Nanotechnology-Driven Therapeutic Potential of Raloxifene in Osteoporosis and Cancer: A Recent Review.

Abstract

Introduction: Osteoporosis (OP) is a prevalent condition in postmenopausal women, marked by reduced bone density and an increased risk of fractures. Raloxifene (RLX), a selective estrogen receptor modulator (SERM), is the only drug approved for the management of OP in this patient population. RLX works by mimicking estrogen's effects on bone, reducing bone resorption and thereby increasing bone mineral density. However, despite its benefits, conventional oral RLX formulations have significant limitations. Its low bioavailability and poor aqueous solubility are compounded by extensive first-pass metabolism, which significantly reduces the drug's efficacy. Recent research has focused on nanocarriers for RLX to overcome these challenges, with lipid-based nanocarriers emerging as a promising approach to improve solubility, enhance absorption, and bypass first-pass metabolism via lymphatic uptake.

Method: The authors gathered information about RLX from articles published up to 2025 and listed in Pub- Med, Web of Science, Elsevier, Google Scholar, and similar databases. The keywords used in our search included "Osteoporosis" "Raloxifene" "nanocarriers" etc. Results: The review of existing literature reveals substantial progress in developing innovative drug delivery systems for RLX, aimed at overcoming the limitations of conventional oral dosage forms in the treatment of OP and cancer. Several studies underscore the potential of novel formulations, including lipid-based nanocarriers, to improve raloxifene's pharmacokinetic profile, particularly through enhanced solubility, dissolution rate, and bioavailability.

Conclusion: The nanocarriers mediated raloxifene delivery represent promising strategies to enhance its bioavailability and therapeutic efficacy in osteoporosis treatment. By improving solubility and bypassing first-pass metabolism, these novel systems can potentially reduce dose-related side effects, offering safer and more effective long-term options for postmenopausal women with osteoporosis. This approach supports the continued exploration of both oral and non-oral delivery methods to overcome the limitations of conventional raloxifene formulations.