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首页> 外文期刊>Carbohydrate Polymers: Scientific and Technological Aspects of Industrially Important Polysaccharides >Preparation and characterization of N-acetylchitosan,N-propionylchitosan and N-butyrylchitosan microspheres for controlled release of 6-mercaptourine
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Preparation and characterization of N-acetylchitosan,N-propionylchitosan and N-butyrylchitosan microspheres for controlled release of 6-mercaptourine

机译:N-乙酰壳聚糖,N-丙酰壳聚糖和N-丁酰壳聚糖微球的制备及表征,用于6-巯基鸟嘌呤的控释

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摘要

In this paper,biodegradable N-acylchitosan microspheres were prepared by a water-in-oil (w/o) interfacial N-acylation method for controlled release of 6-mercaptourine (6-MP).Acetic,propionic and n-butyric anhydrides were used as reagents for the interfacial N-acylation reaction to prepare N-acetylchitosan,N-propionylchitosan and N-butyrylchitosan microspheres.The onset time for the gelation of N-acylchitosan microspheres increased with increasing the molecular weight of used anhydride.While,the particle sizes of N-acetylchitosan microspheres (>50 murn),N-propionylchitosan microspheres (20-50 murn) and N-butyrylchitosan microspheres (~5 murn) decreased with the increase of substituted acyl chain length.The introduction of long acyl chains onto chitosan not only increased hydrophobicity,but also interfered crystallization of the polymer chains,leading to affecting the swelling and drug release properties of prepared N-acylchitosan microspheres.Drug release rates of the N-acylchitosan microspheres decreased in the sequence of N-propionylchitosan (t_50%~19 h)>N-butyrylchitosan (t_50%~36 h)>N-acetylchitosan (t_50%>100h),and were fitted with a two-phase percolation model.The enhancement of drug release for N-propionylchitosan and N-butyrylchitosan microspheres under lysozyme degradation were less significant than their N-acetylchitosan counterpart.The results suggested that the N-acylchitosan microspheres excipient as interesting candidates for drug delivery application.
机译:本文采用油包水界面N-酰化法制备了可生物降解的N-酰基壳聚糖微球,以控制6-巯基鸟嘌呤(6-MP)的释放,分别为乙酸,丙酸酐和正丁酸酐。用作界面N-酰化反应的试剂,以制备N-乙酰壳聚糖,N-丙酰壳聚糖和N-丁酰壳聚糖微球。随着使用酸酐的分子量增加,N-酰基壳聚糖微球凝胶化的开始时间增加。 N-乙酰壳聚糖微球(> 50微米),N-丙酰壳聚糖微球(20-50微米)和N-丁酰壳聚糖微球(〜5微米)的大小随取代酰基链长度的增加而减小。在壳聚糖上引入长酰基链不仅增加了疏水性,而且干扰了聚合物链的结晶,从而影响了制备的N-酰基壳聚糖微球的溶胀和药物释放性能。球形化合物按N-丙酰壳聚糖(t_50%〜19 h)> N-丁酰壳聚糖(t_50%〜36 h)> N-乙酰壳聚糖(t_50%> 100h)的顺序递减,并建立了两相渗流模型。溶菌酶降解下N-丙酰壳聚糖和N-丁酰壳聚糖微球释药的增强作用不如N-乙酰壳聚糖对应物显着。结果表明N-酰基壳聚糖微球作为赋形剂应用有趣的候选物。

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