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粘膜粘附的基本原理及潜在机制。

The basics and underlying mechanisms of mucoadhesion.

作者信息

Smart John D

机构信息

School of Pharmacy and Biomolecular Sciences, University of Brighton, Lewes Road, Brighton, UK.

出版信息

Adv Drug Deliv Rev. 2005 Nov 3;57(11):1556-68. doi: 10.1016/j.addr.2005.07.001. Epub 2005 Sep 29.

Abstract

Mucoadhesion is where two surfaces, one of which is a mucous membrane, adhere to each other. This has been of interest in the pharmaceutical sciences in order to enhance localised drug delivery, or to deliver 'difficult' molecules (proteins and oligonucleotides) into the systemic circulation. Mucoadhesive materials are hydrophilic macromolecules containing numerous hydrogen bond forming groups, the carbomers and chitosans being two well-known examples. The mechanism by which mucoadhesion takes place has been said to have two stages, the contact (wetting) stage followed by the consolidation stage (the establishment of the adhesive interactions). The relative importance of each stage will depend on the individual application. For example, adsorption is a key stage if the dosage form cannot be applied directly to the mucosa of interest, while consolidation is important if the formulation is exposed to significant dislodging stresses. Adhesive joint failure will inevitably occur as a result of overhydration of a dosage form, or as a result of epithelia or mucus turnover. New mucoadhesive materials with optimal adhesive properties are now being developed, and these should enhance the potential applications of this technology.

摘要

粘膜粘附是指两个表面(其中一个是粘膜)相互粘附的现象。在制药科学领域,这一现象备受关注,因为它有助于增强局部药物递送,或者将“难处理”的分子(蛋白质和寡核苷酸)输送到体循环中。粘膜粘附材料是含有大量形成氢键基团的亲水性大分子,卡波姆和壳聚糖就是两个著名的例子。据说粘膜粘附发生的机制有两个阶段,即接触(湿润)阶段,随后是巩固阶段(建立粘附相互作用)。每个阶段的相对重要性将取决于具体应用。例如,如果剂型不能直接应用于目标粘膜,吸附就是一个关键阶段;而如果制剂受到显著的位移应力,巩固则很重要。由于剂型过度水化,或者由于上皮细胞或粘液更新,粘附连接失效将不可避免地发生。目前正在开发具有最佳粘附性能的新型粘膜粘附材料,这些材料应能增强该技术的潜在应用。

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