橙皮苷(Hsd),生物活性植物药,与1型和2型糖尿病相比,经历了抗糖尿病活性。然而,其固有的不良溶解度和生物利用度是反映其口服给药的关键挑战性障碍。从这样的角度来看,本研究的目的是制备和评估负载Hsd的磺丁基醚-β-环糊精/壳聚糖纳米颗粒(Hsd/CD/CSNP),以改善口服Hsd的降血糖活性。Hsd首先与磺丁基醚-β-环糊精(SBE-β-CD)络合,发现形成的络合物(CX)具有50.53±1.46和84.52±3.16%的络合效率百分比和工艺效率百分比,分别。此外,复合物的固态表征确保了SBE-β-CD腔内包含Hsd。然后,使用离子凝胶技术制备Hsd/CD/CSNPs。对所制备的NP进行充分表征,以选择具有455.7±9.04nm均匀粒径的最有前途的NP(F1),正zeta电位为+32.28±1.12mV,包封率为77.46±0.39%。最佳配方(F1)进行了进一步的体外释放研究,离体肠道渗透,稳定性,细胞毒性,和体内降血糖活性。F1的释放和渗透研究的结果表明了Hsd和CX之间的调节模式。在4±1°C下观察到F1的优先稳定性。此外,F1与口腔上皮细胞系(OEC)的生物相容性保留至100µg/mL的浓度.在口服施用F1后,记录到显著的协同降血糖作用,血糖水平降低直至实验结束。总之,Hsd/CD/CSNP可被视为具有增强的抗糖尿病活性的Hsd的有希望的口服递送系统。
Hesperidin (Hsd), a bioactive phytomedicine, experienced an antidiabetic activity versus both Type 1 and Type 2 Diabetes mellitus. However, its intrinsic poor solubility and bioavailability is a key challenging obstacle reflecting its oral delivery. From such perspective, the purpose of the current
study was to prepare and evaluate Hsd-loaded sulfobutylether-β-cyclodextrin/chitosan nanoparticles (Hsd/CD/CS NPs) for improving the hypoglycemic activity of the orally administered Hsd. Hsd was first complexed with sulfobutylether-β-cyclodextrin (SBE-β-CD) and the complex (CX) was found to be formed with percent complexation efficiency and percent process efficiency of 50.53 ± 1.46 and 84.52 ± 3.16%, respectively. Also, solid state characterization of the complex ensured the inclusion of Hsd inside the cavity of SBE-β-CD. Then, Hsd/CD/CS NPs were prepared using the ionic gelation technique. The prepared NPs were fully characterized to select the most promising one (F1) with a homogenous particle size of 455.7 ± 9.04 nm, a positive zeta potential of + 32.28 ± 1.12 mV, and an entrapment efficiency of 77.46 ± 0.39%. The optimal formula (F1) was subjected to further investigation of in vitro release, ex vivo intestinal
permeation, stability, cytotoxicity, and in vivo hypoglycemic activity. The results of the release and
permeation studies of F1 manifested a modulated pattern between Hsd and CX. The preferential stability of F1 was observed at 4 ± 1 °C. Also, the biocompatibility of F1 with oral epithelial cell line (OEC) was retained up to a concentration of 100 µg/mL. After oral administration of F1, a noteworthy synergistic hypoglycemic effect was recorded with decreased blood glucose level until the end of the experiment. In conclusion, Hsd/CD/CS NPs could be regarded as a hopeful oral delivery system of Hsd with enhanced antidiabetic activity.