通过共非晶固体分散体给药:物理化学特性和生物潜力的全面和最新综述。

Shailender Mohan, Abdul Hafeez
{"title":"通过共非晶固体分散体给药:物理化学特性和生物潜力的全面和最新综述。","authors":"Shailender Mohan, Abdul Hafeez","doi":"10.2174/0126673878351727250409094214","DOIUrl":null,"url":null,"abstract":"<p><p>New chemical entities with low aqueous solubility and permeability encounter significant challenges in formulation development. Low solubility is further accompanied by slow dissolution and poor bioavailability, which in turn leads to unpredictability in terms of both bioavailability and toxicity. Therefore, a significant amount of exertion is necessary to enhance solubility, dissolution, and eventually bioavailability. Additionally, to enhance the solubility properties and amorphous stability of BCS Class II medications and ultimately increase drug bioavailability, coamorphization has emerged as a promising strategy. Co-amorphous solid dispersions (CASD) are multi-component single-phase amorphous solid dispersions comprising two or more small molecules (usually known as co-formers) that might be a combination of drug-drug or drug-excipients. The selection of appropriate co-formers is critical, and the surface properties of co-amorphous formulations must be carefully evaluated, as they influence physical and chemical stability in addition to dissolution performance. Scaling up and processing co-amorphous formulations into the final dosage forms presents challenges that need to be addressed. This review will largely concentrate on the challenges, improvements, and innovations in physicochemical properties, biological characterization, and advancements of co-amorphous systems. This review will also furnish a comprehensive explanation of both established and emerging approaches utilized in the estimation of physicochemical attributes and characterization of CASD (in vitro and in vivo). Regarding CASD's potential to improve patient outcomes and therapeutic efficacy, it has emerged as a viable approach for drug candidates posing the problems of solubility and bioavailability. This approach has also increased the physical stability of drugs.</p>","PeriodicalId":94352,"journal":{"name":"Recent advances in drug delivery and formulation","volume":" ","pages":""},"PeriodicalIF":0.0000,"publicationDate":"2025-04-18","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"0","resultStr":"{\"title\":\"Drug Delivery through Co-amorphous Solid Dispersions: A Comprehensive and Updated Review on Physicochemical Characteristics and Biological Potential.\",\"authors\":\"Shailender Mohan, Abdul Hafeez\",\"doi\":\"10.2174/0126673878351727250409094214\",\"DOIUrl\":null,\"url\":null,\"abstract\":\"<p><p>New chemical entities with low aqueous solubility and permeability encounter significant challenges in formulation development. Low solubility is further accompanied by slow dissolution and poor bioavailability, which in turn leads to unpredictability in terms of both bioavailability and toxicity. Therefore, a significant amount of exertion is necessary to enhance solubility, dissolution, and eventually bioavailability. Additionally, to enhance the solubility properties and amorphous stability of BCS Class II medications and ultimately increase drug bioavailability, coamorphization has emerged as a promising strategy. Co-amorphous solid dispersions (CASD) are multi-component single-phase amorphous solid dispersions comprising two or more small molecules (usually known as co-formers) that might be a combination of drug-drug or drug-excipients. The selection of appropriate co-formers is critical, and the surface properties of co-amorphous formulations must be carefully evaluated, as they influence physical and chemical stability in addition to dissolution performance. Scaling up and processing co-amorphous formulations into the final dosage forms presents challenges that need to be addressed. This review will largely concentrate on the challenges, improvements, and innovations in physicochemical properties, biological characterization, and advancements of co-amorphous systems. This review will also furnish a comprehensive explanation of both established and emerging approaches utilized in the estimation of physicochemical attributes and characterization of CASD (in vitro and in vivo). Regarding CASD's potential to improve patient outcomes and therapeutic efficacy, it has emerged as a viable approach for drug candidates posing the problems of solubility and bioavailability. This approach has also increased the physical stability of drugs.</p>\",\"PeriodicalId\":94352,\"journal\":{\"name\":\"Recent advances in drug delivery and formulation\",\"volume\":\" \",\"pages\":\"\"},\"PeriodicalIF\":0.0000,\"publicationDate\":\"2025-04-18\",\"publicationTypes\":\"Journal Article\",\"fieldsOfStudy\":null,\"isOpenAccess\":false,\"openAccessPdf\":\"\",\"citationCount\":\"0\",\"resultStr\":null,\"platform\":\"Semanticscholar\",\"paperid\":null,\"PeriodicalName\":\"Recent advances in drug delivery and formulation\",\"FirstCategoryId\":\"1085\",\"ListUrlMain\":\"https://doi.org/10.2174/0126673878351727250409094214\",\"RegionNum\":0,\"RegionCategory\":null,\"ArticlePicture\":[],\"TitleCN\":null,\"AbstractTextCN\":null,\"PMCID\":null,\"EPubDate\":\"\",\"PubModel\":\"\",\"JCR\":\"\",\"JCRName\":\"\",\"Score\":null,\"Total\":0}","platform":"Semanticscholar","paperid":null,"PeriodicalName":"Recent advances in drug delivery and formulation","FirstCategoryId":"1085","ListUrlMain":"https://doi.org/10.2174/0126673878351727250409094214","RegionNum":0,"RegionCategory":null,"ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"","JCRName":"","Score":null,"Total":0}
引用次数: 0

