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沉积温度对吲哚美辛微晶从层层组装的壳聚糖和海藻酸盐多层膜微胶囊中的释放速率的影响。

Deposition temperature effect on release rate of indomethacin microcrystals from microcapsules of layer-by-layer assembled chitosan and alginate multilayer films.

作者信息

Ye Shiqu, Wang Chaoyang, Liu Xinxing, Tong Zhen

机构信息

Research Institute of Materials Science, South China University of Technology, Guangzhou 510640, China.

出版信息

J Control Release. 2005 Sep 2;106(3):319-28. doi: 10.1016/j.jconrel.2005.05.006.

Abstract

Indomethacin (IDM) microcrystals sized 5 approximately 10 microm were directly encapsulated with nature polysaccharides chitosan (CHI) and sodium alginate (ALG) through layer-by-layer (LbL) self-assembly. Due to partial dissolution of IDM in the deposition solution, the retention of the IDM microcrystals gradually decreased with increasing deposition times and became 47.7% as 10 layers of polysaccharides formed. The release rate of the IDM from the microcapsules was monitored with UV absorbance. The half release time t(1/2) of IDM in the microcapsule increased with the layer number and the initial burst phenomenon was relieved after encapsulation. It was found that added NaCl did not affect the release rate even up to 0.5 M of its concentration, while increasing the release temperature remarkably speeded up the release process. The prolonged release of the encapsulated IDM was still observed when the aqueous release solution containing 20 vol.% ethanol. It was very significant that increasing deposition temperature from 20 to 60 degrees C reduced the release rate efficiently, owing to the increase in multilayer thickness and formation of a more perfect multilayer film. This finding provides a new and simple method to control the permeability of the LbL assembled multilayer films. Because of the biodegradability of CHI and ALG and various methods to tune the release rate, the LbL self-assembly on drug microcrystals promises high potential for encapsulation used in controlled release.

摘要

将尺寸为5至10微米的吲哚美辛(IDM)微晶通过层层(LbL)自组装直接用天然多糖壳聚糖(CHI)和海藻酸钠(ALG)包封。由于IDM在沉积溶液中的部分溶解,IDM微晶的保留率随着沉积次数的增加而逐渐降低,在形成10层多糖时降至47.7%。通过紫外吸光度监测IDM从微胶囊中的释放速率。微胶囊中IDM的半衰期t(1/2)随层数增加,包封后初始突发现象得到缓解。发现添加NaCl即使浓度高达0.5 M也不影响释放速率,而提高释放温度显著加快了释放过程。当水性释放溶液中含有20体积%乙醇时,仍观察到包封的IDM的缓释现象。非常重要的是,将沉积温度从20℃提高到60℃可有效降低释放速率,这是由于多层厚度增加以及形成了更完美的多层膜。这一发现提供了一种控制LbL组装多层膜渗透性的新的简单方法。由于CHI和ALG的生物可降解性以及各种调节释放速率的方法,在药物微晶上进行LbL自组装在控释包封方面具有很高的潜力。

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