Beijing Area Major Laboratory of Peptide and Small Molecular Drugs, Engineering Research Center of Ministry of Education of China, Beijing Laboratory of Biomedical Materials, School of Pharmaceutical Science, Capital Medical University, Beijing, 100069, People's Republic of China.
Discipline of Oral and Maxillofacial Surgery, Faculty of Dentistry, The University of Hong Kong, Hong Kong, 999077, SAR, China.
Pharm Res. 2023 Jan;40(1):231-243. doi: 10.1007/s11095-022-03430-8. Epub 2022 Nov 15.
Osteosarcoma is well-known for its high incidence in children and adolescents and long-term bone pain, which seriously reduces the life quality of patients. Cisplatin (CDDP), as the first-line anti-osteosarcoma drug, has been used in many anticancer treatments. At the same time, the serious side effects of platinum (Pt) drugs have also attracted widespread attention. To accurately deliver Pt drugs to the lesion site and realize controlled release of Pt drugs, certain modified delivery systems have been extensively studied.
Among them, liposomes have been approved for clinical cancer treatment due to their highly biocompatibility and superior modifiability. Here, we developed a bone-targeted dual functional lipid-coated drug delivery system, lipid-coated CDDP alendronate nanoparticles (LCA NPs) to target the bone and precisely deliver the drugs to the tumor site. Cell toxicity, apoptosis and cellular uptake were detected to evaluate the anticancer effect for LCA NPs. Furthermore, transwell assay and wound healing assay were conducted to estimate the osteosarcoma cell migration and invasion. Hemolysis assay was utilized to assess the biocapitibility of the kind of NPs.
With the aim of bone-targeted unit alendronate (ALD), LCA NPs serve as a rich bone homing Pt delivery system to exert efficient anticancer effects and synergistically reduce bone resorption and bone loss potentially.
By providing a highly biocompatible platform for osteosarcoma therapy, LCA NPs may help to significantly enhance the anticancer effect of Pt and greatly reduce the systemic toxicity and side effects of Pt towards osteosarcoma.
骨肉瘤在儿童和青少年中的发病率较高，且长期骨痛，严重降低了患者的生活质量。顺铂（CDDP）作为一线抗骨肉瘤药物，已被广泛应用于多种抗癌治疗中。同时，铂类药物的严重副作用也引起了广泛关注。为了将铂类药物准确递送到病变部位并实现铂类药物的控制释放，已经广泛研究了某些修饰的递药系统。
其中，由于具有高度的生物相容性和优越的可修饰性，脂质体已被批准用于临床癌症治疗。在这里，我们开发了一种骨靶向双功能脂质包覆药物递送系统，即脂质包覆顺铂阿仑膦酸盐纳米颗粒（LCA NPs），以靶向骨骼并将药物精确递送到肿瘤部位。通过检测细胞毒性、细胞凋亡和细胞摄取来评估 LCA NPs 的抗癌效果。此外，还进行了 Transwell 测定和划痕愈合试验来评估骨肉瘤细胞的迁移和侵袭。通过溶血试验评估了这种 NPs 的生物相容性。
以骨靶向单元阿仑膦酸盐（ALD）为目的，LCA NPs 作为一种富含骨骼的铂类药物递送系统，能够发挥高效的抗癌作用，并协同减少潜在的骨质吸收和骨质流失。
通过为骨肉瘤治疗提供一种高度生物相容的平台，LCA NPs 可能有助于显著增强铂类药物的抗癌效果，并大大降低铂类药物对骨肉瘤的全身毒性和副作用。
