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多柔比星聚合物膠束制備、表征及其體外釋藥研究

發(fā)布時(shí)間:2018-03-30 21:48

  本文選題:多柔比星 切入點(diǎn):Soluplus 出處:《中國(guó)抗生素雜志》2015年07期


【摘要】:目的制備多柔比星的soluplus聚合物膠束,并對(duì)其進(jìn)行體外評(píng)價(jià)。方法采用薄膜分散法-p H誘導(dǎo)法相結(jié)合制備多柔比星聚合物膠束;采用粒徑測(cè)定儀、透射電鏡、X-射線衍射(XRD)、差示掃描量熱法(DSC)及紅外光譜(FTIR)對(duì)其進(jìn)行表征;采用HPLC法測(cè)定膠束的包封率和載藥量;采用動(dòng)態(tài)膜透析法考察載藥膠束的體外釋藥特性。結(jié)果本研究制備的膠束呈球形或類(lèi)球形,平均粒徑為(67.57±2.9)nm,平均包封率為(77.81±4.03)%,平均載藥量(10.15±1.56)%;XRD和DSC結(jié)果表明多柔比星以無(wú)定型狀態(tài)或分子狀態(tài)包載在聚合物膠束中;FTIR結(jié)果表明多柔比星分子中羥基和聚合物的羰基之間形成了氫鍵;體外釋放結(jié)果表明多柔比星的soluplus聚合物膠束具有緩釋作用。結(jié)論該膠束制備工藝簡(jiǎn)單,其粒徑、包封率、載藥量可控,具有緩釋作用。
[Abstract]:Objective to prepare soluplus polymer micelles of doxorubicin and evaluate it in vitro. It was characterized by transmission electron microscopy (TEM), X-ray diffraction (XRD), differential scanning calorimetry (DSC) and infrared spectroscopy (FTIR), and the encapsulation efficiency and drug loading of micelles were determined by HPLC method. The release characteristics of drug-loaded micelles in vitro were investigated by dynamic membrane dialysis. Results the micelles prepared in this study were spherical or spherical. The average particle size was 67.57 鹵2.9 nm, the average entrapment efficiency was 77.81 鹵4.03, and the average drug loading was 10.15 鹵1.56 nm. The results of DSC and XRD showed that doxorubicin was carried in amorphous state or molecular state package in the polymer micelle. The results of FTIR showed that doxorubicin was hydroxyl and carbonyl group of polymer in doxorubicin molecule. Hydrogen bonds formed between them; The results of in vitro release showed that the soluplus polymer micelles of doxorubicin had a sustained release effect. Conclusion this micelle has a simple preparation process, its particle size, entrapment efficiency, drug loading is controllable, and it has a sustained release effect.
【作者單位】: 廣東醫(yī)學(xué)院藥學(xué)院;
【基金】:廣東省科技計(jì)劃項(xiàng)目(No.2014A020212296) 東莞市國(guó)際合作項(xiàng)目(No.2013508152013) 廣東省青年創(chuàng)新項(xiàng)目(2014) 廣東省大學(xué)生創(chuàng)新項(xiàng)目(No.1057113028,1057112043)
【分類(lèi)號(hào)】:R943

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