基于磷酸化修饰的核/壳硅纳米颗粒药物缓释体研究

采用反相微乳液体系中功能化基团同步修饰方法制备了包载抗肿瘤药物平阳霉素(PYM)的磷酸化核/壳硅纳米颗粒(PYM-PO4SiNP), 考察了不同量的磷酸化修饰试剂对PYM-PO4SiNP的影响. 结果表明, 随着磷酸化修饰试剂量的增加, 制备的PYM-PO4SiNP的电位逐渐降低, 其包载的PYM 的释放速率逐渐加快, 但对颗粒的粒径没有明显影响. 本文选择能使药物平稳、缓慢释放的磷酸化修饰试剂用量, 制备了稳定性好、药物缓释时间长的PYM-PO4SiNP, 其载药量和包封率分别为7.2%和37.81%, 通过与CNE-2细胞共培育后, 可以使CNE-2细胞的存活率逐渐下降, 而磷酸化核/壳硅纳米颗粒PO4SiNP载体本身是没有毒性的. 这一研究工作的开展拓宽了核/壳硅纳米颗粒在药物载体领域中的应用.

Novel Drug Carrier System Based on Phosphonate-terminated Core/shell Silica Nanoparticles

Pingyangmycin(PYM) doped phosphonate-terminated silica nanoparticles(PYM-PO4SiNP) were prepared via the synchronous modification of functional group in the water-in-oil microemulsion. The effect of the quantum of 3-trihydroxysilylpropyl methylphosphonate(THPMP) on the PYM-PO4SiNP was investigated. The results show that the ζ potential of PYM-PO4SiNP decreased obviously, and the release rate of PYM from the PYM-PO4SiNP accelerated with increase of added THPMP. However, the quantum of THPMP had no impact on the size of PYM-PO4SiNP. PYM-PO4SiNP with a good stability and long acting release was prepared with optimal quantum THPMP, at which the drug can release steadily and slowly. The prepared PYM-PO4SiNP presented drug loading and entrapment efficiency of 7.2% and 37.81%, respectively. The PYM-PO4SiNP could make the survival rate of CNE-2 cells fell gradually, and PO4SiNP itself was nontoxic. The research work expands the applications of core/shell silica nanoparticles in the field of drug carrier.