Department of Pharmacology, School of Medicine, Tehran University of Medical Sciences, Tehran, Iran.
Dental Research Center, Dentistry Research Institute, Tehran University of Medical Sciences, Tehran, Iran.
Nanomedicine. 2020 Oct;29:102273. doi: 10.1016/j.nano.2020.102273. Epub 2020 Jul 22.
Phosphatidylserine nanocochleates (Nanocochs) are novel delivery systems that may play a prominent osteoprotective role with their cargo, vitamin D3 (Vit-D3), against osteoporosis. Therefore, this study was conducted to characterize a Nanococh containing vitamin D3 (Nanococh-D3) and investigate its potential role in improving GIO in a rat model. Roll-shaped Nanococh-D3 particles were obtained in a size range of 320 nm with a sustained release performance. Oral Nanococh-D3 significantly increased the bioavailability of Vit-D3, enhanced bone mechanical strength, and improved osteogenic biomarkers including B-ALP, osteocalcin, Ca, and OPG in GIO rats. This formulation markedly suppressed gene expression of RANK and RANKL in treated rats. Histomorphometric analysis showed significant repairs in bone tissues and TRAP staining indicated a significant decrease in osteoclasts using Nanococh-D3 in osteoporotic rats. Nanococh alone similar to Nanococh-D3 acted better than AL as a standard anti-osteoporotic drug in the improvement of bone strength. In conclusion, our results established the potential role of Nanococh-D3 against osteoporosis in rats.
磷脂酰丝氨酸纳米耳蜗（Nanocochs）是新型的递送系统，其携带的货物维生素 D3（Vit-D3）可能对骨质疏松症发挥显著的护骨作用。因此，本研究旨在对载有维生素 D3 的纳米耳蜗（Nanococh-D3）进行表征，并研究其在改善大鼠模型中的糖皮质激素诱导骨质疏松症（GIO）中的潜在作用。得到了尺寸范围在 320nm 左右的、具有持续释放性能的卷状 Nanococh-D3 颗粒。口服 Nanococh-D3 显著提高了 Vit-D3 的生物利用度，增强了骨机械强度，并改善了 GIO 大鼠的成骨生物标志物，包括 B-ALP、骨钙素、Ca 和 OPG。该配方显著抑制了治疗大鼠中 RANK 和 RANKL 的基因表达。组织形态计量学分析显示，使用 Nanococh-D3 可显著修复骨组织，TRAP 染色表明骨质疏松大鼠的破骨细胞数量显著减少。纳米耳蜗本身与 Nanococh-D3 一样，在改善骨强度方面优于作为标准抗骨质疏松药物的 AL。总之，我们的研究结果确立了 Nanococh-D3 在大鼠对抗骨质疏松症方面的潜在作用。
