Bonferoni Maria Cristina, Sandri Giuseppina, Rossi Silvia, Ferrari Franca, Caramella Carla
University of Pavia, Department of Pharmaceutical Chemistry, Pavia, Italy.
Expert Opin Drug Deliv. 2009 Sep;6(9):923-39. doi: 10.1517/17425240903114142.
This review considers the application of chitosan and its salts in the delivery of drugs intended to act locally towards diseases of the mucosa itself (mucosal delivery), and to undergo systemic absorption by means of transmucosal routes (transmucosal delivery). Those chitosan properties that are particularly useful in mucosal and transmucosal delivery have been reviewed, such as mucoadhesion, penetration enhancement and peptidase inhibition behaviour. Chitosan bioactive properties have also been considered, such as anti-infective, haemostatic, wound healing and immune-stimulating activity. Chitosan is available with a wide range of molecular mass and deacetylation degree: the influence of these properties on polymer performance and solubility has been taken into account. As solubility in particular can strongly limit the results obtained at pH values close to neutrality, particular attention has been paid to chitosan salts and derivatives with modified solubility. Thanks to the presence of positively charged amino groups of the polymer, a subject of increasing interest is the exploitation of its interaction with acidic molecules having potential synergistic behaviour towards bioactive properties, or even with acidic drugs. The aim of the review is to describe not only some properties of chitosan, but also the way they can be modified by the acidic moiety.
本综述探讨了壳聚糖及其盐类在药物递送中的应用，这些药物旨在局部作用于黏膜自身疾病（黏膜给药），并通过黏膜途径进行全身吸收（透黏膜给药）。本文综述了壳聚糖在黏膜和透黏膜给药中特别有用的那些特性，例如黏膜黏附性、渗透增强作用和肽酶抑制行为。还考虑了壳聚糖的生物活性特性，例如抗感染、止血、伤口愈合和免疫刺激活性。壳聚糖具有广泛的分子量和脱乙酰度：已考虑了这些特性对聚合物性能和溶解性的影响。由于溶解性尤其会在接近中性的pH值下严重限制所获得的结果，因此特别关注了具有改性溶解性的壳聚糖盐和衍生物。由于聚合物带正电荷的氨基的存在，一个越来越受关注的主题是利用其与对生物活性具有潜在协同行为的酸性分子，甚至与酸性药物的相互作用。本综述的目的不仅是描述壳聚糖的一些特性，还包括它们如何被酸性部分修饰。
