Department of Pharmaceutics and Drug Delivery, School of Pharmacy, University of Mississippi, MS 38677, USA.
Department of Pharmaceutical Sciences, School of Pharmacy, University of Texas at El Paso, El Paso, TX 79902, USA.
Nanoscale. 2024 Oct 10;16(39):18319-18338. doi: 10.1039/d4nr01487a.
In recent studies, lipid nanoparticles have attracted attention as drug delivery systems owing to their preeminent potential in achieving the desired bioavailability of biopharmaceutics (BCS) class II and class IV drugs. The current debate concerns the bioavailability of these poorly absorbed drugs with their simultaneous oral degradation. Lipid nanoparticles, including solid lipid nanoparticles (SLN) and nanostructured lipid carriers (NLC), are lipid-based carrier systems that can effectively encapsulate both lipophilic and hydrophilic drugs, offering versatile drug delivery systems. The unique properties of lipids (biodegradability and biocompatibility) and their transportation pathways enhance the biological availability of drugs. These particles can increase the gastrointestinal absorption and solubilization of minimally bioavailable drugs a selective lymphatic pathway. This review mainly focuses on providing a brief update on lipid nanoparticles (LNPs) that synergistically increase the bioavailability of limited permeable drugs and highlight the transversal mechanisms of LNPs across the gastrointestinal hurdles, transmembrane absorption, transport kinetics, and computational tools. Finally, the present hurdles and future perspectives of LNPs for oral drug delivery systems are discussed.
在最近的研究中，脂质纳米粒作为药物传递系统引起了人们的关注，因为它们在实现生物药剂学（BCS）II 类和 IV 类药物所需的理想生物利用度方面具有卓越的潜力。目前的争论涉及这些吸收不良的药物同时口服降解的生物利用度。脂质纳米粒，包括固体脂质纳米粒（SLN）和纳米结构脂质载体（NLC），是基于脂质的载体系统，能够有效地包封亲脂性和亲水性药物，提供多功能的药物传递系统。脂质的独特性质（生物降解性和生物相容性）及其运输途径提高了药物的生物利用度。这些颗粒可以通过选择性的淋巴途径增加最小生物利用度药物的胃肠道吸收和溶解。本文主要综述了协同提高有限渗透性药物生物利用度的脂质纳米粒（LNPs），并强调了 LNPs 穿越胃肠道障碍、跨膜吸收、转运动力学和计算工具的横向机制。最后，讨论了 LNPs 用于口服药物传递系统的当前障碍和未来展望。
