a Department of Pharmaceutical Technology , Institute of Pharmacy, University of Innsbruck , Innsbruck , Austria.
b Department of Pharmaceutical Nanotechnology, Faculty of Pharmacy , Tehran University of Medical Sciences , Tehran , Iran.
Expert Opin Drug Deliv. 2018 Oct;15(10):1007-1019. doi: 10.1080/17425247.2018.1517741. Epub 2018 Sep 7.
Mucosal drug delivery is an attractive route of administration, particularly in overcoming deficits of conventional dosage forms including high first-pass metabolism and poor bioavailability. Fast drainage from the target mucosa, however, represents a major limitation as it prevents sufficient drug absorption. In order to address these problems, mucoadhesive in situ gelling drug delivery systems have been investigated as they facilitate easy application in combination with a longer residence time at the administration site resulting in more desirable therapeutic effects.
The present review evaluates the importance of the combination of mucoadhesive and in situ gelling polymers along with mechanisms of in situ gelation and mucoadhesion. In addition, an overview about recent applications in mucosal drug delivery is provided.
In situ gelling and mucoadhesive polymers proved to be essential excipients in order to prolong the mucosal residence time of drug delivery systems. Due to this prolonged residence time both local and systemic therapeutic efficacy of numerous drugs can be substantially improved. Depending on the site of administration and the incorporated drug, combinations of different polymers with in situ gelling and mucoadhesive properties are needed to keep the delivery system as long as feasible at the target site.
黏膜给药剂型是一种有吸引力的给药途径,特别是在克服传统剂型的缺陷方面,包括高首过代谢和生物利用度差。然而,快速从目标黏膜排出是一个主要的限制因素,因为它阻止了足够的药物吸收。为了解决这些问题,人们研究了具有黏膜黏附性的原位凝胶给药系统,因为它们便于与更长的在给药部位的停留时间相结合使用,从而产生更理想的治疗效果。
本综述评估了将黏膜黏附性和原位凝胶聚合物结合使用的重要性,以及原位凝胶化和黏膜黏附的机制。此外,还提供了黏膜药物输送中最近应用的概述。
原位凝胶和黏膜黏附性聚合物已被证明是延长药物传递系统黏膜停留时间的重要赋形剂。由于这种延长的停留时间,可以大大提高许多药物的局部和全身治疗效果。根据给药部位和所包含的药物,需要将具有原位凝胶化和黏膜黏附性的不同聚合物组合使用,以使输送系统在目标部位尽可能长时间地保持。