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通过脂质纳米颗粒的胃肠道黏膜黏附提高难溶性药物的生物利用度。

Improved Bioavailability of Poorly Soluble Drugs through Gastrointestinal Muco-Adhesion of Lipid Nanoparticles.

作者信息

Tan Sui Ling Janet, Billa Nashiru

机构信息

Institut Kanser Negara, Putrajaya 62250, Malaysia.

College of Pharmacy, QU Health, Qatar University, Doha 2713, Qatar.

出版信息

Pharmaceutics. 2021 Oct 31;13(11):1817. doi: 10.3390/pharmaceutics13111817.

Abstract

Gastrointestinal absorption remains indispensable in the systemic delivery of most drugs, even though it presents several challenges that, paradoxically, may also provide opportunities that can be exploited to achieve maximal bioavailability. Drug delivery systems made from nanoparticle carriers and especially, lipid carriers, have the potential to traverse gastrointestinal barriers and deploy in the lymphatic pathway, which aptly, is free from first pass via the liver. Several poorly soluble drugs have presented improved systemic bioavailability when couriered in lipid nanoparticle carriers. In this review, we propose an additional frontier to enhancing the bioavailability of poorly soluble drugs when encapsulated in lipid nano-carriers by imparting muco-adhesion to the particles through application of appropriate polymeric coating to the lipid carrier. The combined effect of gastrointestinal muco-adhesion followed by lymphatic absorption is a promising approach to improving systemic bioavailability of poorly soluble drugs following oral administration. Evidence to the potential of this approach is backed-up by recent studies within the review.

摘要

尽管胃肠道吸收存在诸多挑战,但在大多数药物的全身给药中仍不可或缺,而这些挑战反而可能提供一些可被利用的机会,以实现最大生物利用度。由纳米颗粒载体尤其是脂质载体制成的药物递送系统,有潜力穿越胃肠道屏障并进入淋巴途径,而淋巴途径恰好可避免药物经肝脏的首过效应。当一些难溶性药物被包裹在脂质纳米颗粒载体中时,其全身生物利用度有所提高。在本综述中,我们提出了一个新的前沿领域,即通过在脂质载体上应用适当的聚合物涂层使颗粒具有粘膜粘附性,从而提高包裹在脂质纳米载体中的难溶性药物的生物利用度。胃肠道粘膜粘附随后淋巴吸收的联合效应,是提高口服难溶性药物全身生物利用度的一种有前景的方法。本综述中的近期研究支持了这种方法的潜力。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c324/8620210/0950d9916ec9/pharmaceutics-13-01817-g001.jpg

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