Revisiting Ipriflavone: a Potential Isoflavone for the Management of Postmenopausal Osteoporosis

• Published in: Revista brasileira de farmacognosia 2021-12, Vol.31 (6), p.733-740
• Main Authors: John, Anish, V, Anoop Narayanan, Konkodi, Kiran
• Format: Article
• Language: English
• Subjects: Medicine; Pharmacy; Review
• ISSN: 1981-528X; 1981-528X
• DOI: 10.1007/s43450-021-00192-z

Ipriflavone is a nutraceutical extensively used in Asian countries since 1890 for postmenopausal osteoporosis as a phytoestrogen to inhibit bone resorption, to maintain bone density, and to prevent osteoporosis in postmenopausal women. The drug has shown effectiveness in some preliminary animal experiments, clinical investigations, and cell lines in vitro . Though it is non-estrogenic, the exact mechanism for supporting bone development is unknown. Ipriflavone is considered a selective estrogen receptor modulator and supports the growth of osteoblasts and regulates the multiplication of osteoclasts. The poor aqueous solubility of this molecule is one of the critical parameters that has promoted the exploration for effective novel formulations. Only a few solubility improvement attempts have been reported so far on ipriflavone. After gastrointestinal absorption, this synthetic isoflavone transforms into metabolites that are not well studied for their pharmacokinetic and pharmacodynamic properties. This mini-review aims to summarize the fundamental properties, solubility challenges, and preclinical and clinical developments of ipriflavone to date. Graphical abstract