Self Emulsifying Delivery System of Cissus quadrangularis: Evidence of Enhanced Efficacy and Promising Pharmacokinetic Profile in the Management of Osteoporosis

AAPS PharmSciTech. 2024 May 10;25(5):107. doi: 10.1208/s12249-024-02821-x.

Abstract

Treatment therapies used to manage osteoporosis are associated with severe side effects. So worldwide herbs are widely studied to develop alternative safe & effective treatments. Cissus quadrangularis (CQ) has a significant role in bone health and fracture healing. It is documented that its extracts increase osteoblastic differentiation & mineralization. Currently, Cissus quadrangularis is available in the form of tablets in the market for oral delivery. But these conventional forms are associated with poor bioavailability. There is a need for a novel drug delivery system with improving oral bioavailability. Therefore, a Cissus quadrangularis-loaded self-emulsifying drug delivery system (CQ-SEDDS) was developed which disperses rapidly in the gastrointestinal fluids, yielding nano-emulsions containing a solubilized drug. This solubilized form of the drug can be easily absorbed through lymphatic pathways and bypass the hepatic first-pass effect. The emulsification efficiency, zeta potential, globule size, in-vitro dissolution, ex-vivo, in-vivo and bone marker studies were performed to assess the absorption and permeation potential of CQ incorporated in SEDDS. CQ-SEDDS with excipients Tween 80, Cremophor RH40, Transcutol HP & α-Tocopherol acetate had shown about 76% enhancement in the bioavailability of active constituents of CQ. This study provided the pre-clinical data of CQ-SEDDS using osteoporotic rat model studies.

Keywords: cissus quadrangularis; animal studies; bioavailability; bone marker studies; nano-formulation; self-emulsifying drug delivery system.

MeSH terms

  • Administration, Oral
  • Animals
  • Biological Availability*
  • Cissus* / chemistry
  • Drug Delivery Systems* / methods
  • Emulsions*
  • Excipients / chemistry
  • Female
  • Osteoporosis* / drug therapy
  • Particle Size
  • Plant Extracts / administration & dosage
  • Plant Extracts / chemistry
  • Plant Extracts / pharmacokinetics
  • Rats
  • Rats, Sprague-Dawley
  • Solubility

Substances

  • Emulsions
  • Excipients
  • Plant Extracts