Kesharwani Siddharth S, Sayre Casey L, Kesharwani Sharyu, Burrows Anna
College of Pharmacy, Roseman University of Health Sciences, South Jordan, UT, USA.
Division of Clinical Pharmacology, Pediatrics, School of Medicine, University of Utah, Salt Lake City, UT, USA.
Ther Deliv. 2025 Jul;16(7):651-660. doi: 10.1080/20415990.2025.2510889. Epub 2025 Jun 3.
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.
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.
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.
In summary, the study demonstrates the successful development of a polymer-quercetin complex with improved loading, solubility, stability, and targeted delivery properties.
槲皮素是一种天然膳食化合物，因其具有预防慢性疾病的潜力而闻名。然而，由于槲皮素口服生物利用度差，这一成果向人体的转化受到阻碍，其口服生物利用度差归因于其极低的水溶性和渗透性。这些挑战影响了槲皮素的口服吸收。
目前的工作描述了一种基于聚合物的平台，专门用于将槲皮素递送至结肠。采用共沉淀法制备槲皮素复合物。所使用的聚合物为尤特奇® S100/L100/L100-55。在复合物形成过程中，乙醇和聚乙烯醇分别作为溶剂和表面活性剂。
形成的聚合物复合物显示出高负载量，槲皮素的负载量达到约315μg/mL。所获得的复合物在固态时为无定形，可溶于pH值>5.5的缓冲液中。所得的槲皮素-尤特奇®复合物的水溶性显著增加，浓度>1mg/mL。与槲皮素相比，聚合物复合物在水溶液中30多小时内更稳定。与槲皮素相比，溶解的槲皮素-尤特奇®制剂在结肠癌细胞HCT116和HT29中显示出细胞活力的降低增强。
总之，该研究证明成功开发了一种具有改善的负载、溶解性、稳定性和靶向递送特性的聚合物-槲皮素复合物。
