Development and evaluation of novel oral formulation of cissus quadrangularis for osteoporosis

Abstract

The occurrence of osteoporosis increases day by day. But the traditional therapies are associated with severe side effects. So worldwide herbs are widely studied to develop alternative safe and effective treatments. Cissus quadrangularis (CQ) is a perennial climber which has a significant role in bone health and fracture healing. It is documented that its extracts increase osteoblastic differentiation and mineralization. For a long time, CQ is available in the form of tablets in the market. But these conventional forms are associated with poor bioavailability/efficacy. Its bioavailability is about 35% due to many reasons. So, there was a need to develop a novel drug delivery system that possesses unmatched potential in improving oral bioavailability. Therefore, a CQ-loaded self-emulsifying drug delivery system (CQ-SEDDS) and a food- grade nano-emulsion (CQ-NE) were developed. SEDDS disperses rapidly in the gastrointestinal fluids, yielding nano- emulsions containing a solubilized drug which absorbed through lymphatic pathways and bypass the hepatic first-pass effect. The optimized CQ-SEDDS with excipients Tween 80, Cremophor RH 40, Transcutol HP and -Tocopherol acetate showed about 76% enhancement in the bioavailability of active constituents of CQ. The Globule size, in-vitro dissolution, ex-vivo and in-vivo (pharmacokinetics) studies as well as spectroscopic and microscopic studies of CQ-SEDDS and CQ-NE were performed to assess the intestinal absorption and permeation potential of CQ. Further CQ-NE- loaded functional milk beverage was developed which was evaluated by sensory. The efficacy of CQ-SEDDS and CQ- NE-functional milk beverage was further evaluated by the osteoporotic rat model and bone marker studies and satisfactory results were obtained. newline