Drug Delivery (Dec 2022)

Human serum albumin-based nanoparticles alter raloxifene administration and improve bioavailability

  • Shu-Jyuan Yang,
  • Chih-Hao Chang,
  • Tai-Horng Young,
  • Chung-Hao Wang,
  • Tzu-Hao Tseng,
  • Man-Ling Wang

DOI
https://doi.org/10.1080/10717544.2022.2111479
Journal volume & issue
Vol. 29, no. 1
pp. 2685 – 2693

Abstract

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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.

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