https://scholars.lib.ntu.edu.tw/handle/123456789/632847
標題: | Human serum albumin-based nanoparticles alter raloxifene administration and improve bioavailability | 作者: | Yang, Shu-Jyuan CHIH-HAO CHANG Young, Tai-Horng Wang, Chung-Hao TZU-HAO TSENG MAN-LING WANG |
關鍵字: | Osteoporosis; human serum albumin; nanoparticle; poly(sodium styrene sulfonate); raloxifene | 公開日期: | 十二月-2022 | 出版社: | TAYLOR & FRANCIS LTD | 卷: | 29 | 期: | 1 | 起(迄)頁: | 2685 | 來源出版物: | Drug delivery | 摘要: | Osteoporosis is a disease that reduces bone mass and microarchitecture, which makes bones fragile. Postmenopausal osteoporosis occurs due to estrogen deficiency. Raloxifene is a selective estrogen receptor modulator used to treat postmenopausal osteoporosis. However, it has a low bioavailability, which requires long-term, high-dose raloxifene administration to be effective and causes several side effects. Herein, raloxifene was encapsulated in human serum albumin (HSA)-based nanoparticles (Ral/HSA/PSS NPs) as an intravenous-injection pharmaceutical formulation to increase its bioavailability and reduce the treatment dosage and time. In vitro results indicated that raloxifene molecules were well distributed in HSA-based nanoparticles as an amorphous state, and the resulting raloxifene formulation was stabile during long-term storage duration. The Ral/HSA/PSS NPs were both biocompatible and hemocompatible with a decreased cytotoxicity of high-dose raloxifene. Moreover, the intravenous administration of the prepared Ral/HSA/PSS NPs to rats improved raloxifene bioavailability and improved its half-life in plasma. These raloxifene-loaded nanoparticles may be a potential nanomedicine candidate for treating postmenopausal osteoporosis with lower raloxifene dosages. |
URI: | https://scholars.lib.ntu.edu.tw/handle/123456789/632847 | ISSN: | 1071-7544 | DOI: | 10.1080/10717544.2022.2111479 |
顯示於: | 醫學系 |
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