Gera Sonia, Sampathi Sunitha, Maddukuri Sravya, Dodoala Sujatha, Junnuthula Vijayabhaskarreddy, Dyawanapelly Sathish
Department of Pharmaceutics, National Institute of Pharmaceutical Education and Research (NIPER), Hyderabad 500037, India.
GITAM School of Pharmacy, GITAM Deemed to Be University, Rudraram, Hyderabad 502329, India.
Pharmaceutics. 2022 Jul 11;14(7):1449. doi: 10.3390/pharmaceutics14071449.
Naringenin (NRG) is a flavonoid and has been reported as an anti-osteoporotic agent. However, poor bioavailability may limit the anti-osteoporotic potential of the drug. The purpose of the study was to compare the anti-osteoporotic activity of naringenin nanosuspension (NRG-NS) with the NRG and standard therapeutic drug, raloxifene hydrochloride (RLX). Here, NRG-NS showed anti-osteoporotic activity in MG-63 cells by upregulating the osteocalcin levels. The in vivo anti-osteoporotic activity of NRG-NS was further investigated in an osteoporotic rat model to mimic the post-menopausal condition. The animals were randomized and separated into six groups. The animals were treated with RLX (p.o., 5.4 mg/kg), NRG (p.o., 20 mg/kg), NRG-NS (p.o., 20 mg/kg), and blank-NS for 60 days after completion of a 30-day post-surgery period and compared with control and ovariectomized (OVX) groups. After the treatment, body and uterine weights, biochemical estimation in serum (calcium, phosphorus, acid phosphatase, alkaline phosphatase, osteocalcin), bone parameters (length, diameter, dry weight, density, ash weight, bone mineral content) and bone microarchitecture by histopathology were determined. The results showed the protective effects of NRG-NS on osteoblast-like MG-63 cells. The biochemical estimations confirmed the normalization of parameters viz., alkaline phosphatase, calcium concentrations, and bone density with a decrease in levels of acid phosphatase and inorganic phosphorus with NRG-NS as compared to plain NRG. The results indicated that the oral administration of NRG-NS could be a potential therapeutic formulation for the treatment of osteoporosis.
柚皮素（NRG）是一种黄酮类化合物，已被报道为一种抗骨质疏松药物。然而，较差的生物利用度可能会限制该药物的抗骨质疏松潜力。本研究的目的是比较柚皮素纳米混悬液（NRG-NS）与柚皮素及标准治疗药物盐酸雷洛昔芬（RLX）的抗骨质疏松活性。在此，NRG-NS通过上调骨钙素水平在MG-63细胞中显示出抗骨质疏松活性。为模拟绝经后状况，在骨质疏松大鼠模型中进一步研究了NRG-NS的体内抗骨质疏松活性。将动物随机分为六组。在为期30天的手术后阶段结束后，对动物分别用RLX（口服，5.4 mg/kg）、NRG（口服，20 mg/kg）、NRG-NS（口服，20 mg/kg）和空白纳米混悬液处理60天，并与对照组和去卵巢（OVX）组进行比较。处理后，测定体重和子宫重量、血清生化指标（钙、磷、酸性磷酸酶、碱性磷酸酶、骨钙素）、骨参数（长度、直径、干重、密度、灰重、骨矿物质含量）以及通过组织病理学观察的骨微结构。结果显示NRG-NS对成骨样MG-63细胞具有保护作用。生化测定证实了各项参数的正常化，即碱性磷酸酶、钙浓度和骨密度正常化，与普通NRG相比，NRG-NS使酸性磷酸酶和无机磷水平降低。结果表明，口服NRG-NS可能是一种治疗骨质疏松症的潜在治疗制剂。
