Evaluation of the mucoadhesive properties of N-trimethyl chitosan chloride
Evaluation of the mucoadhesive properties of N-trimethyl chitosan chloride
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DOI：
10.1081/ddc-120016684
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发表时间：
2003-01-01
影响因子：
3.4
通讯作者：
Kotze, AF
中科院分区：
文献类型：
--
作者：
Snyman, D;Hamman, JH;Kotze, AF
以前的研究已经确定，N-三甲基壳聚糖氯化物（TMC）是一种有效的吸收促进剂，肽和大的亲水性化合物跨粘膜表面，特别是在中性和碱性环境中，壳聚糖是无效的吸收促进剂。TMC的季铵化程度对其增吸性能有重要影响。合成了几种具有不同季铵化程度的TMC聚合物，并通过SEC/MALLS测定了聚合物的分子量。TMC聚合物的粘膜粘附特性用基于Willhelmy板法的改进的张力计测量。TMC聚合物对聚合物和粘液的混合物的表面张力的影响用Du Nouy张力计测量。合成的TMC聚合物的季铵化度在22.1%和48.8%之间，并且对于所有聚合物，分子量高于100，000 g/mol。随着TMC聚合物的季铵化程度的增加，粘膜粘附性降低。聚合物和粘液的混合物的表面张力分析显示了过度聚合物水合对粘膜粘附的影响。结果表明，TMC的季铵化程度对该聚合物的粘膜粘附特性具有显著影响：尽管TMC聚合物的粘膜粘附特性低于原始壳聚糖，但它们仍然保留了足够的粘膜粘附特性，以成功地包含到粘膜粘附剂型中。
Previous studies have established that N-trimethyl chitosan chloride (TMC) is a potent absorption enhancer for peptides and large hydrophilic compounds across mucosal surfaces, especially in neutral and basic environments where chitosan is ineffective as an absorption enhancer. The degree of quaternization of TMC plays an important role on its absorption-enhancing properties. Several TMC polymers with different degrees of quaternization were synthesized and the molecular mass of the polymers was determined by SEC/MALLS. The mucoadhesive properties of the TMC polymers were measured with a modified tensiometer based on the Willhelmy plate method. The effect of the TMC polymers on the surface tension of a mixture of polymer and mucus was measured with a Du Nouy tensiometer. The degrees of quaternization of the synthesized TMC polymers were between 22.1% and 48.8% and the molecular mass was above 100,000 g/mole for all the polymers. A decrease in mucoadhesivity with an increase in the degree of quaternization of the TMC polymers was found. Surface-tension analysis of a mixture of polymer and mucus showed the effect of excessive polymer hydration on mucoadhesion. The results show that the degree of quaternization of TMC had a pronounced effect on the mucoadhesive properties of this polymer: Although the mucoadhesive profiles for the TMC polymers were lower than the original chitosan, they still retained sufficient mucoadhesive properties for successful inclusion into mucoadhesive dosage forms.