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制备铁离子交联丙烯酰胺接枝聚(乙烯醇)/海藻酸钠微球及其在抗癌药物 5-氟尿嘧啶控制释放中的应用。

Preparation of ferric ion crosslinked acrylamide grafted poly (vinyl alcohol)/sodium alginate microspheres and application in controlled release of anticancer drug 5-fluorouracil.

机构信息

Department of Chemistry, Faculty of Science, Gazi University , Teknikokullar, Ankara , Turkey.

出版信息

Drug Deliv. 2014 May;21(3):213-20. doi: 10.3109/10717544.2013.844743. Epub 2013 Oct 17.

DOI:10.3109/10717544.2013.844743
PMID:24134656
Abstract

Ionically crosslinked microspheres of acrylamide (AAm) grafted poly (vinyl alcohol) (PVA)/sodium alginate (NaAlg) were prepared by crosslinking with FeCl3 and 5-fluorouracil (5-FU), which is an anticancer drug and was successfully encapsulated into the microspheres. The graft copolymer (PVA-g-PAAm) was characterized by using Fourier transform infrared spectroscopy (FTIR) and elemental analysis. The prepared microspheres were characterized by FTIR and scanning electron microscopy (SEM). Microspheres were also characterized by particle diameter, equilibrium swelling values and release profiles. The release studies were carried out at three pH values 1.2, 6.8 and 7.4, respectively, each for 2 h. The effects of preparation conditions as PVA-g-PAAm/NaAlg ratio, drug/polymer ratio, crosslinker concentration and exposure time to FeCl3 on the release of 5-FU were investigated for 6 h at 37 °C. The highest 5-FU release was found to be as 99.57% (w/w) at the end of 6 h for PVA-g-PAAm/NaAlg ratio of 1:4 (w/w), drug/polymer ratio of 1:8 (w/w), crosslinker concentration of 0.05 M and exposure time of 10 min. The release results were also supported by the swelling measurements of the microspheres. Release kinetics was described by Fickian and non-Fickian approaches.

摘要

用 FeCl3 和 5- 氟尿嘧啶(5-FU)交联制备了丙烯酰胺(AAm)接枝聚(聚乙烯醇)(PVA)/海藻酸钠(NaAlg)的离子交联微球,5-FU 是一种抗癌药物,成功地包裹在微球中。接枝共聚物(PVA-g-PAAm)用傅里叶变换红外光谱(FTIR)和元素分析进行了表征。用 FTIR 和扫描电子显微镜(SEM)对制备的微球进行了表征。还通过粒径、平衡溶胀值和释放曲线对微球进行了表征。在 pH 值分别为 1.2、6.8 和 7.4 的三个 pH 值下进行了释放研究,每个 pH 值释放 2 小时。在 37°C 下,分别研究了 6 小时内 PVA-g-PAAm/NaAlg 比、药物/聚合物比、交联剂浓度和暴露于 FeCl3 的时间对 5-FU 释放的影响。在 PVA-g-PAAm/NaAlg 比为 1:4(w/w)、药物/聚合物比为 1:8(w/w)、交联剂浓度为 0.05 M 和暴露时间为 10 min 的条件下,5-FU 的最大释放量为 99.57%(w/w)。微球的溶胀测量结果也支持了释放结果。释放动力学用菲克和非菲克方法进行描述。

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