverse therapeutic agents, including those with antioxidant, anti-inflammatory, anticancer, antibacterial, anticholinesterase, antihyperlipidemic, anti-hypoglycemic, anti-Alzheimer's, antidiabetic, and hepatoprotective properties. This approach holds significant promise as an alternative for the formulation of low-solubility pharmaceuticals.</p>","PeriodicalId":11290,"journal":{"name":"Drug Design, Development and Therapy","volume":"19 ","pages":"5663-5684"},"PeriodicalIF":4.7000,"publicationDate":"2025-07-03","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC12233025/pdf/","citationCount":"0","resultStr":"{\"title\":\"Ternary Solid Dispersions as an Alternative Approach to Enhance Pharmacological Activity.\",\"authors\":\"Salma Amaliah, Diah Lia Aulifa, Amirah Mohd Gazzali, Arif Budiman\",\"doi\":\"10.2147/DDDT.S533359\",\"DOIUrl\":null,\"url\":null,\"abstract\":\"<p><p>Poor solubility and limited bioavailability remain significant challenges in developing oral drugs, affecting the clinical efficacy of many active pharmaceutical ingredients (APIs). Enhancing solubility has become a primary focus in improving API bioavailability. Among the most commonly employed strategies are amorphous solid dispersions (ASDs) and co-amorphous systems, collectively called binary systems. However, these systems often suffer from wettability and physicochemical limitations, which can hinder drug release. Adding a third component to form ternary solid dispersions (TSDs) significantly enhance drug release and bioavailability, ultimately improving therapeutic outcomes. While numerous studies have investigated the application of TSDs in enhancing API pharmacological activity, only limited studies have a comprehensive analysis of this approach. Therefore, this review aims to summarize and elucidate the mechanisms of TSD systems in improving pharmacological activity. The review includes available literature from Scopus, PubMed, and Google Scholar that utilizes the keywords \\\"ternary solid dispersion\\\" and \\\"pharmacological activity\\\", summarizing the importance of TSDs in therapeutic formulations for enhancing pharmacological activity. Various in vitro and in vivo studies consistently demonstrate that TSDs outperform binary systems by significantly enhancing the pharmacological effects of diverse therapeutic agents, including those with antioxidant, anti-inflammatory, anticancer, antibacterial, anticholinesterase, antihyperlipidemic, anti-hypoglycemic, anti-Alzheimer's, antidiabetic, and hepatoprotective properties. This approach holds significant promise as an alternative for the formulation of low-solubility pharmaceuticals.</p>\",\"PeriodicalId\":11290,\"journal\":{\"name\":\"Drug Design, Development and Therapy\",\"volume\":\"19 \",\"pages\":\"5663-5684\"},\"PeriodicalIF\":4.7000,\"publicationDate\":\"2025-07-03\",\"publicationTypes\":\"Journal Article\",\"fieldsOfStudy\":null,\"isOpenAccess\":false,\"openAccessPdf\":\"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC12233025/pdf/\",\"citationCount\":\"0\",\"resultStr\":null,\"platform\":\"Semanticscholar\",\"paperid\":null,\"PeriodicalName\":\"Drug Design, Development and Therapy\",\"FirstCategoryId\":\"3\",\"ListUrlMain\":\"https://doi.org/10.2147/DDDT.S533359\",\"RegionNum\":2,\"RegionCategory\":\"医学\",\"ArticlePicture\":[],\"TitleCN\":null,\"AbstractTextCN\":null,\"PMCID\":null,\"EPubDate\":\"2025/1/1 0:00:00\",\"PubModel\":\"eCollection\",\"JCR\":\"Q1\",\"JCRName\":\"CHEMISTRY, MEDICINAL\",\"Score\":null,\"Total\":0}","platform":"Semanticscholar","paperid":null,"PeriodicalName":"Drug Design, Development and Therapy","FirstCategoryId":"3","ListUrlMain":"https://doi.org/10.2147/DDDT.S533359","RegionNum":2,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"2025/1/1 0:00:00","PubModel":"eCollection","JCR":"Q1","JCRName":"CHEMISTRY, MEDICINAL","Score":null,"Total":0}
引用次数: 0

