Karl Franzens University of Graz, Institute of Pharmaceutical Sciences/Pharmaceutical Technology, Graz 8010, Austria.
Small. 2013 Feb 11;9(3):457-66. doi: 10.1002/smll.201201789. Epub 2012 Oct 30.
Drugs can be absorbed well in the oral cavity, which eliminates problems related to intestinal and hepatic first-pass metabolism. Although it is well-established that nanoparticles are small enough to penetrate/permeate epithelial barriers, there is no clear understanding of how they interact with the buccal mucosa. This work provides useful information regarding particle properties with regard to mucosal uptake and can be used for the rational design of nanocarriers. In the buccal mucosa, the uptake of neutral polystyrene nanoparticles (PP) is size-dependent. Compared to 25 and 50 nm particles, 200 nm PP particles penetrate into deeper regions of the mucosa. This is attributed to the structure of the buccal mucosa, i.e., mucus layer and microplicae. The particles permeate the mucus layer and deposit in ridge-like folds of superficial buccal cells. Thus, the effects of thermodynamic driving forces and/or interparticle electrostatic repulsion are enhanced and cellular uptake might be reduced for smaller particle sizes.
药物在口腔中能被很好地吸收，这解决了与肠内和肝内首过代谢相关的问题。虽然已经证实纳米颗粒足够小，可以穿透/渗透上皮屏障，但对于它们与口腔黏膜的相互作用还没有明确的认识。这项工作为黏膜摄取方面的颗粒性质提供了有用的信息，可用于合理设计纳米载体。在口腔黏膜中，中性聚苯乙烯纳米颗粒（PP）的摄取具有尺寸依赖性。与 25nm 和 50nm 颗粒相比，200nm 的 PP 颗粒穿透到黏膜的更深区域。这归因于口腔黏膜的结构，即黏液层和微皱褶。这些颗粒穿透黏液层并沉积在浅层口腔细胞的脊状褶皱中。因此，对于较小的颗粒尺寸，热力学驱动力和/或颗粒间静电排斥的作用增强，细胞摄取可能会减少。
