Use of Solid Lipid Nanoparticles to Improve the Oral Bioavailability of Poorly Water-Soluble Drugs

Abstract

The low bioavailability of orally administered drugs because of their poor water solubility remains a challenge towards the development of promising drug products. Approximately 40% of drugs with regulatory approval and nearly 90% of drugs in the discovery pipeline are poorly water-soluble. Among other drug delivery systems comprising lipid excipients, the use of solid lipid nanoparticles (SLNs) has emerged for improving the oral bioavailability of loaded poorly water-soluble drugs. This chapter focuses on the following topics. First, it presents the key roles of SLNs as delivery systems, compared to the other drug delivery approaches. Second, the chapter reviews the criteria for selecting suitable lipid excipients and fabrication techniques of SLNs based on the characteristics of drugs and lipids. Third, upon the preparation of drug-loaded SLNs, this chapter presents methods employed for characterizations of this delivery system and discusses in detail the underlying mechanisms by which SLNs facilitate the bioavailability enhancement of poorly water-soluble drugs administered orally. Finally, this chapter presents some of the recent progress of SLNs and their applications towards pharmaceutical development.