摘要

低水溶性、低渗透性的新型化学实体在配方开发中遇到了重大挑战。低溶解度进一步伴随着溶解缓慢和生物利用度差,这反过来导致生物利用度和毒性方面的不可预测性。因此,需要大量的努力来提高溶解度、溶解度和最终的生物利用度。此外,为了提高BCS II类药物的溶解度和无定形稳定性,并最终提高药物的生物利用度,共晶化已成为一种很有前途的策略。共非晶固体分散体(CASD)是由两个或多个小分子(通常称为共成体)组成的多组分单相非晶固体分散体,可能是药物-药物或药物-赋形剂的组合。选择合适的共晶是至关重要的,必须仔细评估共晶配方的表面特性,因为它们除了影响溶解性能外,还会影响物理和化学稳定性。扩大规模并将共非晶制剂加工成最终剂型提出了需要解决的挑战。这篇综述将主要集中在挑战,改进和创新的物理化学性质,生物表征,和共非晶系统的进展。这篇综述也将提供一个全面的解释,既建立的和新兴的方法用于估计CASD的物理化学属性和表征(体外和体内)。考虑到CASD在改善患者预后和治疗效果方面的潜力,它已成为解决溶解度和生物利用度问题的候选药物的可行方法。这种方法也增加了药物的物理稳定性。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
Drug Delivery through Co-amorphous Solid Dispersions: A Comprehensive and Updated Review on Physicochemical Characteristics and Biological Potential.

New chemical entities with low aqueous solubility and permeability encounter significant challenges in formulation development. Low solubility is further accompanied by slow dissolution and poor bioavailability, which in turn leads to unpredictability in terms of both bioavailability and toxicity. Therefore, a significant amount of exertion is necessary to enhance solubility, dissolution, and eventually bioavailability. Additionally, to enhance the solubility properties and amorphous stability of BCS Class II medications and ultimately increase drug bioavailability, coamorphization has emerged as a promising strategy. Co-amorphous solid dispersions (CASD) are multi-component single-phase amorphous solid dispersions comprising two or more small molecules (usually known as co-formers) that might be a combination of drug-drug or drug-excipients. The selection of appropriate co-formers is critical, and the surface properties of co-amorphous formulations must be carefully evaluated, as they influence physical and chemical stability in addition to dissolution performance. Scaling up and processing co-amorphous formulations into the final dosage forms presents challenges that need to be addressed. This review will largely concentrate on the challenges, improvements, and innovations in physicochemical properties, biological characterization, and advancements of co-amorphous systems. This review will also furnish a comprehensive explanation of both established and emerging approaches utilized in the estimation of physicochemical attributes and characterization of CASD (in vitro and in vivo). Regarding CASD's potential to improve patient outcomes and therapeutic efficacy, it has emerged as a viable approach for drug candidates posing the problems of solubility and bioavailability. This approach has also increased the physical stability of 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
CiteScore
2.40
自引率
0.00%
发文量
0
×
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:481959085
Book学术官方微信