Ethypharm, 92213-Saint-Cloud Cedex, France.
Nanomedicine (Lond). 2010 Feb;5(2):287-306. doi: 10.2217/nnm.09.110.
Oral route is the most common route for the delivery of drugs because it is simple to implement and improves patient compliance and quality of life. However, oral absorption is limited by various physiological barriers and remains a scientific challenge. Nanometric-sized drug delivery systems are being extensively studied and provide promising potential for oral drug delivery. Many different technological solutions have been proposed to enhance the bioavailability or the targeting of drug after oral administration. To reach these goals, it is important to analyze the biopharmaceutical parameters to consider in order to alter the fate of nanocarriers after oral delivery. In the present review, the gastrointestinal barrier and physiological stress factors with regard to nanocarriers' performance or integrity issues are first described. Second, the different characteristics offered by the nanocarriers (size, surface composition and properties mediated by external factors such as ligands) and their effect on the optimal transport of drug into the bloodstream are discussed. Finally, the integrity issue is discussed in function of the expected role of the nanocarriers: bioavailability enhancement or pharmacological targeting.
口服途径是药物给药最常用的途径，因为它简单易行，可提高患者的顺应性和生活质量。然而，口服吸收受到各种生理屏障的限制，仍然是一个科学挑战。纳米级药物传递系统正在被广泛研究，并为口服药物传递提供了有前途的潜力。为了提高口服给药后药物的生物利用度或靶向性，已经提出了许多不同的技术解决方案。为了实现这些目标，分析改变口服给药后纳米载体命运时需要考虑的生物制药参数非常重要。在本综述中，首先描述了胃肠道屏障和与纳米载体性能或完整性问题有关的生理应激因素。其次，讨论了纳米载体的不同特性（大小、表面组成和性质，这些特性受配体等外部因素的调节）及其对药物最佳进入血流的影响。最后，根据纳米载体的预期作用讨论了完整性问题：生物利用度增强或药理学靶向。
