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基于磷酸化修饰的核/壳硅纳米颗粒药物缓释体研究

何晓晓, 海罗, 王柯敏, 伍旭, 谭蔚泓   

  1. 湖南大学生物医学工程中心, 化学生物传感与计量学国家重点实验室, 化学化工学院, 生命科学与技术研究院, 生物纳米与分子工程湖南省重点实验室, 长沙 410082
  • 收稿日期:2008-09-19 修回日期:1900-01-01 出版日期:2009-02-10 发布日期:2009-02-10
  • 通讯作者: 王柯敏

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

HE Xiao-Xiao, HAI Luo, WANG Ke-Min*, WU Xu, TAN Wei-Hong   

  1. Biomedical Engineering Center, State Key Laboratory of Chemo/Biosensing and Chemometrics, College of Chemistry and Chemical Engineering, Hunan University, Key Laboratory for Bio-Nanotechnology and Molecule Engineering of Hunan Province, Changsha 410082, China
  • Received:2008-09-19 Revised:1900-01-01 Online:2009-02-10 Published:2009-02-10
  • Contact: WANG Ke-Min

摘要: 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.

关键词: 药物缓释, 药物载体, 平阳霉素, 磷酸化硅纳米颗粒

Abstract: 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.

Key words: Drug sustained release, Drug carrier, Pingyangmycine, Phosphonate-terminated silica nanoparticles

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