Laksitorini Marlyn, Prasasty Vivitri D, Kiptoo Paul K, Siahaan Teruna J
Department of Pharmaceutical Chemistry, The University of Kansas, 2095 Constant Avenue, Lawrence, KS 66047, USA.
Ther Deliv. 2014 Oct;5(10):1143-63. doi: 10.4155/tde.14.67.
One of the major hurdles in developing therapeutic agents is the difficulty in delivering drugs through the intestinal mucosa and blood-brain barriers (BBB). The goal here is to describe the general structures of the biological barriers and the strategies to enhance drug delivery across these barriers. Prodrug methods used to improve drug penetration via the transcellular pathway have been successfully developed, and some prodrugs have been used to treat patients. The use of transporters to improve absorption of some drugs (e.g., antiviral agents) has also been successful in treating patients. Other methods, including blocking the efflux pumps to improve transcellular delivery, and modulation of cell-cell adhesion in the intercellular junctions to improve paracellular delivery across biological barriers, are still in the investigational stage.
开发治疗药物的主要障碍之一是药物难以透过肠黏膜和血脑屏障（BBB）。本文旨在描述这些生物屏障的一般结构以及增强药物跨这些屏障递送的策略。已成功开发出通过跨细胞途径提高药物渗透性的前药方法，并且一些前药已用于治疗患者。利用转运体改善某些药物（如抗病毒药物）的吸收在治疗患者方面也取得了成功。其他方法，包括阻断外排泵以改善跨细胞递送，以及调节细胞间连接中的细胞间粘附以改善药物跨生物屏障的细胞旁递送，仍处于研究阶段。
