Roy Indrajit, Mitra Susmita, Maitra Amarnath, Mozumdar Subho
Department of Chemistry, University of Delhi, Delhi 110007, India.
Int J Pharm. 2003 Jan 2;250(1):25-33. doi: 10.1016/s0378-5173(02)00452-0.
Calcium phosphate nanoparticles present a unique class of non-viral vectors, which can serve as efficient and alternative DNA carriers for targeted delivery of genes. In this study we report the design and synthesis of ultra-low size, highly monodispersed DNA doped calcium phosphate nanoparticles of size around 80 nm in diameter. The DNA encapsulated inside the nanoparticle is protected from the external DNase environment and could be used safely to transfer the encapsulated DNA under in vitro and in vivo conditions. Moreover, the surface of these nanoparticles could be suitably modified by adsorbing a highly adhesive polymer like polyacrylic acid followed by conjugating the carboxylic groups of the polymer with a ligand such as p-amino-1-thio-beta-galactopyranoside using 1-ethyl-3-(3-dimethylaminopropyl)-carbodiimide hydrochloride as a coupling agent. We have demonstrated in our studies that these surface modified calcium phosphate nanoparticles can be used in vivo to target genes specifically to the liver.
磷酸钙纳米颗粒是一类独特的非病毒载体，可作为高效的替代性DNA载体用于基因的靶向递送。在本研究中，我们报道了直径约80nm的超低尺寸、高度单分散的掺杂DNA的磷酸钙纳米颗粒的设计与合成。包裹在纳米颗粒内部的DNA受到外部DNase环境的保护，可在体外和体内条件下安全地用于转移包裹的DNA。此外，这些纳米颗粒的表面可通过吸附一种高粘性聚合物（如聚丙烯酸）进行适当修饰，然后使用1-乙基-3-(3-二甲基氨基丙基)-碳二亚胺盐酸盐作为偶联剂，将聚合物的羧基与配体（如对氨基-1-硫代-β-吡喃半乳糖苷）进行共轭。我们在研究中已证明，这些表面修饰的磷酸钙纳米颗粒可在体内用于将基因特异性靶向至肝脏。
