Calcium phosphate nanoparticles (CaPNPs) have good biocompatibility as gene carriers; however, CaPNPs typically exhibit a low transfection efficiency. Cell penetrate peptide (TAT) can increase the uptake of nanoparticles but is limited by its non-specificity. Grafting adhesion peptide adhesion peptide on carriers can enhance their targeting. The Plekho1 gene encodes casein kinase-2 interacting protein-1 (CKIP-1) , which can negatively regulate osteogenic differentiation. Based on the above, we produced a Mg-CaPNPs-RGD-TAT-CKIP-1 siRNA carrier system via hydrothermal synthesis, silanization and adsorption. The effects of this carrier system on cell endocytosis and biological effects were evaluated by cell culture in vitro. The results demonstrate that CaPNPs with 7% Mg (60 nm particle size, short rod shape and good dispersion) were suitable for use as gene carriers. The carrier system boosted the endocytosis of MG63 cells and was helpful for promoting the differentiation of osteoblasts, and the dual-ligand system possessed a synergistic effect. The findings of this study show the tremendous potential of the Mg-CaPNPs-RGD-TAT-CKIP-1 siRNA carrier system for efficient delivery into cells and osteogenesis inducement.

磷酸钙纳米颗粒（CaPNPs）作为基因载体具有良好的生物相容性；然而，CaPNPs 通常表现出低转染效率。细胞穿透肽 (TAT) 可以增加纳米颗粒的吸收，但受到其非特异性的限制。在载体上嫁接粘附肽粘附肽可以增强其靶向性。Plekho1 基因编码酪蛋白激酶-2 相互作用蛋白-1 (CKIP-1)，可负向调节成骨分化。基于上述，我们通过水热合成、硅烷化和吸附制备了Mg-CaPNPs-RGD-TAT-CKIP-1 siRNA载体系统。该载体系统对细胞内吞作用和生物学效应的影响通过体外细胞培养进行评估。结果表明，含有 7% Mg（60 nm 粒径，短棒状和良好的分散性）适合用作基因载体。载体系统增强了MG63细胞的内吞作用，有助于促进成骨细胞的分化，双配体系统具有协同作用。这项研究的结果显示了 Mg-CaPNPs-RGD-TAT-CKIP-1 siRNA 载体系统在有效递送到细胞和诱导成骨方面的巨大潜力。