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纳曲酮从聚(N-异丙基丙烯酰胺)微凝胶中的缓释。

Sustained release of naltrexone from poly(n-isopropylacrylamide) microgels.

作者信息

Kjøniksen Anna-Lena, Calejo Maria Teresa, Zhu Kaizheng, Cardoso Ana Maria S, de Lima Maria C Pedroso, Jurado Amália S, Nyström Bo, Sande Sverre Arne

机构信息

Department of Pharmacy, School of Pharmacy, University of Oslo, Blindern, N-0316, Oslo, Norway; Faculty of Engineering, Østfold University College, N-1757, Halden, Norway.

出版信息

J Pharm Sci. 2014 Jan;103(1):227-34. doi: 10.1002/jps.23780. Epub 2013 Nov 11.

Abstract

The release of the opioid antagonist naltrexone from neutral poly(N-isopropylacrylamide) (PNIPAAM) microgels and negatively charged PNIPAAM microgels containing acrylic acid groups (PNIPAAM-co-PAA) has been studied at various microgel and drug concentrations. The release curves were found to be well represented by the Weibull equation. The release rates were observed to be dependent on the microgel concentration. At most conditions, the release from the charged microgels was slower than for the neutral microgels. In addition, the charged microgels exhibited a release lag time, which was dependent on the microgel concentration. No significant lag time could be observed for the neutral microgels. Increasing the naltrexone concentration did not significantly affect the release rates from the neutral microgels, but the release from the charged microgels became faster. The microgels did not exhibit any significant cytotoxic effect on HeLa cells at the tested concentrations.

摘要

已在不同微凝胶和药物浓度下研究了阿片类拮抗剂纳曲酮从中性聚(N-异丙基丙烯酰胺)(PNIPAAM)微凝胶以及含有丙烯酸基团的带负电荷的PNIPAAM微凝胶(PNIPAAM-co-PAA)中的释放情况。发现释放曲线能用威布尔方程很好地表示。观察到释放速率取决于微凝胶浓度。在大多数情况下,带电荷微凝胶的释放比中性微凝胶慢。此外,带电荷微凝胶表现出释放滞后时间,该时间取决于微凝胶浓度。中性微凝胶未观察到明显的滞后时间。增加纳曲酮浓度对中性微凝胶的释放速率没有显著影响,但带电荷微凝胶的释放变得更快。在所测试的浓度下,微凝胶对HeLa细胞未表现出任何显著的细胞毒性作用。

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