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用于药物递送应用的原位交联N-马来酰壳聚糖-氧化海藻酸钠水凝胶的制备

Preparation of In Situ Cross-Linked N-Maleoyl Chitosan-Oxidized Sodium Alginate Hydrogels for Drug Delivery Applications.

作者信息

Pasaribu Subur P, Kaban Jamaran, Ginting Mimpin, Silalahi Jansen

机构信息

Department of Chemistry, Faculty of Mathematics and Natural Sciences, Universitas Sumatera Utara, Medan-20155, Indonesia.

Department of Chemistry, Faculty of Mathematics and Natural Sciences, Mulawarman University, Samarinda-75123, Indonesia.

出版信息

Open Access Maced J Med Sci. 2019 Oct 14;7(21):3546-3553. doi: 10.3889/oamjms.2019.850. eCollection 2019 Nov 15.

Abstract

AIM

This study was aimed to prepare in situ cross-linked N-maleoyl chitosan - oxidised sodium alginate (MCS - OSA) hydrogel loaded with metronidazole (MTZ) for drug delivery applications.

METHODS

The hydrogel was prepared by in situ cross-linking via Schiff base reaction between amine (-NH2) groups from MCS and aldehyde (-CHO) groups from OSA at the different ratio, and the MTZ was loaded into the hydrogels along with the gelatin processes.

RESULTS

The highest drug entrapment efficiency (DEE) was exhibited by MTZ-H3 (5: 5) with DEE of 99.20% and a gel fraction of 97.52%. FTIR results revealed that Schiff base reaction was occurred by the absorption peak of -C = N- groups at 1628 cm and indicated that there is insignificant alteration at different ratio of MCS and OSA. The best sustained of in vitro release profiles of MTZ was shown by MTZ-H3, which is 74.92% and 75.65% at pH 1.2 and 7.4 for 12 h of release, respectively.

CONCLUSION

The optimised ratio between MCS and OSA to prepare in situ cross-linked hydrogels were found to be 5:5 according to the results of DEE and in vitro drug release profiles of MTZ and the MTZ loaded MCS-OSA hydrogels have a great potential which can be applied in biomedical applications.

摘要

目的

本研究旨在制备负载甲硝唑(MTZ)的原位交联N-马来酰壳聚糖-氧化海藻酸钠(MCS-OSA)水凝胶用于药物递送。

方法

通过MCS中的胺基(-NH2)与OSA中的醛基(-CHO)之间的席夫碱反应,以不同比例原位交联制备水凝胶,并在明胶制备过程中将MTZ负载到水凝胶中。

结果

MTZ-H3(5:5)表现出最高的药物包封率(DEE),为99.20%,凝胶分数为97.52%。傅里叶变换红外光谱(FTIR)结果显示,在1628 cm处出现了-C=N-基团的吸收峰,表明席夫碱反应发生,且不同比例的MCS和OSA之间无明显变化。MTZ-H3表现出最佳的MTZ体外释放曲线,在pH 1.2和7.4条件下12小时释放率分别为74.92%和75.65%。

结论

根据DEE以及MTZ的体外药物释放曲线结果,发现制备原位交联水凝胶的MCS和OSA的最佳比例为5:5,且负载MTZ的MCS-OSA水凝胶具有很大的应用潜力,可应用于生物医学领域。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/5805/6986498/4f60596cc7d8/OAMJMS-7-3546-g001.jpg

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