本文選題：聚乙二醇 + 左旋聚乳酸��； 參考：《首都醫(yī)科大學(xué)學(xué)報(bào)》2015年02期

【摘要】：目的制備聚乙二醇(polyethylene glycol,PEG)包裹表阿霉素脂質(zhì)體,對(duì)其藥劑學(xué)性質(zhì)和活性進(jìn)行評(píng)價(jià)。方法采用乳化溶劑揮發(fā)法制備聚乙二醇包裹表阿霉素的脂質(zhì)體,用掃描電鏡和透射電鏡觀察其形態(tài),用激光納米粒度儀測(cè)定粒徑分布及Zeta電位、并對(duì)包封率、穩(wěn)定性及體外釋藥特性進(jìn)行研究,采用MMT法和S180小鼠模型評(píng)價(jià)體內(nèi)外抗腫瘤活性。結(jié)果聚乙二醇包裹表阿霉素的脂質(zhì)體的粒徑為(231.4±2.0)nm,動(dòng)電位為(-25.62±0.68)m V,包封率為(53.14±4.85)%,各項(xiàng)穩(wěn)定性均有明顯提高,體外釋放緩慢,小鼠劑量可增加到6μmol/kg,給藥間隔可延長(zhǎng)至72 h,并顯示比表阿霉素好的抗腫瘤活性。結(jié)論本實(shí)驗(yàn)獲得了較理想的聚乙二醇包裹表阿霉素脂質(zhì)體,體外釋藥符合長(zhǎng)效制劑特征,血漿中穩(wěn)定,具有p H敏感性,可改善表阿霉素用藥安全性,延長(zhǎng)藥物作用時(shí)間。
[Abstract]:Aim to prepare PEG coated epirubicin liposome and evaluate its pharmacological properties and activity. Methods the polyethylene glycol encapsulated adriamycin liposomes were prepared by emulsifying solvent volatilization method. The morphology of the liposomes was observed by scanning electron microscope and transmission electron microscope. The particle size distribution and Zeta potential were measured by laser nano-particle size analyzer, and the encapsulation efficiency was evaluated. The stability and drug release characteristics in vitro were studied. The anti-tumor activity in vivo and in vitro was evaluated by MMT method and S180 mouse model. Results the particle size, dynamic potential and entrapment efficiency of PEG-encapsulated epirubicin liposome were 231.4 鹵2.0 nm, 25.62 鹵0.68 mg / v and 53.14 鹵4.85 mg 路L ~ (-1), respectively. The stability of the liposomes was significantly improved and the release in vitro was slow. The dose of mice was increased to 6 渭 mol / kg, the interval of administration was prolonged to 72 hours, and the antitumor activity was better than that of epirubicin. Conclusion in this experiment, a more ideal PEG-encapsulated epirubicin liposome was obtained. The drug release in vitro was consistent with the characteristics of long-acting preparation, stable in plasma and sensitive to pH, which could improve the safety of epirubicin and prolong the time of drug action.
【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)院藥物化學(xué)系;
【基金】：“十二五”重大新藥創(chuàng)制科技重大專項(xiàng)(2011ZX09302-007-01)~~
【分類號(hào)】：R943

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