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壳聚糖包衣的海藻酸钙凝胶珠中亮蓝的释放行为:制备方法的影响

The release behavior of brilliant blue from calcium-alginate gel beads coated by chitosan: the preparation method effect.

作者信息

Shu X Z, Zhu K J

机构信息

Department of Polymer Science and Engineering, Zhejiang University, Hangzhou, People's Republic of China.

出版信息

Eur J Pharm Biopharm. 2002 Mar;53(2):193-201. doi: 10.1016/s0939-6411(01)00247-8.

Abstract

The aim of this study is to reveal how the release behavior of a model drug (brilliant blue, BB) from chitosan coating calcium-alginate gel beads (CCAGB) was influenced by the preparation methods. The CCAGB were prepared by dropping alginate solution into CaCl(2)/chitosan solution (method 1(a)), or into chitosan solution then gelled by CaCl(2) (method 1(b)), or into CaCl(2) solution then coated by chitosan (method 2). Scanning electron microscopy was used for morphology observation, and elemental analysis was applied to determine the chitosan content bound on calcium-alginate gel beads (CAGB). Compared to CAGB, the dried CCAGB had poorer shape and rougher surface morphology especially in methods 1(a) and (b); moreover, CCAGB was found to be more instable in 0.9% NaCl and serious burst of beads occurred when high concentration of alginate (3.0 and 5.0% w/v) was used. The influence on BB release from the beads by chitosan coating was not only related to the chitosan density on bead surface, but also preparation method and other factors. Under un-dried bead state in method 1(a), the increase of chitosan content prolonged BB release in 0.9% (w/v) NaCl; while in method 2, the increase of chitosan concentration over 0.1% (w/v) (3.0% (w/v) alginate concentration was used) resulted in more serious burst of beads and hence facilitated BB release. Furthermore, in both methods 1(a) and 2, the increase of alginate from 1.5 to 3.0 or 5.0% (w/v) usually resulted in the significant burst of beads and accelerated BB release when 0.3 or 0.5% (w/v) chitosan was used for coating. Drying process greatly influenced BB release profile due to the destroying of alginate-chitosan film. The acceleration of BB release from CCAGB by drying process was more significant in the case of method 1 than of method 2.

摘要

本研究的目的是揭示模型药物(亮蓝,BB)从壳聚糖包衣的海藻酸钙凝胶珠(CCAGB)中的释放行为是如何受到制备方法影响的。CCAGB通过以下方法制备:将海藻酸钠溶液滴入CaCl₂/壳聚糖溶液中(方法1(a)),或滴入壳聚糖溶液中然后用CaCl₂凝胶化(方法1(b)),或滴入CaCl₂溶液中然后用壳聚糖包衣(方法2)。使用扫描电子显微镜进行形态观察,并应用元素分析来测定结合在海藻酸钙凝胶珠(CAGB)上的壳聚糖含量。与CAGB相比,干燥后的CCAGB形状较差且表面形态更粗糙,尤其是在方法1(a)和1(b)中;此外,发现CCAGB在0.9% NaCl中更不稳定,当使用高浓度海藻酸钠(3.0和5.0% w/v)时珠子会严重破裂。壳聚糖包衣对珠子中BB释放的影响不仅与珠子表面的壳聚糖密度有关,还与制备方法和其他因素有关。在方法1(a)的未干燥珠子状态下,壳聚糖含量的增加延长了BB在0.9%(w/v)NaCl中的释放;而在方法2中,壳聚糖浓度超过0.1%(w/v)(使用3.0%(w/v)海藻酸钠浓度)的增加导致珠子更严重的破裂,从而促进了BB的释放。此外,在方法1(a)和2中,当使用0.3或0.5%(w/v)壳聚糖进行包衣时,海藻酸钠从1.5%增加到3.0%或5.0%(w/v)通常会导致珠子显著破裂并加速BB释放。干燥过程由于海藻酸盐 - 壳聚糖膜的破坏而极大地影响了BB的释放曲线。干燥过程对CCAGB中BB释放的加速在方法1的情况下比方法2更显著。

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