PDF(Pubmed)
Abstract：
UNASSIGNED: Osteoporosis, characterized by dysregulation of osteoclastic bone resorption and osteoblastic bone formation, severely threatens human health during aging. However, there is still no good therapy for osteoporosis, so this direction requires our continuous attention, and there is an urgent need for new drugs to solve this problem.
UNASSIGNED: Traditional Chinese Medicine Salvia divinorum monomer pomolic acid (PA) could effectively inhibit osteoclastogenesis and ovariectomized osteoporosis. However, its poor solubility and lack of targeting severely limits its further application. A novel bone-targeting nanomedicine (PA@TLipo) has been developed to reconstruct the osteoporotic microenvironment by encapsulating pomolic acid in alendronate-functionalized liposomes. Through a series of operations such as synthesis, purification, encapsulation, and labeling, the PA@TLipo have been prepared. Moreover, the cytotoxicity, bone targeting and anti-osteoporosis effect was verified by cell and animal experiments.
UNASSIGNED: In the aspect of targeting, the PA@TLipo can effectively aggregate on the bone tissue to reduce bone loss, and in terms of toxicity, PA@TLipo could increase the bone target ability in comparison to nontargeted liposome, thereby mitigating systemic cytotoxicity. Moreover, PA@TLipo inhibited osteoclast formation and bone resorption in vitro and reduced bone loss in ovariectomy-induced osteoporotic mice.
UNASSIGNED: In this study, a novel therapeutic agent was designed and constructed to treat osteoporosis, consisting of a liposome material as the drug pocket, PA as the anti-osteoporosis drug, and ALN as the bone-targeting molecule. And our study is the first to employ a bone-targeted delivery system to deliver PA for OVX-induced bone loss, providing an innovative solution for treating osteoporosis.
UNASSIGNED: Traditional Chinese Medicine Salvia divinorum monomer pomolic acid (PA) could effectively inhibit osteoclastogenesis and ovariectomized osteoporosis. However, its poor solubility and lack of targeting severely limits its further application. A novel bone-targeting nanomedicine (PA@TLipo) has been developed to reconstruct the osteoporotic microenvironment by encapsulating pomolic acid in alendronate-functionalized liposomes. Through a series of operations such as synthesis, purification, encapsulation, and labeling, the PA@TLipo have been prepared. Moreover, the cytotoxicity, bone targeting and anti-osteoporosis effect was verified by cell and animal experiments.
UNASSIGNED: In the aspect of targeting, the PA@TLipo can effectively aggregate on the bone tissue to reduce bone loss, and in terms of toxicity, PA@TLipo could increase the bone target ability in comparison to nontargeted liposome, thereby mitigating systemic cytotoxicity. Moreover, PA@TLipo inhibited osteoclast formation and bone resorption in vitro and reduced bone loss in ovariectomy-induced osteoporotic mice.
UNASSIGNED: In this study, a novel therapeutic agent was designed and constructed to treat osteoporosis, consisting of a liposome material as the drug pocket, PA as the anti-osteoporosis drug, and ALN as the bone-targeting molecule. And our study is the first to employ a bone-targeted delivery system to deliver PA for OVX-induced bone loss, providing an innovative solution for treating osteoporosis.
摘要：
■骨质疏松症，以破骨细胞骨吸收和成骨细胞骨形成失调为特征，在衰老过程中严重威胁人类健康。然而,骨质疏松症仍然没有好的治疗方法，所以这个方向需要我们持续的关注，迫切需要新药来解决这个问题。
■中药丹参单体磷酚酸（PA）能有效抑制破骨细胞生成和去卵巢骨质疏松。然而,溶解性差和缺乏靶向性严重限制了其进一步应用。已开发出一种新型的骨靶向纳米药物（PA@TLipo），通过在阿仑膦酸盐官能化的脂质体中包封波莫诺酸来重建骨质疏松的微环境。通过合成等一系列操作，净化,封装，和标签，PA@TLipo已经准备好了。此外，细胞毒性，通过细胞和动物实验验证了骨靶向和抗骨质疏松作用。
■在瞄准方面，PA@TLipo能有效聚集在骨组织上，减少骨丢失，就毒性而言，与非靶向脂质体相比，PA@TLipo可以增加骨靶向能力，从而减轻全身细胞毒性。此外，PA@TLipo在体外抑制破骨细胞形成和骨吸收，并减少卵巢切除引起的骨质疏松小鼠的骨丢失。
■在这项研究中，一种新的治疗剂被设计和制造来治疗骨质疏松症，由作为药物袋的脂质体材料组成，PA作为抗骨质疏松药物，和ALN作为骨靶向分子。我们的研究是第一个采用骨靶向递送系统为OVX引起的骨丢失递送PA，提供治疗骨质疏松症的创新解决方案。
■中药丹参单体磷酚酸（PA）能有效抑制破骨细胞生成和去卵巢骨质疏松。然而,溶解性差和缺乏靶向性严重限制了其进一步应用。已开发出一种新型的骨靶向纳米药物（PA@TLipo），通过在阿仑膦酸盐官能化的脂质体中包封波莫诺酸来重建骨质疏松的微环境。通过合成等一系列操作，净化,封装，和标签，PA@TLipo已经准备好了。此外，细胞毒性，通过细胞和动物实验验证了骨靶向和抗骨质疏松作用。
■在瞄准方面，PA@TLipo能有效聚集在骨组织上，减少骨丢失，就毒性而言，与非靶向脂质体相比，PA@TLipo可以增加骨靶向能力，从而减轻全身细胞毒性。此外，PA@TLipo在体外抑制破骨细胞形成和骨吸收，并减少卵巢切除引起的骨质疏松小鼠的骨丢失。
■在这项研究中，一种新的治疗剂被设计和制造来治疗骨质疏松症，由作为药物袋的脂质体材料组成，PA作为抗骨质疏松药物，和ALN作为骨靶向分子。我们的研究是第一个采用骨靶向递送系统为OVX引起的骨丢失递送PA，提供治疗骨质疏松症的创新解决方案。
