Construction of METHFR shRNA/5-fluorouracil co-loaded folate-targeted chitosan polymeric nanoparticles and its anti-carcinoma effect on gastric cells growth

被引：7
作者：
Xin, Lin [1 ]
Fan, Ji-Chang [1 ]
Le, Yi-Guan [1 ]
Zeng, Fei [1 ]
Cheng, Hua [1 ]
Hu, Xiao-yun [1 ]
Cao, Jia-Qing [1 ]
机构：
[1] Nanchang Univ, Affiliated Hosp 2, Dept Gen Surg, Nanchang 330006, Jiangxi, Peoples R China
来源：
JOURNAL OF NANOPARTICLE RESEARCH | 2016年 / 18卷 / 05期
基金：
中国国家自然科学基金;
关键词：
Polymeric nanoparticles; Folate; Targeting; Drug delivery; Nanomedicine; MULTIDRUG-RESISTANCE; STEALTH LIPOSOMES; P-GLYCOPROTEIN; DOXORUBICIN;
D O I：
10.1007/s11051-016-3410-5
中图分类号：
O6 [化学];
学科分类号：
0703 ;
摘要：
PEGylated and folate-targeted chitosan polymeric nanoparticles (FPNs) for the treatment of gastric carcinoma were prepared successfully. OQC-anchored folate conjugates were synthesized and used in assembling FPNs nano-system for enhancing intracellular uptake against folate receptor overexpressing cancer cells. The results indicated that folate-targeted chitosan polymeric nanoparticles (CPNs) can reverse drug-resistant SGC-7901 cells of 5-fluorouracil (5-FU) compared with non-targeted CPNs. Increased therapeutic efficiency of 5-FU/METHFR shRNA co-loaded PNs were also tested in SGC-7901 cells and compaed with 5-FU or METHFR shRNA in solution, which was associated with increased cell inhibition function for single drug group and synergistic effects of 5-FU and METHFR shRNA at 2.0 mu g/mL FPNs concentration. In addition, the cell accumulation levels of 5-FU in SGC-7901 cells was time dependent for these nanoparticles. FPNs (effective diameter: 83.2 +/- 1.1 nm; polydispersity index: 0.193) could significantly boost cellular accumulation of 5-FU and overcome the drug efflux mechanism of MDR than 5-FU-loaded NPNs and 5-FU in solution. In conclusion, ligand-targeted PNs can be used as a potentially effective drug delivery system.
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页数：12
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