Lee Mi-Kyung
Department of Pharmaceutical Sciences, Woosuk University, Jeonbuk 55338, Korea.
Pharmaceutics. 2020 Mar 13;12(3):264. doi: 10.3390/pharmaceutics12030264.
It has been known that a considerable number of drugs in clinical use or under development are water-insoluble drugs with poor bioavailability (BA). The liposomal delivery system has drawn attention as one of the noteworthy approaches to increase dissolution and subsequently absorption in the gastrointestinal (GI) tract because of its biocompatibility and ability to encapsulate hydrophobic molecules in the lipid domain. However, there have been several drawbacks, such as structural instability in the GI tract and poor permeability across intestinal epithelia because of its relatively large size. In addition, there have been no liposomal formulations approved for oral use to date, despite the success of parenteral liposomes. Nevertheless, liposomal oral delivery has resurged with the rapid increase of published studies in the last decade. However, it is discouraging that most of this research has been in vitro studies only and there have not been many water-insoluble drugs with in vivo data. The present review focused on the in vivo evidence for the improved BA of water-insoluble drugs using liposomes to resolve doubts raised concerning liposomal oral delivery and attempted to provide insight by highlighting the approaches used for in vivo achievements.
众所周知，许多临床使用或正在研发的药物都是生物利用度（BA）较差的水不溶性药物。脂质体递送系统因其生物相容性以及在脂质域中封装疏水分子的能力，作为一种提高胃肠道（GI）中药物溶解并随后促进吸收的值得关注的方法而受到关注。然而，它存在一些缺点，例如在胃肠道中结构不稳定，并且由于其相对较大的尺寸，肠道上皮的通透性较差。此外，尽管肠胃外脂质体取得了成功，但迄今为止尚无批准用于口服的脂质体制剂。尽管如此，在过去十年中，随着已发表研究的迅速增加，脂质体口服递送又重新兴起。然而，令人沮丧的是，大多数此类研究仅为体外研究，并且没有多少水不溶性药物有体内数据。本综述聚焦于使用脂质体提高水不溶性药物生物利用度的体内证据，以解决有关脂质体口服递送的疑问，并试图通过强调用于体内研究成果的方法来提供见解。
