Design and Development of A Commercially Viable In Situ Nanoemulgel for The Treatment of Postmenopausal Osteoporosis

作者：Foziyah Zakir, Adil Ahmad, Uzma Farooq, Mohd. Aamir Mirza, Alok Tripathi, Divya Singh, Faiyaz Shakeel, Sradhanjali Mohapatra, Farhan Jalees Ahmad, Kanchan Kohli · 发表于：Nanomedicine · 年份：2020 · DOI：10.2217/nnm-2020-0079 · 被引用次数：45 · 研究领域：Advanced Drug Delivery Systems、Estrogen and related hormone effects、Nanoparticle-Based Drug Delivery

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.