Development of a self-microemulsifying drug delivery system of raloxifene for enhanced oral bioavailability

Alam Zeb – Research Associate Professor, College of Pharmacy, Hanyang University ERICA, Ansan, Republic of Korea; Muhammad Mohsin Ansari – Associate Professor, Riphah Institute of Pharmaceutical Sciences, Riphah International University, Islamabad, Pakistan; Ho-Ik Choi – Postdoc, College of Pharmacy, Hanyang University ERICA, Ansan, Republic of Korea; Jeong-Su Ryu – Student, College of Pharmacy, Hanyang University ERICA, Ansan, Republic of Korea; Ha-Yeon Noh – Student, College of Pharmacy, Hanyang University ERICA, Ansan, Republic of Korea; Min-Ju Kim – Student, College of Pharmacy, Hanyang University ERICA, Ansan, Republic of Korea; Se-Yun Kim – Student, College of Pharmacy, Hanyang University ERICA, Ansan, Republic of Korea; Hoseung Han – Student, College of Pharmacy, Hanyang University ERICA, Ansan, Republic of Korea

Introduction: Raloxifene hydrochloride (RLX) is a Biopharmaceutics Classification System (BCS) class II drug, and it is widely used to protect postmenopausal women from breast cancer and osteoporosis by functioning as an estrogen antagonist and agonist in the breast and bone tissues, respectively. Owing to its poor aqueous solubility, RLX exhibits extremely low oral bioavailability in humans (< 2%) and rats (~39%).This study was aimed to develop RLX-loaded self-microemulsifying drug delivery system (RLX-SMEDDS) for enhancing its solubility, dissolution and oral bioavailability.