title: Lactosaminated mesoporous silica nanoparticles for asialoglycoprotein receptor targeted anticancer drug delivery.
abstract: BACKGROUND
  Mesoporous silica nanoparticles (MSNs) have several attractive properties as a drug delivery system, such as ordered porous structure, large surface area, controllable particle size as well as interior and exterior dual-functional surfaces. The purpose of this study was to develop novel lactosaminated mesoporous silica nanoparticles (Lac-MSNs) for asialoglycoprotein receptor (ASGPR) targeted anticancer drug delivery.
  
  
  RESULTS
  Lac-MSNs with an average diameter of approximately 100 nm were prepared by conjugation of lactose with 3-aminopropyl triethoxysilane modified MSNs. Characterization of Lac-MSNs indicated a huge Brunauer-Emmett-Teller (BET) surface area (1012 m(2)/g), highly ordered 2D hexagonal symmetry, an unique mesoporous structure with average pore size of 3.7 nm. The confocal microscopy and flow cytometric analysis illustrated Lac-MSNs were effectively endocytosed by ASGPR-positive hepatoma cell lines, HepG2 and SMMC7721. In contrast, non-selective endocytosis of Lac-MSNs was found in ASGPR-negative NIH 3T3 cells. The cellular uptake study showed the internalization process was energy-consuming and predominated by clathrin-mediated pathway. Model drug docetaxel (DTX) was loaded in the mesopores of Lac-MSNs by wetness impregnation method. In vitro cytotoxicity assay showed that DTX transported by Lac-MSNs effectively inhibited the growth of HepG2 and SMMC7721 cells in a time- and concentration- dependent manner.
  
  
  CONCLUSIONS
  These results demonstrated that Lac-MSNs could be a promising inorganic carrier system for targeted intracellular anti-cancer drug delivery.
authors: School of Pharmaceutical Sciences, Sun Yat-Sen University, Guangzhou, 510006, People's Republic of China. xiaoplanet@163.com.
authors: Guilan
authors: G
authors: Quan
authors: School of Pharmaceutical Sciences, Sun Yat-Sen University, Guangzhou, 510006, People's Republic of China. mercurypan@foxmail.com.
authors: Xin
authors: X
authors: Pan
authors: School of Pharmaceutical Sciences, Sun Yat-Sen University, Guangzhou, 510006, People's Republic of China. 350348391@qq.com.
authors: Zhouhua
authors: Z
authors: Wang
authors: School of Pharmaceutical Sciences, Sun Yat-Sen University, Guangzhou, 510006, People's Republic of China. 1159718683@qq.com.
authors: Qiaoli
authors: Q
authors: Wu
authors: Guangzhou Neworld Pharmaceutical Ltd. Co., Guangzhou, 510006, People's Republic of China. ww236@hotmail.com.
authors: Ge
authors: G
authors: Li
authors: School of Pharmaceutical Sciences, Guangdong Medical College, Dongguan, 523808, People's Republic of China. dianlh@163.com.
authors: Linghui
authors: L
authors: Dian
authors: School of Pharmaceutical Sciences, Sun Yat-Sen University, Guangzhou, 510006, People's Republic of China. lsscb@mail.sysu.edu.cn.
authors: Bao
authors: B
authors: Chen
authors: School of Pharmaceutical Sciences, Sun Yat-Sen University, Guangzhou, 510006, People's Republic of China. chuanbin_wu@126.com.
authors: Chuanbin
authors: C
authors: Wu
mesh_terms: D000606:Amino Sugars / Q000737:chemistry; D000818:Animals; D000970:Antineoplastic Agents / Q000008:administration & dosage* / Q000737:chemistry; D037263:Asialoglycoprotein Receptor; D000077143:Docetaxel; D016503:Drug Delivery Systems / Q000379:methods*; D004705:Endocytosis / Q000187:drug effects; D056945:Hep G2 Cells / Q000187:drug effects; D006801:Humans; D051379:Mice; D008855:Microscopy, Electron, Scanning; D058990:Molecular Targeted Therapy / Q000379:methods; D041681:NIH 3T3 Cells / Q000187:drug effects; D053758:Nanoparticles / Q000008:administration & dosage* / Q000737:chemistry*; D012822:Silicon Dioxide / Q000737:chemistry; D043823:Taxoids / Q000008:administration & dosage / Q000737:chemistry
chemical_list: D000606:Amino Sugars; D000970:Antineoplastic Agents; D037263:Asialoglycoprotein Receptor; D043823:Taxoids; C032233:lactosamine; D000077143:Docetaxel; D012822:Silicon Dioxide
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