本文關(guān)鍵詞： 主動(dòng)靶向 還原敏感性 聚合物膠束 阿霉素 細(xì)胞毒性　出處：《西北師范大學(xué)學(xué)報(bào)(自然科學(xué)版)》2016年06期 　論文類型：期刊論文

【摘要】：先用開環(huán)聚合(ROP)合成大分子的RAFT試劑(PCL-SS-DMP),然后采用可逆加成-斷裂鏈轉(zhuǎn)移(RAFT)法,合成了親水性的N-(2-羥丙基)甲基丙烯酰胺(HPMA)和主動(dòng)靶向配體葉酸單體丙烯酰胺-葉酸(AA-FA),制備了具有主動(dòng)靶向還原敏感性的兩親性嵌段共聚物(PCL-SS-b-PHPMA-b-PFA),用核磁共振(1 HNMR)對(duì)其結(jié)構(gòu)進(jìn)行表征.此共聚物在水溶液中可自組裝形成聚合物膠束,由透射電子顯微鏡(TEM)和動(dòng)態(tài)光散射(DLS)表征可知膠束為尺寸約100nm的球形顆粒,用DLS觀察到膠束粒徑在10mmol二硫蘇糖醇作用下隨時(shí)間的增加而逐漸增大.以抗癌藥物阿霉素(DOX)為模型藥物,研究載藥膠束在模擬人體環(huán)境中的控釋行為.用四氮唑鹽還原法(MTT)研究不同濃度的聚合物膠束對(duì)人宮頸癌HeLa細(xì)胞的細(xì)胞毒性,并評(píng)價(jià)載藥膠束在細(xì)胞中的抗癌效果.結(jié)果表明,PCL-SS-b-PHPMA-b-PFA可作為包載DOX的一種新型納米材料,載藥膠束的體外釋放呈明顯的還原依賴性,且具有較好的體外抗腫瘤活性,有望成為理想的抗腫瘤藥物載體.
[Abstract]:The RAFT reagent, PCL-SS-DMPN, was synthesized by ring-opening polymerization (RP-ROP), and then the reversible addition-break chain transfer method (RATFT) was used. Amphiphilic block copolymers (PCL-SS-b-PHPMA-b-PFAA) with active targeting ligands, acrylamide / folate (AA-FAA) and active ligand folate monomers, were synthesized by the synthesis of hydrophilic N-PMA-2-hydroxypropyl) methacrylamide (HPMA-b-PFAA). The amphiphilic block copolymers with active targeting reduction sensitivity were prepared by 1HNMRs. The copolymer is self-assembled in aqueous solution to form polymer micelles. The micelles were characterized by TEM (TEM) and DLSs (dynamic light scattering). The micelles were spherical particles about 100nm in size. It was observed by DLS that the micelle particle size increased with the increase of time under the action of 10mmol / L disulfide. Dox, an anticancer drug, was used as the model drug. To study the controlled release behavior of drug-loaded micelles in simulated human environment, the cytotoxicity of different concentrations of polymer micelles to human cervical cancer HeLa cells was studied by tetrazolium reduction method. The results showed that PCL-SS-b-PHPMA-b-PFA could be used as a new nano-material for encapsulating DOX, and the release of drug-loaded micelles was obviously reductive in vitro and had good antitumor activity in vitro, the results showed that PCL-SS-b-PHPMA-b-PFA could be used as a novel nano-material for encapsulating DOX. It is expected to be an ideal antitumor drug carrier.
【作者單位】： 西北師范大學(xué)化學(xué)化工學(xué)院;
【分類號(hào)】：TQ317.5;;R945
，

本文編號(hào)：1539832