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引用本文:魏伟,李博乐,王晨.包裹5-氟尿嘧啶的二氧化硅纳米颗粒的制备及细胞毒性研究[J].中国现代应用药学,2016,33(1):59-62.
WEI Wei,LI Bole,WANG Chen.Synthesis of 5-Fluorouracil Doped Silica Nanoparticles and Their Cytotoxicity[J].Chin J Mod Appl Pharm(中国现代应用药学),2016,33(1):59-62.
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包裹5-氟尿嘧啶的二氧化硅纳米颗粒的制备及细胞毒性研究
魏伟, 李博乐, 王晨
天津医科大学肿瘤医院药学部,国家肿瘤临床医学研究中心,天津市肿瘤防治重点实验室,天津 300060
摘要:
目的 制备包裹5-氟尿嘧啶的二氧化硅(5-Fu/SiO2)纳米颗粒,并对其药剂学参数及体外细胞毒性进行研究。方法 利用反相微乳化法制备5-Fu/SiO2纳米颗粒,对5-Fu投入量及反应时间等合成条件进行优化,考察纳米颗粒的稳定性及体外释药行为,并采用MTT法对其体外细胞毒性进行研究。结果 当5-Fu投入量为1.33 mg及反应时间为24 h时,5-Fu/SiO2纳米的载药率及包封率达到最高,分别为1.03%及24.77%,同时该纳米在48 h内释放率达到41.31%,7 d内粒径无明显变化。细胞毒性实验表明,5-Fu/SiO2纳米对人肝癌细胞具有明显的抑制效果,而空白SiO2纳米对细胞活性影响较小。结论 成功制备了稳定性好、缓释时间长的5-Fu/SiO2纳米颗粒,为开发5-Fu缓释剂型提供了新的思路。
关键词:  5-氟尿嘧啶  二氧化硅纳米  细胞毒性;药物载体
DOI:
分类号:R284.1;R917.101
基金项目:天津医科大学肿瘤医院药检放专项基金(Y1208)
Synthesis of 5-Fluorouracil Doped Silica Nanoparticles and Their Cytotoxicity
WEI Wei, LI Bole, WANG Chen
Key Laboratory of Cancer Prevention and Therapy, National Clinical Research Center for Cancer, Department of Pharmacy, Tianjin Medical University Cancer Institute and Hospital, Tianjin 300060, China
Abstract:
OBJECTIVE To synthesize 5-fluorouracil(5-Fu) doped silica(5-Fu/SiO2) nanoparticles, and to evaluate their parameter of pharmacy and cytotoxicity in vitro. METHODS The 5-Fu/SiO2 nanoparticles were prepared in the water-in-oil microemulsion, and the administered dose of 5-Fu and the reaction time were optimized to improve the drug loading and entrapment efficiency. The stability and the in vivo release of 5-Fu/SiO2 were also investigated. The antitumor activities in vitro were evaluated by MTT method. RESULTS With adding 1.33 mg 5-Fu and reacting 24 h, the 5-Fu loading and entrapment efficiency reached maximum yields as 1.03% and 24.77%, respectively. The 5-Fu was released slowly for 48 h, and the size of 5-Fu/SiO2 nanoparticles had no obvious changing in 7 d. The MTT experiments showed that 5-Fu/SiO2 nanoparticles had an inhibition on the human hepatic cancer cells, while the SiO2 nanoparticles had no similar effects. CONCLUSION The 5-Fu/SiO2 nanoparticles with a good stability and long release is prepared successfully, which provides a new fitting way for developing the 5-Fu dosage forms.
Key words:  5-fluorouracil  silica nanoparticles  cytotoxicity  pharmaceutical carrier
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