CHIH-HAO CHANGYang, Shu-JyuanShu-JyuanYangYao, Wei-ChengWei-ChengYaoYOUNG, TAI-HORNGTAI-HORNGYOUNG2025-09-302025-09-302024https://scholars.lib.ntu.edu.tw/handle/123456789/732590Owing to its promising advantages, including improved drug bioavailability and therapeutic efficiency at low doses and frequency, increased patient convenience and compliance, and prolonged storage life, nanomedicine has received heightened attention over conventional pharmaceuticals. Human serum albumin (HSA)-based nanoparticles have been used as drug carriers in injectable formulations, with great success and versatility. In this study, raloxifene and vitamin D3 were co-encapsulated in HSA-based nanoparticles (Ral/VitaD/HSA/PSS NPs) as an intravenously injected pharmaceutical formulation in order to enhance their bioavailability in the body. The lyophilization–hydration method was utilized to develop the Ral/VitaD/HSA/PSS NPs. In addition, the characteristics and stability of the NP and the effect of the co-loading of vitamin D3 on raloxifene release in vitro and in vivo were discussed. The raloxifene and vitamin D3 molecules were successfully encapsulated and well dispersed in an amorphous state within Ral/VitaD/HSA/PSS NPs. The prepared Ral/VitaD/HSA/PSS NPs were lyophilized for long-term storage and were both biocompatible and hemocompatible, enhancing alkaline phosphtase activity in osteoblasts. Delivered via intravenous injection, Ral/VitaD/HSA/PSS NPs improved the bioavailability and residence time of raloxifene and vitamin D3 in the body at reduced dosages. Overall, the established raloxifene–vitamin D3-co-loaded NPs may be a potential nanomedicine contender for treating postmenopausal osteoporosis. © 2024, The Authors. All rights reserved.enHuman serum AlbuminNanomedicineOsteoporosisraloxifenevitamin D3[SDGs]SDG2other10.2139/ssrn.49538722-s2.0-85209457504