In vitro–in vivo study of CoQ10-loaded lipid nanoparticles in comparison with nanocrystals

The present work described the effect of CoQ10 dissolution characteristics in nanocrystals and lipid nanoparticles (LNs) on its oral absorption in rats. Nanocrystals and LNs were prepared by melt-high pressure homogenization and sucrose monolaurate was used as a stabilizer in all formulations. Witepsol®W35 and medium-chain triglycerides (MCT) were selected as lipid additives to form LNCoQ10+W35 and LNCoQ10+MCT, respectively. From the results obtained, the particle size of CoQ10 nanocrystals was 285 nm, while it was reduced to 150 nm by mixture with an equal amount of lipid additives due to their lower melting points. In vitro dissolution results indicated that the drug release from two LNs was delayed compared with that from nanocrystals, and LNCoQ10+W35 exhibited the highest drug release over 4 h. Finally, in vivo evaluation demonstrated that the oral absorption of CoQ10 was markedly increased by using nanocrystals and LNs compared with a coarse suspension. A good relationship was found between the in vitro dissolution and in vivo evaluation. The enhanced oral absorption of CoQ10 by nanocrystals and LNs was due to improved dissolution. In conclusion, Witepsol®W35 was shown to be a better lipid additive for the preparation of LNs to increase the oral absorption of CoQ10.

The present work described the effect of CoQ10 dissolution characteristics in nanocrystals and lipid nanoparticles (LNs) on its oral absorption in rats. Nanocrystals and LNs were prepared by melt-high pressure homogenization and sucrose monolaurate was used as a stabilizer in all formulations. Witepsol®W35 and medium-chain triglycerides (MCT) were selected as lipid additives to form LNCoQ10+W35 and LNCoQ10+MCT, respectively. The results obtained demonstrated that the enhanced oral absorption of CoQ10 by nanocrystals and LNs was due to improved dissolution, and Witepsol®W35 was shown to be a better lipid additive for the preparation of LNs to increase the oral absorption of CoQ10.Figure optionsDownload as PowerPoint slide