發(fā)布時(shí)間：2018-03-28 15:44

  本文選題：多西紫杉醇　切入點(diǎn)：納米結(jié)構(gòu)脂質(zhì)載體　出處：《首都醫(yī)科大學(xué)學(xué)報(bào)》2015年02期

【摘要】：目的探討多西紫杉醇(docetaxel,DTX)海豹油脂質(zhì)體的抗腫瘤活性以及與脂肪乳的比較。方法采用正交試驗(yàn)設(shè)計(jì)法篩選處方,通過(guò)高壓乳勻法制備多西紫杉醇海豹油脂質(zhì)體。測(cè)定其粒徑、電位、包封率、體外釋藥、血漿中穩(wěn)定性等。并采用四甲基偶氮唑鹽〔3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide,MTT〕進(jìn)行體外抗腫瘤活性研究,以及采用荷肉瘤S180小鼠進(jìn)行體內(nèi)抗腫瘤活性研究,考察各組抑瘤率和存活率。結(jié)果多西紫杉醇海豹油脂質(zhì)體的粒徑在200 nm左右,Zeta電位為-30~-50 m V,包封率達(dá)95%以上。體外釋放研究證明多西紫杉醇脂肪乳與多西紫杉醇海豹油脂質(zhì)體具有一定的p H敏感性,且推測(cè)多西紫杉醇海豹油脂質(zhì)體具有更強(qiáng)的緩釋作用。血漿中穩(wěn)定性研究證明多西紫杉醇脂肪乳與多西紫杉醇海豹油脂質(zhì)體在血漿中較穩(wěn)定,釋放行為緩慢。結(jié)論由MTT法結(jié)果得多西紫杉醇海豹油脂質(zhì)體、多西紫杉醇脂肪乳與DTX均表現(xiàn)出較強(qiáng)的細(xì)胞毒性作用,且多西紫杉醇海豹油脂質(zhì)體具有一定的緩釋作用。以荷肉瘤S180小鼠為模型的體內(nèi)抗腫瘤活性研究表明多西紫杉醇脂肪乳與多西紫杉醇海豹油脂質(zhì)體在血漿中12 h內(nèi)累積釋放量分別為(13.82±0.59)%與(12.91±0.60)%。說(shuō)明劑型在血漿中較穩(wěn)定,釋放行為緩慢。另外,DTX組小鼠9 d存活率為0,多西紫杉醇脂肪乳組于9 d存活率為93.3%,而多西紫杉醇海豹油脂質(zhì)體組小鼠9 d存活率為100%,說(shuō)明多西紫杉醇海豹油脂質(zhì)體使得耐受劑量提高,降低了藥物的不良反應(yīng),提高用藥安全性與用藥的順應(yīng)性。
[Abstract]:Objective to investigate the antitumor activity of docetaxella-DTX seal liposome and its comparison with fat emulsion. Methods the prescription was screened by orthogonal design, and the liposome of docetaxelon seal oil was prepared by high pressure emulsion leveling. The particle size of the liposome was determined. Potential, encapsulation efficiency, drug release in vitro, stability in plasma, etc. Antitumor activity in vitro was studied by tetrazolium bromidetran MTTT with tetrazolium bromide MTT, and antitumor activity in vivo in S180 mice was studied by using tetrazolium tetrazolium 5-diphenyltetrazolium tetrazolium (MTTT), a tetrazolium tetrazolium tetrazolium 5-diphenyltetrazolium tetrazolium tetrazolium tetrazolium in vitro. Results the diameter of docetaxel seal liposomes was about 200 nm and the entrapment efficiency was over 95%. The in vitro release studies showed that docetaxel fat emulsion and docetaxel were more than 95%. Seal oil liposomes have a certain pH sensitivity. It is suggested that docetaxel seal oil liposomes have stronger sustained release effect. The stability of docetaxel fat emulsion and docetaxel seal oil liposome is more stable in plasma than that of docetaxel seal oil liposome in plasma. Conclusion docetaxel seal oil liposome, docetaxel fat emulsion and DTX showed strong cytotoxicity by MTT method. The antitumor activity of docetaxel seal liposome in vivo using S180 mice as model showed that docetaxel fat emulsion and docetaxel seal oil liposome were in plasma for 12 h. The cumulative release was 13.82 鹵0.59% and 12.91 鹵0.60%, respectively. In addition, the survival rate was 0 in DTX group, 93.3 in docetaxel fat emulsion group and 100 in docetaxel seal oil liposome group. Plastids increase the tolerance dose, The safety and compliance of the drug were improved by reducing the adverse drug reactions.
【作者單位】： 首都醫(yī)科大學(xué)化學(xué)生物學(xué)與藥學(xué)院藥劑學(xué)系;首都醫(yī)科大學(xué)化學(xué)生物學(xué)與藥學(xué)院藥藥物化學(xué)系;
【基金】：“十二五”重大新藥創(chuàng)制科技重大專(zhuān)項(xiàng)(2011ZX09302-007-01)~~
【分類(lèi)號(hào)】：R96;TB383.1

【共引文獻(xiàn)】

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