為增強(qiáng)抗腫瘤藥物的聚合物膠束的腫瘤靶向性遞送,本研究基于葉酸修飾的聚-（2-乙基-2-噁唑啉）-聚乳酸嵌段共聚物和聚-（2-乙基-2-噁唑啉）-聚乳酸嵌段共聚物,設(shè)計(jì)并制備了腫瘤細(xì)胞表面過表達(dá)的葉酸受體的配體葉酸修飾的pH敏感的聚合物膠束,用于包載抗腫瘤藥物阿霉素。所制備的載阿霉素的聚合物膠束的粒徑約為36nm,粒徑分布較窄,透射電鏡觀察膠束呈規(guī)則的球形,并具有pH敏感的釋藥行為。此外,體外的細(xì)胞攝取、細(xì)胞毒性以及荷瘤裸鼠體內(nèi)的近紅外熒光成像的結(jié)果均證明了所制備的聚合物膠束增強(qiáng)的腫瘤靶向性,并歸因于葉酸受體的介導(dǎo)和膠束pH敏感性的協(xié)同作用。因此,靶向葉酸受體的pH敏感膠束在腫瘤靶向遞送難溶藥物方面具有一定的潛力。 

【文章來源】：Journal of Chinese Pharmaceutical Sciences. 2020,29(09)CSCD

【文章頁數(shù)】：11 頁

【文章目錄】：
1. Introduction
2. Materials and methods
    2.1. Materials
    2.2. Preparation of drug-loaded polymeric micelles
    2.3. Characterization of polymeric micelles
    2.4. Cell culture
    2.5. Cytotoxicity assessment
    2.6. Cellular uptake assay
        2.6.1. Confocal microscopy observation
        2.6.2. Flow cytometric analysis
    2.7. Tumor model establishment
    2.8. Real-time tumor imaging
    2.9. Statistical analysis
3. Results and discussion
    3.1. Characterization of polymeric micelles
    3.2. In vitro cytotoxicity
    3.3. Cellular uptake
    3.4. Real-time tumor imaging and biodistribution
4. Conclusions



本文編號(hào)：3183717