Alendronic acid modified PLGA drug delivery system loaded with 17β-Estradiol and vitamin D3 has anti-osteoporotic effect
Yonghui Wang, Sidi Zhang, Xinrun Ma, Donghao Hu, Junran Liu, Lu Wei, Xue Lei, Yan Hu, Fuyou Li, Yanhong Gao
TL;DR
A new drug delivery system targets bones to treat osteoporosis safely, avoiding side effects of traditional hormone therapy.
Contribution
A bone-targeted PLGA nanocarrier modified with alendronic acid co-delivers estradiol and vitamin D3 for safer osteoporosis treatment.
Findings
The nanocarrier significantly improved bone mineral density in ovariectomized mice.
It reduced endometrial thickening caused by estradiol and showed sustained drug release.
The combination enhanced osteogenesis via activation of the PI3K/AKT/mTOR signaling pathway.
Abstract
Postmenopausal osteoporosis caused by estrogen deficiency often requires hormone replacement therapy (HRT), but its systemic side effects limit clinical application. Here, we developed a bone-targeted Poly (lactic-co-glycolic acid) (PLGA) nanocarrier modified with Alendronic acid (ADA) to co-deliver 17β-Estradiol (E2) and Vitamin D3 (VitD3), aiming to enhance efficacy and safety. The ADA-functionalized nanoparticles (E2+VD@PLGAIR780ADA) showed high drug loading (7.2 wt% for E2 and 2.3 wt% for VitD3), sustained release (>90 % over 48 h). In ovariectomized (OVX) mice, targeted delivery significantly improved bone mineral density, restored trabecular structure, and reduced serum bone resorption markers, while markedly alleviating E2-induced endometrial thickening. In vivo imaging confirmed selective bone accumulation. Mechanistically, co-administration of VitD3 and E2 elicits enhanced…
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Taxonomy
TopicsBone health and osteoporosis research · Bone Metabolism and Diseases · Bone Tissue Engineering Materials