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Effect of molecular weight and degree of deacetylation on controlled release of isoniazid from chitosan microspheres

机译：分子量和脱乙酰度对异烟肼从壳聚糖微球中控释的影响

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Glutaraldehyde cross-linked chitosan microspheres for controlled release of isoniazid were prepared using chitosan of different molecular weights (MWs) and degrees of deacetylation (DDAs). Chitosan microspheres were characterized for their size, hydrophobocity, degree of swelling and loading of isoniazid. Hydrophobicity of chitosan microspheres increased on increasing the degree of cross-linking and MW of chitosan. Chitosan microspheres with high degree of deacetylation (DDA) (75 wt%), high MW chitosan (2227 kg mol(-1)), and with 12 wt% concentration of glutaraldehyde showed optimum loading and release of isoniazid. The isoniazid from chitosan microspheres was released in two steps, i.e. burst (%R-B) and controlled (%R-C) steps. The microspheres with low MW chitosan (260 kg mol-1) and low DDA (48 wt%) showed prominent burst release of isoniazid, but microspheres with high MW chitosan (2227 kg mol(-1)) and high DDA (75 wt%) have released more isoniazid in a controlled manner (60 wt%) at 37 degrees C in a solution of pH 5.0 +/- 0.1. The burst step of drug release (%R-B) has followed first order kinetics, whereas controlled step of drug release (%R-C) followed zero order kinetics. The burst step of drug release was Fickian and controlled step was non-Fickian in nature. The diffusion constant (D) for isoniazid release was influenced by the properties of chitosan and degree of cross-linking. Copyright (c) 2007 John Wiley & Sons, Ltd.
机译：使用不同分子量（MWs）和脱乙酰度（DDAs）的壳聚糖制备用于异烟肼控制释放的戊二醛交联壳聚糖微球。壳聚糖微球的大小，疏水性，溶胀度和异烟肼载量得到了表征。壳聚糖微球的疏水性随着壳聚糖交联度和分子量的增加而增加。具有高脱乙酰度（DDA）（75 wt％），高分子量壳聚糖（2227 kg mol（-1））和12 wt％戊二醛浓度的壳聚糖微球显示出最佳的负载和异烟肼的释放。壳聚糖微球中的异烟肼分两个步骤释放，即爆破（％R-B）和受控（％R-C）步骤。具有低分子量壳聚糖（260 kg mol-1）和低DDA（48 wt％）的微球显示出异烟肼的突释释放，但是具有高分子量壳聚糖（2227 kg mol（-1））和高DDA（75 wt％）的微球）在37°C下在pH 5.0 +/- 0.1的溶液中以受控方式（60 wt％）释放了更多的异烟肼。药物释放的突发步骤（％R-B）遵循一级动力学，而药物释放的受控步骤（％R-C）遵循零级动力学。本质上，药物释放的爆发步骤是菲克式，而受控步骤是非菲克式。异烟肼释放的扩散常数（D）受壳聚糖性质和交联度的影响。版权所有（c）2007 John Wiley＆Sons，Ltd.

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