Design and development of a commercially viable in situ nanoemulgel for the treatment of postmenopausal osteoporosis.

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.