Muranishi S
Kyoto College of Pharmacy, Japan.
Crit Rev Ther Drug Carrier Syst. 1990;7(1):1-33.
Many current therapeutic drugs, e.g., antibiotics and peptide drugs, are impermeable to outer tissue barriers. Drug delivery of impermeable drugs through such barriers is currently one of the major interests in pharmaceutical research. New classes of absorption enhancers provide rapid absorption in the gastrointestinal tract or skin, with no side effects. This review covers the history of enhancer research, an overview of a variety of absorption enhancers, the nature of enhancing action, and site specificity. The final section focuses on the mechanisms of enhancer action which transiently abolishes or reverses barrier resistance, from the viewpoints of the lipid bilayer barrier containing SH proteins, as well as transcellular/paracellular pathways. Fully understanding these mechanisms is of importance for therapeutic applications.
许多当前的治疗药物，如抗生素和肽类药物，无法穿透外部组织屏障。通过此类屏障递送这类无法穿透的药物是目前药物研究的主要关注点之一。新型吸收促进剂可在胃肠道或皮肤中实现快速吸收，且无副作用。本综述涵盖了吸收促进剂研究的历史、各类吸收促进剂的概述、增强作用的本质以及部位特异性。最后一部分从含有SH蛋白的脂质双分子层屏障以及跨细胞/细胞旁途径的角度，重点探讨了吸收促进剂作用的机制，这些机制可暂时消除或逆转屏障阻力。充分理解这些机制对于治疗应用至关重要。
