Siddharth S Kesharwani, Casey L Sayre, Sharyu Kesharwani, Anna Burrows
{"title":"Quercetin-Eudragit® polymer complexes with enhanced loading, solubility, stability, and site-specific targeting.","authors":"Siddharth S Kesharwani, Casey L Sayre, Sharyu Kesharwani, Anna Burrows","doi":"10.1080/20415990.2025.2510889","DOIUrl":null,"url":null,"abstract":"<p><strong>Aim: </strong>Quercetin is a natural dietary compound known for its potential to prevent chronic diseases. However, the translation of this success to humans is hindered due to quercetin's poor oral bioavailability, attributed to its extremely low water solubility and permeability. These challenges affect the oral absorption of quercetin.</p><p><strong>Methods: </strong>The current work describes a polymer-based platform specifically targeted for the delivery of quercetin to the colon. Quercetin complexes were prepared using co-precipitation. The polymers used are Eudragit® S100/L100/L100-55. Ethanol and polyvinyl alcohol are the solvent and surfactant respectively in the complex formation process.</p><p><strong>Results: </strong>The formed polymer complexes demonstrate a high loading capacity, reaching approximately 315 μg/mL of quercetin. The complexes obtained were amorphous in the solid state and soluble in buffer with pHs > 5.5. The resulting Quercetin-Eudragit® complexes demonstrate significantly increased aqueous solubility, reaching concentrations > 1 mg/mL. The polymer complexes were more stable for > 30 h in aqueous solutions compared to quercetin. The solubilized Quercetin-Eudragit® formulations demonstrated enhanced reduction in cell viability in colon cancer cells HCT116 and HT29 when compared to quercetin.</p><p><strong>Conclusions: </strong>In summary, the study demonstrates the successful development of a polymer-quercetin complex with improved loading, solubility, stability, and targeted delivery properties.</p>","PeriodicalId":22959,"journal":{"name":"Therapeutic delivery","volume":" ","pages":"1-10"},"PeriodicalIF":3.0000,"publicationDate":"2025-06-03","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"0","resultStr":null,"platform":"Semanticscholar","paperid":null,"PeriodicalName":"Therapeutic delivery","FirstCategoryId":"1085","ListUrlMain":"https://doi.org/10.1080/20415990.2025.2510889","RegionNum":0,"RegionCategory":null,"ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"Q2","JCRName":"PHARMACOLOGY & PHARMACY","Score":null,"Total":0}
引用次数: 0
Abstract
Aim: Quercetin is a natural dietary compound known for its potential to prevent chronic diseases. However, the translation of this success to humans is hindered due to quercetin's poor oral bioavailability, attributed to its extremely low water solubility and permeability. These challenges affect the oral absorption of quercetin.
Methods: The current work describes a polymer-based platform specifically targeted for the delivery of quercetin to the colon. Quercetin complexes were prepared using co-precipitation. The polymers used are Eudragit® S100/L100/L100-55. Ethanol and polyvinyl alcohol are the solvent and surfactant respectively in the complex formation process.
Results: The formed polymer complexes demonstrate a high loading capacity, reaching approximately 315 μg/mL of quercetin. The complexes obtained were amorphous in the solid state and soluble in buffer with pHs > 5.5. The resulting Quercetin-Eudragit® complexes demonstrate significantly increased aqueous solubility, reaching concentrations > 1 mg/mL. The polymer complexes were more stable for > 30 h in aqueous solutions compared to quercetin. The solubilized Quercetin-Eudragit® formulations demonstrated enhanced reduction in cell viability in colon cancer cells HCT116 and HT29 when compared to quercetin.
Conclusions: In summary, the study demonstrates the successful development of a polymer-quercetin complex with improved loading, solubility, stability, and targeted delivery properties.
期刊介绍：
Delivering therapeutics in a way that is right for the patient - safe, painless, reliable, targeted, efficient and cost effective - is the fundamental aim of scientists working in this area. Correspondingly, this evolving field has already yielded a diversity of delivery methods, including injectors, controlled release formulations, drug eluting implants and transdermal patches. Rapid technological advances and the desire to improve the efficacy and safety profile of existing medications by specific targeting to the site of action, combined with the drive to improve patient compliance, continue to fuel rapid research progress. Furthermore, the emergence of cell-based therapeutics and biopharmaceuticals such as proteins, peptides and nucleotides presents scientists with new and exciting challenges for the application of therapeutic delivery science and technology. Successful delivery strategies increasingly rely upon collaboration across a diversity of fields, including biology, chemistry, pharmacology, nanotechnology, physiology, materials science and engineering. Therapeutic Delivery recognizes the importance of this diverse research platform and encourages the publication of articles that reflect the highly interdisciplinary nature of the field. In a highly competitive industry, Therapeutic Delivery provides the busy researcher with a forum for the rapid publication of original research and critical reviews of all the latest relevant and significant developments, and focuses on how the technological, pharmacological, clinical and physiological aspects come together to successfully deliver modern therapeutics to patients. The journal delivers this essential information in concise, at-a-glance article formats that are readily accessible to the full spectrum of therapeutic delivery researchers.
求助内容：
应助结果提醒方式：
京公网安备 11010802042870号
