Mühlberg Eric, Burtscher Mira, Umstätter Florian, Fricker Gert, Mier Walter, Uhl Philipp
Department of Nuclear Medicine, Heidelberg University Hospital, Im Neuenheimer Feld 400, Heidelberg, 69120, Germany.
Department of Pharmaceutical Technology & Biopharmacy, Institute for Pharmacy & Molecular Biotechnology, Ruprecht-Karls University, Im Neuenheimer Feld 329, Heidelberg, 69120, Germany.
Nanomedicine (Lond). 2021 Aug;16(20):1813-1832. doi: 10.2217/nnm-2021-0177. Epub 2021 Jul 16.
The number of approved macromolecular drugs such as peptides, proteins and antibodies steadily increases. Since drugs with high molecular weight are commonly not suitable for oral delivery, research on carrier strategies enabling oral administration is of vital interest. In past decades, nanocarriers, in particular liposomes, have been exhaustively investigated as oral drug-delivery platform. Despite their successful application as parenteral delivery vehicles, liposomes have up to date not succeeded for oral administration. However, a plenitude of approaches aiming to increase the oral bioavailability of macromolecular drugs administered by liposomal formulations has been published. Here, we summarize the strategies published in the last 10 years (vaccine strategies excluded) with a main focus on strategies proven efficient in animal models.
诸如肽、蛋白质和抗体等已获批的大分子药物数量稳步增长。由于高分子量药物通常不适合口服给药,因此关于实现口服给药的载体策略的研究至关重要。在过去几十年中,纳米载体,尤其是脂质体,已作为口服给药平台进行了详尽研究。尽管脂质体作为肠胃外给药载体已成功应用,但迄今为止尚未成功用于口服给药。然而,已经发表了大量旨在提高脂质体制剂给药的大分子药物口服生物利用度的方法。在此,我们总结过去10年发表的策略(不包括疫苗策略),主要侧重于在动物模型中已证明有效的策略。