Clinical significance of Rutin (RUT) is limited by poor dissolution rate and low oral bioavailability. The study was designed to improve the physicochemical and therapeutic potential of the drug by formulating nanosuspension (NS) for osteoporosis. Rutin nanosuspension (RUT-NS) was prepared after screening a range of stabilizers and their combinations at a different concentration by antisolvent precipitation technique. Effect of precipitation on crystallinity (differential scanning calorimetry DSC, X-ray diffraction studies XRD), morphology (scanning electron microscopy, SEM) and chemical interaction (attenuated total reflectance fourier-transform infrared spectroscopy ATR-FTIR) were studied through biophysical techniques. An optimized nanosuspension exhibited a minimum particle size of 122.85 ± 5.02 nm with higher dissolution of RUT-NS (87. 63 ± 2.29%) as compared to pure drug (39.77 ± 2.8 6%). The enhanced intestine absorption and apparent permeability were achieved due to the improved particle size, surface area and dissolution. RUT-NS displayed greater (3 folds) AUC_0–24 h than pure drug. In vitro assays with RUT-NS depicted an increased cell proliferation, antioxidant (ROS) activity and osteocalcin production in MG-63 osteoblast cells. The augmented biochemical in vivo biomarkers and bone quality proved the protective effect of RUT-NS. The results supported RUT-NS as a potential therapy for maintaining bone health.

芦丁（RUT）的临床意义受到不良的溶出度和低的口服生物利用度的限制。该研究旨在通过制定用于骨质疏松症的纳米悬浮液（NS）来提高药物的理化和治疗潜力。在通过反溶剂沉淀技术筛选了一系列不同浓度的稳定剂及其组合后，制备了芦丁纳米悬浮液（RUT-NS）。通过生物物理技术研究了沉淀对结晶度（差示扫描量热法DSC，X射线衍射研究XRD），形态学（扫描电子显微镜，SEM）和化学相互作用（衰减全反射傅里叶变换红外光谱ATR-FTIR）的影响。优化的纳米悬浮液的最小粒径为122.85±5.02 nm，RUT-NS的溶出度更高（87. 63±2。与纯药物（39.77±2.8 6％）相比，为29％）。由于粒径，表面积和溶出度提高，肠吸收和表观通透性提高。RUT-NS显示更大（3倍）AUC比纯药物_0-24小时。用RUT-NS进行的体外测定表明，MG-63成骨细胞中细胞增殖，抗氧化剂（ROS）活性和骨钙素产生增加。增强的体内生化标志物和骨质量证明了RUT-NS的保护作用。结果支持RUT-NS作为维持骨骼健康的潜在疗法。