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Nobiletin-loaded micelles reduce ovariectomy-induced bone loss by suppressing osteoclastogenesis
Yabing Wang1, Jian Xie1, Zexin Ai2
1Department of Prosthodontics, School & Hospital of Stomatology, Tongji University, Shanghai Engineering Research Center of Tooth Restoration and Regeneration, Shanghai 200072, People's Republic of China.
Background:
Nobiletin (NOB), a polymethoxy flavonoid, possesses anti-cancer and anti-inflammatory activities, has been reported that it played role in anti-osteoporosis treatment. However, previous research did not focus on practical use due to lack of hydrophilicity and cytotoxicity at high concentrations. The aim of this study was to develop a therapeutic formulation for osteoporosis based on the utilization of NOB.
Methods:
In this study, NOB-loaded poly(ethylene glycol)-block-poly(e-caprolactone) (NOB-PEG-PCL) was prepared by dialysis method. The effects on osteoclasts and anti-osteoporosis functions were investigated in a RANKL-induced cell model and ovariectomized (OVX) mice.
Results:
Dynamic light scattering and transmission electron microscopy examination results revealed that the NOB-PEG-PCL had a round shape, with a mean diameter around 124 nm. The encapsulation efficiency and drug loading were 76.34±3.25% and 7.60±0.48%, respectively. The in vitro release of NOB from NOB-PEG-PCL showed a remarkably sustained releasing characteristic and could be retained at least 48 hrs in pH 7.4 PBS. Anti-osteoclasts effects demonstrated that the NOB-PEG-PCL significantly inhibited the formation of tartrate-resistant acid phosphatase (TRAP)-positive multinuclear cells stimulated by RANKL. Furthermore, the NOB-PEG-PCL did not produce cytotoxicity on bone marrow-derived macrophages (BMMs). The mRNA expressions of genetic markers of osteoclasts including TRAP and cathepsin K were significantly decreased in the presence of NOB-PEG-PCL. In addition, the NOB-PEG-PCL inhibited OC differentiation of BMMs through RANKL-induced MAPK signal pathway. After administration of the NOB-PEG-PCL, NOB-PEG-PCL prevented bone loss and improved bone density in OVX mice. These findings suggest that NOB-PEG-PCL might have great potential in the treatment of osteoporosis.
Conclusion:
The results suggested that NOB-PEG-PCL micelles could effectively prevent NOB fast release from micelles and extend circulation time. The NOB-PEG-PCL delivery system may be a promising way to prevent and treat osteoporosis.
Insights
This study developed a novel nobiletin (NOB)-loaded nanoparticle formulation (NOB-PEG-PCL) to overcome NOB
Area of Science:
- Biomaterials Science
- Nanotechnology
- Pharmacology
Background:
- Nobiletin (NOB), a flavonoid, shows anti-cancer, anti-inflammatory, and anti-osteoporosis potential.
- Limitations of NOB include poor hydrophilicity and cytotoxicity at high concentrations, hindering practical application.
- Development of a stable, effective NOB formulation is crucial for osteoporosis treatment.
Purpose of the Study:
- To develop a novel drug delivery system for nobiletin (NOB) to treat osteoporosis.
- To create NOB-loaded poly(ethylene glycol)-block-poly(e-caprolactone) (NOB-PEG-PCL) nanoparticles.
- To evaluate the anti-osteoporosis efficacy and safety of the NOB-PEG-PCL formulation.
Main Methods:
- NOB-loaded nanoparticles (NOB-PEG-PCL) were synthesized using a dialysis method.
- Characterization included dynamic light scattering and transmission electron microscopy.
- In vitro studies involved drug release, cytotoxicity assays on bone marrow-derived macrophages (BMMs), and RANKL-induced osteoclast differentiation models. In vivo studies used ovariectomized (OVX) mice.
Main Results:
- NOB-PEG-PCL nanoparticles exhibited a spherical shape with a mean diameter of approximately 124 nm.
- High encapsulation efficiency (76.34±3.25%) and drug loading (7.60±0.48%) were achieved.
- The formulation demonstrated sustained NOB release over 48 hours, significantly inhibited osteoclast formation and differentiation (TRAP-positive cells, mRNA expression of TRAP and cathepsin K), and showed no cytotoxicity to BMMs. In vivo, it prevented bone loss and improved bone density in OVX mice.
Conclusions:
- NOB-PEG-PCL micelles effectively control NOB release and prolong circulation time.
- The NOB-PEG-PCL delivery system shows significant potential for preventing and treating osteoporosis.
- This formulation addresses NOB's limitations, offering a promising therapeutic strategy.
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