Department of Pharmaceutical Technology, Institute of Pharmacy, University of Innsbruck, A-6020 Innsbruck, Austria.
Nanomedicine (Lond). 2017 Feb;12(3):255-269. doi: 10.2217/nnm-2016-0331. Epub 2017 Jan 17.
Pre-uptake metabolism within the GI tract is responsible for the poor oral bioavailability of numerous drugs. As nanocarriers function as a 'shield', protecting incorporated drugs from enzymatic attack, there is an increasing interest in utilizing them as a tool for overcoming drug degradation. Degradation of carriers resulting in the release of incorporated drugs, mucus permeation, enzyme inhibitory properties and their toxicity are crucial factors that must be taken into account when designing proper nanocarriers. The use of polymer- and lipid-based nanocarriers as protective vehicles are discussed within this review. Lipid-based carriers and novel mucopenetrating particles seem to have a great potential in avoiding metabolizing enzymes. Accordingly, nanocarriers are promising tools for improving the bioavailability of drugs, being sensitive to a pre-uptake metabolism.
胃肠道内的吸收前代谢会导致许多药物的口服生物利用度较差。由于纳米载体起到了“保护盾”的作用,可防止包裹的药物受到酶的攻击,因此人们越来越有兴趣将其用作克服药物降解的工具。载体的降解会导致包裹的药物释放、黏液渗透、酶抑制特性和毒性,这些都是在设计合适的纳米载体时必须考虑的关键因素。本文讨论了聚合物和脂质纳米载体作为保护载体的应用。基于脂质的载体和新型黏膜穿透颗粒似乎在避免代谢酶方面具有很大的潜力。因此,纳米载体是提高药物生物利用度的有前途的工具,对吸收前代谢敏感。