Oil-enriched, ultra-small nanostructured lipid carriers (usNLC): a novel delivery system based on flip-flop structure

Abstract

For the development of ultra-small NLC (usNLC) the determination of the required HLB (hydrophilic lipophilic balance) was found to be a suitable method, i.e., usNLC with a size below 50 nm were obtained by this method. Loading with 5% (w/w) coenzyme Q10 (Q10) led to usNLC with a size of about 85 nm. In comparison to classical NLC with a size of 230 nm and a nanoemulsion with similar size, the Q10 loaded usNLC show a higher release, a higher antioxidant capacity, and a better skin penetration for Q10. The reason for this is a flip-flop core-shell structure of the lipid matrix, i.e., the oil with dissolved active is surrounding the solid lipid based core. As the flip-flop structure was probably achieved by admixing high contents of liquid lipid, oil enriched usNLC might represent a novel and promising carrier system for the improved delivery of lipophilic actives.

Keywords: Coenzyme Q10; Flip–flop core–shell structure; Lipid nanoparticles; Nanostructured lipid carriers; Required HLB; Ultra-small NLC.