Huang Y, Donovan MD
The University of Iowa, College of Pharmacy, Iowa City, IA 52242, USA
Adv Drug Deliv Rev. 1998 Jan 5;29(1-2):147-155. doi: 10.1016/s0169-409x(97)00066-5.
One of the characteristics influencing the increased interest in the nasal cavity as a site for systemic drug delivery is the ability of large molecules to permeate through the nasal mucosa into the systemic circulation. Compilations of data regarding the absorption of large therapeutic agents, peptides and proteins in particular, along with more systematic studies using polymeric compounds have shown that for compounds larger than 1000 Da, bioavailability can be directly predicted from a knowledge of molecular weight. In general, the bioavailability of these large molecules ranges from 0.5 to 5%. Particulate uptake also occurs in the nasal mucosa, and particles up to approximately 1 µm have been shown to rapidly enter the bloodstream following intranasal administration. The unique barrier properties of this mucosal delivery site give it great promise as a route for the systemic administration of large molecules.
影响鼻腔作为全身给药部位兴趣增加的一个特征是大分子透过鼻黏膜进入体循环的能力。关于大型治疗剂，特别是肽和蛋白质吸收的数据汇编，以及使用聚合物化合物进行的更系统的研究表明，对于分子量大于1000 Da的化合物，生物利用度可根据分子量知识直接预测。一般来说，这些大分子的生物利用度在0.5%至5%之间。鼻腔黏膜也会发生微粒摄取，鼻内给药后，直径达约1 µm的微粒已被证明能迅速进入血液。这种黏膜给药部位独特的屏障特性使其作为大分子全身给药途径具有很大潜力。
