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A Facile Synthesis of Itaconic Acid Based Biodegradable Co-polyesters: An In-Vitro Anticancer Evaluation and Controlled Drug Delivery System

机译:基于衣康酸的可生物降解共聚酯的简便合成:体外抗癌评估和药物控制系统

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A series of aliphatic co-polyesters were prepared via one-step polycondensation reaction of itaconic acid, 1,4-cyclohexane dimethanol and diols using titanium tetraisopropoxide (TTIP) as a catalyst. The chemical structure of the repeating units present in the polymer chains were confirmed by FTIR, H-1 and C-13 NMR spectral data. The glass transition temperature (T-g), melting temperature (T-m) and decomposition temperature (T-d) of the co-polyesters were evaluated by Differential Scanning Calorimetry (DSC). The biodegradability of the synthesized co-polyesters would be qualitatively studied by hydrolytic degradation at different pH followed by studying the change in surface morphology of the co-polyesters before and after degradation using Scanning Electron Microscope (SEM) images and the extent of crystallinity would also be studied using wide angle X-ray Diffraction (W-XRD) data. In-vitro anticancer activity of the synthesized co-polyesters were tested against human breast cancer (MCF-7) cell lines, all the co-polyesters show good IC50 value at lower concentration but among them PICMCD [Poly (1,4-cyclohexanedimethanol itaconate-co-1,4-cyclohexane diol itaconate)] has higher toxicity on MCF-7 cells. The drug delivery property of the co-polyesters would be investigated on tamoxifen citrate using spray down tablet coating process and PICMCD found to be a potential drug carrier. Graphic
机译:使用四异丙醇钛(TTIP)作为衣康酸,1,4-环己烷二甲醇和二醇的一步缩聚反应,制备了一系列脂族共聚酯。通过FTIR,H-1和C-13 NMR光谱数据证实了存在于聚合物链中的重复单元的化学结构。通过差示扫描量热法(DSC)评价共聚酯的玻璃化转变温度(T-g),熔融温度(T-m)和分解温度(T-d)。定性研究合成的共聚酯的生物降解性,方法是在不同pH值下进行水解降解,然后使用扫描电子显微镜(SEM)图像研究降解前后的共聚酯表面形态的变化,以及结晶度。使用广角X射线衍射(W-XRD)数据进行研究。测试了合成的共聚酯对人乳腺癌(MCF-7)细胞系的体外抗癌活性,所有共聚酯在较低浓度下均显示出良好的IC50值,但其中PICMCD [聚(1,4-环己烷二甲醇衣康酸酯) -co-1,4-环己烷二醇衣康酸酯)]对MCF-7细胞具有更高的毒性。共聚酯的药物传递特性将通过喷雾片剂包衣法在柠檬酸他莫昔芬上进行研究,发现PICMCD是潜在的药物载体。图形化

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