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Design and Development of A Commercially Viable <i>In Situ</i> Nanoemulgel for The Treatment of Postmenopausal Osteoporosis

Foziyah Zakir, Adil Ahmad, Uzma Farooq, Mohd. Aamir Mirza, Alok Tripathi, Divya Singh, Faiyaz Shakeel, Sradhanjali Mohapatra, Farhan Jalees Ahmad, Kanchan Kohli

2020Nanomedicine45 citationsDOI

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.

Topics & Concepts

BioavailabilityOsteoporosisRaloxifenePharmacodynamicsMedicineClinical efficacyIn vivoPharmacologyNasal administrationPharmacokineticsInternal medicineBiologyEstrogen receptorBiotechnologyCancerBreast cancerAdvanced Drug Delivery SystemsEstrogen and related hormone effectsNanoparticle-Based Drug Delivery
Design and Development of A Commercially Viable <i>In Situ</i> Nanoemulgel for The Treatment of Postmenopausal Osteoporosis | Litcius