Sunoqrot Suhair, Alkurdi Malak, Al Bawab Abdel Qader, Hammad Alaa M, Tayyem Rabab, Abu Obeed Ali, Abufara Mohammed
Department of Pharmacy, Faculty of Pharmacy, Al-Zaytoonah University of Jordan, Amman 11733, Jordan.
ACDIMA Biocenter, Amman 11190, Jordan.
Saudi Pharm J. 2023 Jun;31(6):845-853. doi: 10.1016/j.jsps.2023.04.010. Epub 2023 Apr 15.
Morin (3,5,7,2',4'-pentahydroxyflavone; MR) is a bioactive plant polyphenol whose therapeutic efficacy is hindered by its poor biopharmaceutical properties. The purpose of this study was to develop a nanoparticle (NP) formulation to enhance the bioactivity and oral bioavailability of MR. The nanoprecipitation technique was employed to encapsulate MR in lipid-cored poly(lactide-co-glycolide) (PLGA) NPs. The optimal NPs were about 200 nm in size with an almost neutral surface charge and a loading efficiency of 82%. The NPs exhibited sustained release of MR within 24 h. In vitro antioxidant assays showed that MR encapsulation did not affect its antioxidant activity. On the other hand, anti-inflammatory assays in lipopolysaccharide-stimulated macrophages revealed a superior anti-inflammatory activity of MR NPs compared to free MR. Furthermore, oral administration of MR NPs to mice at a single dose of 20 mg/kg MR achieved a 5.6-fold enhancement in bioavailability and a prolongation of plasma half-life from 0.13 to 0.98 h. The results of this study present a promising NP formulation for MR which can enhance its oral bioavailability and bioactivity for the treatment of different diseases such as inflammation.
桑色素（3,5,7,2',4'-五羟基黄酮；MR）是一种具有生物活性的植物多酚，但其较差的生物药剂学性质阻碍了其治疗效果。本研究的目的是开发一种纳米颗粒（NP）制剂，以提高MR的生物活性和口服生物利用度。采用纳米沉淀技术将MR包裹在脂质核心的聚（丙交酯-共-乙交酯）（PLGA）纳米颗粒中。最佳纳米颗粒大小约为200nm，表面电荷几乎呈中性，负载效率为82%。纳米颗粒在24小时内实现了MR的缓释。体外抗氧化试验表明，包裹MR不影响其抗氧化活性。另一方面，在脂多糖刺激的巨噬细胞中进行的抗炎试验显示，与游离MR相比，MR纳米颗粒具有更强的抗炎活性。此外，以20mg/kg MR的单剂量给小鼠口服MR纳米颗粒，生物利用度提高了5.6倍，血浆半衰期从0.13小时延长至0.98小时。本研究结果为MR提供了一种有前景的纳米颗粒制剂，可提高其口服生物利用度和生物活性，用于治疗炎症等不同疾病。
