Targeting osteoporosis: Rutin-loaded proniosomes and their role in OPG/RANKL modulation in ovariectomized rats

The current study aimed to investigate effect of Rutin loaded proniosomes on ovariectomized female rats for the treatment of osteoporosis. Rutin-loaded proniosomes (Rutin-PNs) were developed using coacervation phase separation method. The developed Rutin-PNs was characterised by determining its entrapment efficiency percentage (EE%), particle size (PS), zeta potential (ZP) and in-vitro release profiles. <i>In-vivo</i> study was performed for one month on female albino rats to study the effect of Rutin-PNs on Osteoprotegerin (OPG), Bone morphogenetic proteins (BMP2) and its receptor Smad-1(Suppressor of mothers against decapentaplegic), Receptor activator of nuclear factor kappa-Β ligand (RANKL) and bone metabolism marker as Alkaline phosphatase (ALP). The developed PNs exhibited high EE% that ranged from 65.85 ± 2.34 to 91.25 ± 2.41%, with PS of 371.3 ± 4.4 to 533.8 ± 5.73 nm, and ZP values from -22.1 ± 6.21 to -40.7 ± 7.21 mV. <i>In-vivo</i> study revealed the efficiency of Rutin-PNs formulation in improving the bone trabecula thickness and denseness <i>via</i> elevating OPG, Smad-1, and BMP2 values with reduction in the RANKL and ALP values. Thus, we can conclude that the developed Rutin-PNs has enhanced the anti-osteoporotic activity of rutin. Moreover, it could be considered as an alternative therapeutic agent for the management of postmenopausal osteoporosis.