Ozsoy Yildiz, Gungor Sevgi, Cevher Erdal
Istanbul University, Faculty of Pharmacy, Department of Pharmaceutical Technology, 34116-Universite, Istanbul, Turkey.
Molecules. 2009 Sep 23;14(9):3754-79. doi: 10.3390/molecules14093754.
Nasal drug delivery may be used for either local or systemic effects. Low molecular weight drugs with are rapidly absorbed through nasal mucosa. The main reasons for this are the high permeability, fairly wide absorption area, porous and thin endothelial basement membrane of the nasal epithelium. Despite the many advantages of the nasal route, limitations such as the high molecular weight (HMW) of drugs may impede drug absorption through the nasal mucosa. Recent studies have focused particularly on the nasal application of HMW therapeutic agents such as peptide-protein drugs and vaccines intended for systemic effects. Due to their hydrophilic structure, the nasal bioavailability of peptide and protein drugs is normally less than 1%. Besides their weak mucosal membrane permeability and enzymatic degradation in nasal mucosa, these drugs are rapidly cleared from the nasal cavity after administration because of mucociliary clearance. There are many approaches for increasing the residence time of drug formulations in the nasal cavity resulting in enhanced drug absorption. In this review article, nasal route and transport mechanisms across the nasal mucosa will be briefly presented. In the second part, current studies regarding the nasal application of macromolecular drugs and vaccines with nano- and micro-particulate carrier systems will be summarised.
鼻腔给药可用于局部或全身效应。低分子量药物可通过鼻黏膜快速吸收。主要原因是鼻上皮具有高渗透性、相当宽的吸收面积、多孔且薄的内皮基底膜。尽管鼻腔给药途径有诸多优点，但药物的高分子量等限制因素可能会阻碍药物通过鼻黏膜吸收。最近的研究尤其关注用于全身效应的高分子量治疗剂如肽 - 蛋白质药物和疫苗的鼻腔应用。由于其亲水性结构，肽和蛋白质药物的鼻腔生物利用度通常低于1%。除了它们在鼻黏膜中的弱膜通透性和酶降解外，这些药物在给药后由于黏液纤毛清除作用而迅速从鼻腔清除。有许多方法可增加药物制剂在鼻腔中的停留时间，从而提高药物吸收。在这篇综述文章中，将简要介绍鼻腔给药途径和穿过鼻黏膜的转运机制。在第二部分，将总结目前关于使用纳米和微粒载体系统进行高分子量药物和疫苗鼻腔应用的研究。
