Abstract
Aim: To investigate the potential of a thermosensitive intranasal formulation of raloxifene hydrochloride (RH) for systemic delivery with the possibility of enhanced bioavailability and anti-osteoporotic efficacy. Methods: In this work, a commercially scalable nanoemulsion in thermosensitive gel, aligned with better clinical acceptability, has been developed and evaluated. Results: A significant 7.4-fold improvement in bioavailability of RH was recorded when compared with marketed tablets. Likewise, in vivo pharmacodynamics studies suggested 162% enhanced bone density and significantly improved biochemical markers compared with per-oral marketed tablet. Conclusion: The formulation, being safe and patient compliant, successfully tuned anti-osteoporotic effects with improved therapeutic performance. Further, the work provided an exceptional lead to carry out the study in clinical settings.
Graphical abstract