University of Navarra, School of Pharmacy, Department of Pharmaceutics and Pharmaceutical Technology, Pamplona, Spain.
Expert Opin Drug Deliv. 2011 Jun;8(6):721-34. doi: 10.1517/17425247.2011.572069. Epub 2011 Apr 4.
The oral administration of drugs belonging to Class IV of the Biopharmaceutical Classification System (BCS) represents a major challenge. These drugs display poor aqueous solubility and specific permeability characteristics. Most of these compounds are substrates of the P-glycoprotein and/or the cytochrome P450. Among other types of drug, various anti-cancer drugs also suffer from these drawbacks (i.e., paclitaxel), which limits the possibilities for developing oral treatments.
This review discusses the factors that influence the bioavailability of drugs when administered by the oral route, as well as the capabilities of cyclodextrins when associated with nanoparticles. In particular, evidence is given regarding the synergistic effect between cyclodextrins and bioadhesive nanoparticles, on the oral delivery of pharmaceuticals.
This article aims to provide an overview of the multiple gains in incorporating cyclodextrins in poly(anhydride) nanoparticles, including improvement of their bioadhesive capability, the loading of lipophilic drugs and the effect on efflux membrane proteins and cytochrome P450. The combination between bioadhesive nanoparticles and P-gp inhibitors without pharmacological activity (i.e., cyclodextrins) may be useful to promote the oral bioavailability of drugs ascribed to Class IV of the BCS.
属于生物药剂分类系统（BCS）IV 类的药物经口服给药具有很大的挑战性。这些药物表现出较差的水溶性和特定的渗透性特征。这些化合物大多是 P-糖蛋白和/或细胞色素 P450 的底物。除了其他类型的药物外，各种抗癌药物也存在这些缺陷（如紫杉醇），这限制了口服治疗的可能性。
本文讨论了影响口服给药时药物生物利用度的因素，以及环糊精与纳米粒子结合时的能力。特别是，本文提供了关于环糊精和生物黏附纳米粒子在药物口服传递方面协同作用的证据。
本文旨在概述将环糊精纳入聚（酸酐）纳米粒子中所带来的多种益处，包括改善其生物黏附能力、载运亲脂性药物以及对流出膜蛋白和细胞色素 P450 的影响。具有生物黏附性的纳米粒子与无药理活性的 P-糖蛋白抑制剂（即环糊精）的结合可能有助于提高属于 BCS 分类 IV 类的药物的口服生物利用度。
