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Synthesis and characterization of a non-cytotoxic and biocompatible acrylamide grafted pullulan - Application in pH responsive controlled drug delivery

机译:非细胞毒性和生物相容性丙烯酰胺接枝淀粉的合成与表征 - 在pH激素响应控制药物递送中的应用

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The aim of present study was to develop a pH responsive rate controlling polymer by acrylamide grafting onto pullulan. Grafting was performed using free radical induced microwave assisted irradiation technique using ceric ammonium nitrate as free radical inducer. Acrylamide grafted pullulan (Aam-g-pull) was characterized by Fourier transform infrared spectroscopy, solid state C-13 nuclear magnetic resonance and field emission scanning electron microscopy. In vitro enzymatic degradation of Aam-g-pull showed degradation of 22.45% after 8 h with degradation rate constant (k) of 0.019 min(-1). In vitro cytotoxicity test did not show cell viability below 80% on HepG2 cell line. Pirfenidone tablets were prepared by utilizing wet granulation method using Aam-g-pull as the only rate controlling polymer. The tablets were characterized in terms of in-process quality control parameters like weight variation, hardness, assay, and in vitro dissolution study. The dissolution study showed that the cumulative drug release in phosphate buffer pH 6.8 (rel(3) h = 44.12 +/- 0.56%) got a significant jump as compared to the release in 0.1 N hydrochloric acid (rel(2) (h) = 26.78 +/- 0.23%), confirming the material to be pH responsive. Aam-g-pull can be used as pH responsive rate controlling polymer. (C) 2018 Elsevier B.V. All rights reserved.
机译:目前研究的目的是通过丙烯酰胺接枝在胰蛋白酶上进行pH响应速率控制聚合物。使用自由基诱导的微波辅助辐射技术使用酸氨铵作为自由基诱导剂进行接枝。通过傅里叶变换红外光谱,固态C-13核磁共振和场发射扫描电子显微镜表征丙烯酰胺接枝的胰蛋白(AAM-G拉)。在8小时后,AAM-G拉的体外酶促降解显示为0.019分钟的降解速率(K)后的8小时后22.45%。体外细胞毒性试验未在HepG2细胞系上显示低于80%的细胞活力。通过使用AAM-G拉的湿造粒方法作为唯一速率控制聚合物来制备Pirfenidone片剂。本发明的药片以体重变化,硬度,测定和体外溶解研究等工艺质量控制参数表征。溶解研究表明,磷酸盐缓冲液pH6.8中的累积药物释放(Rel(3)H = 44.12 +/- 0.56%)与0.1N盐酸中的释放相比(rel(2)(h) = 26.78 +/- 0.23%),确认材料响应物的pH值。 AAM-G拉链可用作pH响应速率控制聚合物。 (c)2018年elestvier b.v.保留所有权利。

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