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用于口腔黏膜递药的黏膜黏附聚合物:综述。

Mucoadhesive polymers for oral transmucosal drug delivery: a review.

机构信息

Service of Stomatology, University General Hospital of Valencia, Spain.

出版信息

Curr Pharm Des. 2012;18(34):5497-514. doi: 10.2174/138161212803307545.

Abstract

The oral mucosa offers an interesting site for the application of dosage forms that release drugs within/throughout the oral mucosa, by assuring a high drug bioavailability for topic and systemic effects. However, the relative permeability of the oral mucosa and the washing effect related to the oral fluids and mechanical stresses must be considered in the formulation of oral dosage forms. Since a sustained drug release can be guaranteed only if dosage forms remain in contact with the oral site of absorption/application for a prolonged time, the development of mucoadhesive dosage forms is mandatory. The mucoadhesion is a complex phenomenon and the mucoadhesive bond consists of two different parts, the mucoadhesive polymers and the mucous substrate. In addition to factors related to the oral mucosa and oral environment features, the physical-chemical characteristics of mucoadhesive polymers must be also considered as factors influencing the mucoadhesive bonds. While it is not possible to modify the mucosal features or it is possible to modify or inhibit only in part certain mucosal processes, the knowledge of polymer properties influencing mucoadhesive bonds allows to modify or to control these properties in developing increasingly effective mucoadhesive systems. The aims of this review are to discuss the several mechanisms and factors behind the phenomenon of mucoadhesion with particular reference to the features of the oral environment, oral mucosa, and polymeric compounds influencing mucoadhesion process. Finally, a brief mention to the main mucoadhesive dosage forms designed for oral transmucosal drug delivery is made.

摘要

口腔黏膜为应用剂型提供了一个有趣的部位,通过确保药物在口腔黏膜内/通过口腔黏膜释放,实现局部和全身作用的高药物生物利用度。然而,在设计口腔剂型时,必须考虑口腔黏膜的相对通透性以及与口腔液和机械应力相关的冲洗作用。由于只有当剂型长时间保持与吸收/应用的口腔部位接触,才能保证药物的持续释放,因此必须开发黏膜黏附剂型。黏膜黏附是一种复杂的现象,黏膜黏附结合由两个不同部分组成,即黏膜黏附聚合物和黏液基质。除了与口腔黏膜和口腔环境特征相关的因素外,黏膜黏附聚合物的物理化学特性也必须被视为影响黏膜黏附结合的因素。虽然无法改变黏膜特征,但可以部分改变或抑制某些黏膜过程,但是,了解影响黏膜黏附结合的聚合物特性,可以在开发越来越有效的黏膜黏附系统时对这些特性进行修改或控制。本文综述的目的是讨论黏膜黏附现象背后的几种机制和因素,特别参考口腔环境、口腔黏膜和影响黏膜黏附过程的聚合物化合物的特征。最后,简要提及了为口腔黏膜给药设计的主要黏膜黏附剂型。

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