Almukainzi May, El-Masry Thanaa A, El Zahaby Enas I, El-Nagar Maysa M F
Department of Pharmaceutical Sciences, College of Pharmacy, Princess Nourah bint Abdulrahman University, P.O. Box 84428, Riyadh 11671, Saudi Arabia.
Department of Pharmacology and Toxicology, Faculty of Pharmacy, Tanta University, Tanta 31527, Egypt.
Pharmaceuticals (Basel). 2024 Jul 29;17(8):999. doi: 10.3390/ph17080999.
One flavonoid glycoside with demonstrated therapeutic potential for several illnesses, including cancer, is hesperidin. However, because of its limited bioavailability and solubility, it is only marginally absorbed, necessitating a delivery mechanism to reach the intended therapeutic target. Additionally, the cytoskeleton of crustaceans yields chitosan, a naturally occurring biopolymer with mucoadhesive properties that has been used to improve the absorption of advantageous chemical substances like flavonoids. Chitosan/hesperidin nanoparticles (Hes-Nanoparticles) were made using the ion gelation technique. The synthesis of Hes-Nanoparticles was confirmed by several characterization methods, including the swelling test, zeta potential, particle size, FTIR, XRD, TEM, and SEM. DPPH and ABTS were used to demonstrate radical scavenging activity in antioxidant assays of chitosan, hesperidin, and the synthesized Hes-Nanoparticles. In addition, by a viability assay against MDA-MB-231, the anticancer efficacies of chitosan, hesperidin, and the synthesized Hes-Nanoparticles were assessed. Furthermore, annexin-V/PI double staining and the cycle of cell analysis were determined by flow cytometry. The results displayed that Hes-Nanoparticles have higher antioxidant activity than chitosan and hesperidin alone. Also, it has been demonstrated that Hes-Nanoparticles are more effective in early cell cycle arrest, suppressing the viability of cancer cells, and increasing cell apoptosis than chitosan and hesperidin alone. In conclusion, Hes-Nanoparticles demonstrated more antioxidant and antitumor activities than chitosan and hesperidin alone. Moreover, it has been established that Hes-Nanoparticles, in a highly soluble form, increase activity in contrast to the poorly soluble form of hesperidin alone.
橙皮苷是一种黄酮类糖苷,对包括癌症在内的多种疾病具有已被证实的治疗潜力。然而,由于其生物利用度和溶解度有限,它仅能被少量吸收,因此需要一种递送机制来达到预期的治疗靶点。此外,甲壳类动物的细胞骨架可产生壳聚糖,这是一种具有粘膜粘附特性的天然生物聚合物,已被用于改善黄酮类等有益化学物质的吸收。采用离子凝胶化技术制备了壳聚糖/橙皮苷纳米颗粒(橙皮苷纳米颗粒)。通过多种表征方法,包括溶胀试验、zeta电位、粒径、傅里叶变换红外光谱(FTIR)、X射线衍射(XRD)、透射电子显微镜(TEM)和扫描电子显微镜(SEM),证实了橙皮苷纳米颗粒的合成。在壳聚糖、橙皮苷和合成的橙皮苷纳米颗粒的抗氧化测定中,使用二苯基苦味酰基自由基(DPPH)和2,2'-联氮-双-3-乙基苯并噻唑啉-6-磺酸(ABTS)来证明自由基清除活性。此外,通过针对人乳腺癌细胞系MDA-MB-231的活力测定,评估了壳聚糖、橙皮苷和合成的橙皮苷纳米颗粒的抗癌效果。此外,通过流式细胞术测定膜联蛋白-V/碘化丙啶(PI)双染和细胞周期分析。结果显示,橙皮苷纳米颗粒比单独的壳聚糖和橙皮苷具有更高的抗氧化活性。此外,已证明橙皮苷纳米颗粒在早期细胞周期阻滞、抑制癌细胞活力和增加细胞凋亡方面比单独的壳聚糖和橙皮苷更有效。总之,橙皮苷纳米颗粒比单独的壳聚糖和橙皮苷表现出更强的抗氧化和抗肿瘤活性。此外,已经确定,与单独的难溶性橙皮苷相比,高度可溶形式的橙皮苷纳米颗粒能提高活性。