Potential of Lipid Nanoparticles (SLNs and NLCs) in Enhancing Oral Bioavailability of Drugs with Poor Intestinal Permeability.

Abstract

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.