Why is chitosan mucoadhesive?
Why is chitosan mucoadhesive?
复制标题
DOI：
10.1021/bm800276d
复制
发表时间：
2008-07-01
影响因子：
6.2
通讯作者：
Khutoryanskiy, Vitaliy V.
中科院分区：
文献类型：
--
作者：
Sogias, Ioannis A.;Williams, Adrian C.;Khutoryanskiy, Vitaliy V.
壳聚糖是一种生物相容性和可生物降解的氨基多糖，其可溶于pH < 6.5的水溶液中。由于其优异的粘膜粘附特性，其已被广泛用于开发药物递送系统。尽管许多研究报道壳聚糖是粘膜粘附的，但壳聚糖和粘蛋白之间相互作用的性质仍然不清楚。在这里，我们已经研究了伯氨基的作用和静电吸引力的作用，氢键，和疏水作用的聚集在壳聚糖的存在下的胃粘蛋白。通过其半乙酰化减少氨基的数量导致壳聚糖的pH溶解度窗口扩大至pH 7.4，但也降低了其聚集粘蛋白的能力。我们证明，壳聚糖和胃粘蛋白之间的静电吸引力可以被抑制在0.2 mol/L氯化钠的存在下，然而，这并不能阻止粘蛋白颗粒的聚集在这种生物聚合物的存在下。溶液中8 mol/L尿素或10%v/v乙醇的存在也会影响壳聚糖存在下的粘蛋白聚集，分别证明了氢键和疏水效应在粘膜粘附中的作用。
Chitosan is a biocompatible and biodegradable amino polysaccharide, which is soluble in aqueous solutions at pH < 6.5. It has been widely used for developing drug delivery systems because of its excellent mucoadhesive properties. Although many studies report on chitosan being mucoadhesive, the nature of interactions between chitosan and mucin remains poorly defined. Here, we have examined the role of primary amino groups and the role of electrostatic attraction, hydrogen bonding, and hydrophobic effects on aggregation of gastric mucin in the presence of chitosan. Reducing the number of amino groups through their half acetylation results in expansion of chitosan's pH-solubility window up to pH 7.4 but also reduces its capacity to aggregate mucin. We demonstrated that electrostatic attraction forces between chitosan and gastric mucin can be suppressed in the presence of 0.2 mol/L sodium chloride; however, this does not prevent the aggregation of mucin particles in the presence of this biopolymer. The presence of 8 mol/L urea or 10% v/v ethanol in solutions also affects mucin aggregation in the presence of chitosan, demonstrating the role of hydrogen bonding and hydrophobic effects, respectively, in mucoadhesion.