Center for Nanomedicine at the Wilmer Eye Institute, Johns Hopkins University School of Medicine, Baltimore, MD 21231, USA.
Adv Drug Deliv Rev. 2012 May 1;64(6):557-70. doi: 10.1016/j.addr.2011.12.009. Epub 2011 Dec 24.
Oral delivery is the most common method for drug administration. However, poor solubility, stability, and bioavailability of many drugs make achieving therapeutic levels via the gastrointestinal (GI) tract challenging. Drug delivery must overcome numerous hurdles, including the acidic gastric environment and the continuous secretion of mucus that protects the GI tract. Nanoparticle drug carriers that can shield drugs from degradation and deliver them to intended sites within the GI tract may enable more efficient and sustained drug delivery. However, the rapid secretion and shedding of GI tract mucus can significantly limit the effectiveness of nanoparticle drug delivery systems. Many types of nanoparticles are efficiently trapped in and rapidly removed by mucus, making controlled release in the GI tract difficult. This review addresses the protective barrier properties of mucus secretions, how mucus affects the fate of orally administered nanoparticles, and recent developments in nanoparticles engineered to penetrate the mucus barrier.
口服是最常见的给药方式。然而,许多药物的溶解度、稳定性和生物利用度较差,使得通过胃肠道(GI)道达到治疗水平具有挑战性。药物输送必须克服许多障碍,包括酸性胃环境和不断分泌的粘液,以保护胃肠道。纳米药物载体可以保护药物免受降解,并将其递送到胃肠道内的预定部位,从而实现更有效的和持续的药物输送。然而,胃肠道粘液的快速分泌和脱落会显著限制纳米药物输送系统的有效性。许多类型的纳米颗粒会被粘液有效地捕获并迅速去除,这使得在胃肠道中进行控制释放变得困难。本文综述了粘液分泌的保护屏障特性、粘液如何影响口服给予的纳米颗粒的命运,以及为穿透粘液屏障而设计的纳米颗粒的最新进展。