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静电纺丝法制备具有黏附性的 N,N,N-三甲基壳聚糖-高半胱氨酸硫内酯/藻酸盐/卡拉胶载喜树碱电纺纤维

Electrosprayed polyelectrolyte complexes between mucoadhesive N,N,N,-trimethylchitosan-homocysteine thiolactone and alginate/carrageenan for camptothecin delivery.

机构信息

Program of Petrochemistry and Polymer Science, Faculty of Science, Chulalongkorn University, 254 Phayathai Road, Pathumwan, Bangkok 10330, Thailand.

出版信息

Carbohydr Polym. 2012 Nov 6;90(4):1469-79. doi: 10.1016/j.carbpol.2012.07.017. Epub 2012 Jul 16.

Abstract

Novel hydrogel polyelectrolyte complexes (PECs) between the N,N,N,-trimethylchitosan-homocysteine thiolactone (TM-HT-chitosan) and two anionic polymers were investigated. The particles of pure thiolated chitosan and its PECs with alginate and carrageenan were fabricated using the electrospray ionization technique. The hydrogel PEC particles were characterized by scanning electron microscopy, dynamic light scattering, Fourier transform infrared microscopy, thermogravimetric analysis, encapsulation efficiency (EE), mucoadhesive property and in vitro drug release behavior. TM-HT-chitosan/alginate particles could be loaded with camptothecin (CPT), employed as a model anti-cancer drug, at an over 70% EE, and revealed both a reduced burst effect and a prolonged release of CPT over 3 days. The resultant TM-HT-chitosan/alginate PEC particles displayed a 5.60-, 1.86- and 1.55-fold stronger mucoadhesive property compared to that of the unmodified chitosan/alginate PEC at pH 1.2, 4.0 and 6.4, respectively, and this was not affected by the CPT loading level.

摘要

研究了 N,N,N-三甲基壳聚糖-同型半胱氨酸硫内酯(TM-HT-壳聚糖)与两种阴离子聚合物之间的新型水凝胶聚电解质复合物(PECs)。使用电喷雾电离技术制备了纯巯基化壳聚糖及其与藻酸盐和卡拉胶的 PEC 颗粒。通过扫描电子显微镜、动态光散射、傅里叶变换红外显微镜、热重分析、包封效率(EE)、粘膜粘附性能和体外药物释放行为对水凝胶 PEC 颗粒进行了表征。TM-HT-壳聚糖/藻酸盐颗粒可以负载喜树碱(CPT)作为模型抗癌药物,EE 超过 70%,并且在 3 天内显示出 CP 的释放减少和释放延长。与未修饰的壳聚糖/藻酸盐 PEC 相比,所得 TM-HT-壳聚糖/藻酸盐 PEC 颗粒在 pH 值为 1.2、4.0 和 6.4 时的粘膜粘附性能分别提高了 5.60、1.86 和 1.55 倍,并且不受 CPT 负载水平的影响。

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