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当前用于口服药物递送的基于脂质的纳米载体方法。

Current approaches in lipid-based nanocarriers for oral drug delivery.

机构信息

Faculty of Pharmacy, Cellular Neurobiology and Molecular Chemistry of the Central Nervous System Group, 02008, Albacete, Spain.

Regional Centre of Biomedical Research (CRIB), University of Castilla-La Mancha (UCLM), 02008, Albacete, Spain.

出版信息

Drug Deliv Transl Res. 2021 Apr;11(2):471-497. doi: 10.1007/s13346-021-00908-7. Epub 2021 Feb 2.

Abstract

Lipid-based nanocarriers have gained much interest as carriers of drugs with poor oral bioavailability because of their remarkable advantages like low toxicity, affordable scale-up manufacture, strong biocompatibility or high drug loading efficiency. The potential of these nanocarriers lies in their ability to improve the gastrointestinal stability, solubility and permeability of their cargo drugs. However, achieving efficient oral drug delivery through lipid-based nanocarriers is a challenging task, since they encounter multiple physicochemical barriers along the gastrointestinal tract, e.g. the gastric acidic content, the intestinal mucus layer or the enzymatic degradation, that they must surmount to reach their target. These limitations may be turned into opportunities through a rational design of lipid-based nanocarriers. For that purpose, this review focuses on the main challenges of the oral route indicating the strategies undertaken for lipid-based nanocarriers in order to overcome them. Understanding their shortcomings and identifying their strengths will determine the future clinical success of lipid-based nanocarriers.

摘要

脂质纳米载体因其低毒性、可负担的规模化生产、强生物相容性或高载药效率等显著优势,已成为口服生物利用度差的药物的载体而备受关注。这些纳米载体的潜力在于它们能够提高货物药物的胃肠道稳定性、溶解度和渗透性。然而,通过脂质纳米载体实现有效的口服药物递送是一项具有挑战性的任务,因为它们在胃肠道中会遇到多种物理化学屏障,例如胃酸性内容物、肠粘液层或酶降解,它们必须克服这些屏障才能到达目标。通过合理设计脂质纳米载体,可以将这些限制转化为机会。为此,本综述重点介绍了口服途径的主要挑战,并指出了为克服这些挑战而采取的脂质纳米载体策略。了解其缺点和确定其优势将决定脂质纳米载体未来的临床成功。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/1760/7852471/3443e19b106f/13346_2021_908_Fig1_HTML.jpg

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