天津医药
天津醫藥
천진의약
TIANJIN MEDICAL JOURNAL
2015年
8期
852-855
,共4页
孟艾%杨涛%王娉婷%王剑%隋磊
孟艾%楊濤%王娉婷%王劍%隋磊
맹애%양도%왕빙정%왕검%수뢰
纳米管,碳%顺铂%抗肿瘤药%药物载体%迟效制剂%多壁碳纳米管%靶向作用%释放模式
納米管,碳%順鉑%抗腫瘤藥%藥物載體%遲效製劑%多壁碳納米管%靶嚮作用%釋放模式
납미관,탄%순박%항종류약%약물재체%지효제제%다벽탄납미관%파향작용%석방모식
nanotubes,carbon%cisplatin%antineoplastic agents%drug carriers%delayed-action preparations%multi-walled carbon nanotubes%targeting property%release profile
目的:制备大内径多壁碳纳米管(LID-MWCNT)基靶向抗肿瘤药物缓释系统,分析其功能特性并检测其对肿瘤细胞的增殖抑制作用。方法纯化、切割LID-MWCNT,制备碳管载体及同源封堵物超短LID-MWCNT (UST)。碳管表面负载靶向分子叶酸(FA)及荧光标记分子;管内负载抗肿瘤药物顺铂(CDDP),并以UST封堵药物通道。观察载药系统显微形态;测定载药率及药物释放曲线;观察载药系统对肿瘤细胞的靶向趋化状况及增殖抑制效应。结果成功制备大内径多壁碳纳米管基靶向抗肿瘤药物缓释系统(CDDP@UST-FA-LID-MWCNT),其载药率为70.97%。体外释放呈双相缓释模式,持续释放时间约18 h。载体系统具备了一定靶向趋化能力;较低载药浓度的CDDP@UST-FA-LID-MWCNT即对肿瘤细胞具有增殖抑制作用,且随着药物浓度的增加,抑制作用增强。结论载药系统CDDP@UST-FA-LID-MWCNT具有较高的载药率及良好的药物缓释效果,能够靶向作用于肿瘤细胞,具有较强的抗肿瘤作用。
目的:製備大內徑多壁碳納米管(LID-MWCNT)基靶嚮抗腫瘤藥物緩釋繫統,分析其功能特性併檢測其對腫瘤細胞的增殖抑製作用。方法純化、切割LID-MWCNT,製備碳管載體及同源封堵物超短LID-MWCNT (UST)。碳管錶麵負載靶嚮分子葉痠(FA)及熒光標記分子;管內負載抗腫瘤藥物順鉑(CDDP),併以UST封堵藥物通道。觀察載藥繫統顯微形態;測定載藥率及藥物釋放麯線;觀察載藥繫統對腫瘤細胞的靶嚮趨化狀況及增殖抑製效應。結果成功製備大內徑多壁碳納米管基靶嚮抗腫瘤藥物緩釋繫統(CDDP@UST-FA-LID-MWCNT),其載藥率為70.97%。體外釋放呈雙相緩釋模式,持續釋放時間約18 h。載體繫統具備瞭一定靶嚮趨化能力;較低載藥濃度的CDDP@UST-FA-LID-MWCNT即對腫瘤細胞具有增殖抑製作用,且隨著藥物濃度的增加,抑製作用增彊。結論載藥繫統CDDP@UST-FA-LID-MWCNT具有較高的載藥率及良好的藥物緩釋效果,能夠靶嚮作用于腫瘤細胞,具有較彊的抗腫瘤作用。
목적:제비대내경다벽탄납미관(LID-MWCNT)기파향항종류약물완석계통,분석기공능특성병검측기대종류세포적증식억제작용。방법순화、절할LID-MWCNT,제비탄관재체급동원봉도물초단LID-MWCNT (UST)。탄관표면부재파향분자협산(FA)급형광표기분자;관내부재항종류약물순박(CDDP),병이UST봉도약물통도。관찰재약계통현미형태;측정재약솔급약물석방곡선;관찰재약계통대종류세포적파향추화상황급증식억제효응。결과성공제비대내경다벽탄납미관기파향항종류약물완석계통(CDDP@UST-FA-LID-MWCNT),기재약솔위70.97%。체외석방정쌍상완석모식,지속석방시간약18 h。재체계통구비료일정파향추화능력;교저재약농도적CDDP@UST-FA-LID-MWCNT즉대종류세포구유증식억제작용,차수착약물농도적증가,억제작용증강。결론재약계통CDDP@UST-FA-LID-MWCNT구유교고적재약솔급량호적약물완석효과,능구파향작용우종류세포,구유교강적항종류작용。
Objective To prepare a targeted antitumor drug delivery system using large-inner-diameter multi-walled carbon nanotubes (LID-MWCNTs) for sustained release and to study its performance. Methods LID-MWCNTs were puri?fied and oxidized,then use nanocarriers and USTs as homologous blockers. Folic acid and fluorescent labels were conjugat?ed onto the external surfaces of nanocarriers. CDDP (cisplatin) was encapsulated and ultrashort tubes (USTs) were employed to block the drug entry/exit paths. The microstructure of resulted drug delivery system (DDS) was observed, while drug load?ing efficiency and drug release profile in vitro were determined. The tumor-targeting property and cytotoxicity of DDS were also assessed. Results LID-MWCNT based sustained release targeted drug delivery system was established. Drug loading efficiency of CDDP@UST-FA-LID-MWCNTs was as high as 70.97%. A typical biphasic sustained release pattern was dem?onstrated, and the accumulating release time was 18 h. DDS exhibited a certain kind of tumor-targeting property, and inhibit?ed proliferation of tumor cells in a dose-dependent manner. Conclusion CDDP@UST-FA-LID-MWCNT drug delivery system exhibited an improved drug loading efficiency and a sustained drug release profile. It could specifically target the tu?mor cells and had a significant antitumor effect.