Delhi Pharmaceutical Sciences and Research University (DPSRU), Mehrauli-Badarpur Road, Pusp Vihar Sector 3, New Delhi, 110017, India.
AAPS PharmSciTech. 2019 Feb 25;20(3):121. doi: 10.1208/s12249-019-1337-8.
Lipid-based drug delivery systems has become a popular choice for oral delivery of lipophilic drugs with dissolution rate limited oral absorption. Lipids are known to enhance oral bioavailability of poorly water-soluble drugs in multiple ways like facilitating dissolution as micellar solution, enhancing the lymphatic uptake and acting as inhibitors of efflux transporters. Lipid nanoparticles are matrix type lipid-based carrier systems which can effectively encapsulate both lipophilic and hydrophilic drugs. Lipid nanoparticles namely solid lipid nanoparticles (SLN) and nanostructured lipid carriers (NLC) are versatile drug delivery system and can be used for multiple routes of delivery like parenteral, topical, ocular, transdermal, and oral. Lipid nanoparticles are particularly attractive vehicles for peroral delivery of drugs with oral bioavailability problems as they are composed of lipid excipients which are cheap, easily available, and non-toxic; manufacturing technique is simple and readily scalable for large-scale production; the formulations provide controlled release of active components and have no stability issue. A large number of drugs have been incorporated into lipid nanoparticles with the objective of overcoming their poor oral bioavailability. This review tries to assess the potential of lipid nanoparticles for enhancing the oral bioavailability of drugs with permeability limited oral absorption such as drugs belonging to class IV of Biopharmaceutic Classification System (BCS) and protein and peptide drugs and also discusses the mechanism behind the bioavailability enhancement and safety issues related to such delivery systems.
脂质体给药系统已成为具有溶解速率限制口服吸收的亲脂性药物口服递送的热门选择。众所周知,脂质可以通过多种方式提高亲脂性药物的口服生物利用度,例如促进溶解为胶束溶液、增强淋巴摄取和作为外排转运体的抑制剂。脂质纳米粒是基质型脂质载体系统,可有效包封亲脂性和亲水性药物。脂质纳米粒,即固体脂质纳米粒 (SLN) 和纳米结构脂质载体 (NLC),是一种多功能的药物递送系统,可用于多种给药途径,如注射、局部、眼部、透皮和口服。由于脂质纳米粒由廉价、易得且无毒的脂质赋形剂组成,制造技术简单且易于大规模生产,制剂可控制活性成分的释放,且不存在稳定性问题,因此对于具有口服生物利用度问题的口服给药药物,脂质纳米粒特别具有吸引力。本文综述了脂质纳米粒在提高具有渗透性限制口服吸收的药物(如生物药剂学分类系统 (BCS) 分类 IV 类药物和蛋白和肽类药物)的口服生物利用度方面的潜力,并讨论了提高生物利用度的机制和与这些给药系统相关的安全性问题。