摘要

溶解度差和生物利用度有限仍然是开发口服药物的重大挑战,影响了许多活性药物成分(api)的临床疗效。提高溶解度已成为提高原料药生物利用度的主要焦点。其中最常用的策略是非晶固体分散体(asd)和共非晶系统,统称为二元系统。然而,这些系统往往受到润湿性和物理化学限制,这可能会阻碍药物释放。添加第三种成分形成三元固体分散体(TSDs)可显著提高药物释放和生物利用度,最终改善治疗效果。虽然有许多研究探讨了TSDs在增强原料药药理活性方面的应用,但对这种方法进行全面分析的研究有限。因此,本文旨在总结和阐明TSD系统提高药理活性的机制。本文结合Scopus、PubMed、谷歌Scholar等网站的文献,利用关键词“三元固体分散体”和“药理活性”,总结了TSDs在治疗配方中增强药理活性的重要性。各种体外和体内研究一致表明,TSDs通过显着增强多种治疗药物的药理作用而优于二元系统,包括抗氧化,抗炎,抗癌,抗菌,抗胆碱酯酶,抗高血脂,抗低血糖,抗阿尔茨海默氏症,抗糖尿病和肝脏保护特性。这种方法作为低溶解度药物制剂的替代方案具有重要的前景。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
Ternary Solid Dispersions as an Alternative Approach to Enhance Pharmacological Activity.

Poor solubility and limited bioavailability remain significant challenges in developing oral drugs, affecting the clinical efficacy of many active pharmaceutical ingredients (APIs). Enhancing solubility has become a primary focus in improving API bioavailability. Among the most commonly employed strategies are amorphous solid dispersions (ASDs) and co-amorphous systems, collectively called binary systems. However, these systems often suffer from wettability and physicochemical limitations, which can hinder drug release. Adding a third component to form ternary solid dispersions (TSDs) significantly enhance drug release and bioavailability, ultimately improving therapeutic outcomes. While numerous studies have investigated the application of TSDs in enhancing API pharmacological activity, only limited studies have a comprehensive analysis of this approach. Therefore, this review aims to summarize and elucidate the mechanisms of TSD systems in improving pharmacological activity. The review includes available literature from Scopus, PubMed, and Google Scholar that utilizes the keywords "ternary solid dispersion" and "pharmacological activity", summarizing the importance of TSDs in therapeutic formulations for enhancing pharmacological activity. Various in vitro and in vivo studies consistently demonstrate that TSDs outperform binary systems by significantly enhancing the pharmacological effects of diverse therapeutic agents, including those with antioxidant, anti-inflammatory, anticancer, antibacterial, anticholinesterase, antihyperlipidemic, anti-hypoglycemic, anti-Alzheimer's, antidiabetic, and hepatoprotective properties. This approach holds significant promise as an alternative for the formulation of low-solubility pharmaceuticals.

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
Drug Design, Development and Therapy
Drug Design, Development and Therapy CHEMISTRY, MEDICINAL-PHARMACOLOGY & PHARMACY
CiteScore
9.00
自引率
0.00%
发文量
382
审稿时长
>12 weeks
期刊介绍: Drug Design, Development and Therapy is an international, peer-reviewed, open access journal that spans the spectrum of drug design, discovery and development through to clinical applications. The journal is characterized by the rapid reporting of high-quality original research, reviews, expert opinions, commentary and clinical studies in all therapeutic areas. Specific topics covered by the journal include: Drug target identification and validation Phenotypic screening and target deconvolution Biochemical analyses of drug targets and their pathways New methods or relevant applications in molecular/drug design and computer-aided drug discovery* Design, synthesis, and biological evaluation of novel biologically active compounds (including diagnostics or chemical probes) Structural or molecular biological studies elucidating molecular recognition processes Fragment-based drug discovery Pharmaceutical/red biotechnology Isolation, structural characterization, (bio)synthesis, bioengineering and pharmacological evaluation of natural products** Distribution, pharmacokinetics and metabolic transformations of drugs or biologically active compounds in drug development Drug delivery and formulation (design and characterization of dosage forms, release mechanisms and in vivo testing) Preclinical development studies Translational animal models Mechanisms of action and signalling pathways Toxicology Gene therapy, cell therapy and immunotherapy Personalized medicine and pharmacogenomics Clinical drug evaluation Patient safety and sustained use of medicines.
×
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
确定
请完成安全验证×
copy
已复制链接
快去分享给好友吧!
我知道了
右上角分享
点击右上角分享
0
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 布克学术 All rights reserved.
京ICP备2023020795号-1
ghs 京公网安备 11010802042870号
Book学术文献互助
Book学术文献互助群
群 号:604180095
Book学术官方微信