期刊
NANO LETTERS
卷 21, 期 19, 页码 7998-8007出版社
AMER CHEMICAL SOC
DOI: 10.1021/acs.nanolett.1c02150
关键词
osteoporosis; polymer vesicles; bone-targeting; self-assembly
类别
资金
- National natural science foundation of China [21925505, 22075212, 2210010521]
- Shanghai International Scientific Collaboration Fund [21520710100]
- National Science Fund for Distinguished Young Scholars
- China Postdoctoral Science Foundation [2020M671197]
This study presents a biomimicking polymer vesicle for bone-targeted delivery of beta-estradiol, which showed enhanced therapeutic effect in reversing bone loss in osteoporosis rat models. The vesicle, self-assembled from a specific diblock copolymer, demonstrated a high bone affinity and synergistic effects with E-2. This work offers new insights into the treatment of osteoporosis.
With the aging of the population, postmenopausal osteoporosis becomes increasingly widespread and severe as fractures caused by osteoporosis may lead to permanent disabilities and even death. Inspired by extracellular vesicles that participate in bone remodeling, we present a biomimicking polymer vesicle for bone-targeted beta-estradiol (E-2) delivery. This vesicle is self-assembled from a poly(epsilon-caprolactone)(28)-block-poly[(L-glutamic acid)(7)-stat-(L-glutamic acid-alendronic acid)(4)] (PCL28-b-P[Glu(7)-stat-(Glu-ADA)(4)]) diblock copolymer. The alendronic acid (ADA) on the coronas endows the polymer vesicles with a high bone affinity and acts synergistically with E-2 to achieve an enhanced therapeutic effect. As confirmed with ovariectomized osteoporosis rat models, bone loss was significantly reversed as the recovery rates of total BMD (bone mineral density) and trabecular BMD were 70.4% and 99.3%, respectively. Overall, this work provides fresh insight into the treatment of osteoporosis.
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