PEGylated Solanesol for Oral Delivery of Coenzyme Q10

Abstract

Coenzyme Q₁₀ (CoQ₁₀) is widely used in preventive or curative treatment of cardiovascular diseases. However, CoQ₁₀ exhibits an extremely low solubility in aqueous medium as well as a poor oral bioavailability. Therefore, solanesyl poly(ethylene glycol) succinate (SPGS) and CoQ₁₀ were formulated as CoQ₁₀-SPGS micelles with a high content of CoQ₁₀ to improve the bioavailability of CoQ₁₀ in rat. Findings indicate that, in the CoQ₁₀-SPGS micelles, SPGS is self-assembled into stable nanosized micelles with a CoQ₁₀ loading capacity of more than 39%. The CoQ₁₀-SPGS micelles exhibit an enhanced photostability upon exposure to simulated sunlight. In vivo experiments demonstrate that, as compared to that of the coarse suspensions of CoQ₁₀, there was three-fold enhancement of oral bioavailability for CoQ₁₀-loaded SPGS micelles depending on varying molecular weight of SPGS. In the encapsulation of CoQ₁₀ by SPGS micelles, the self-assembled nanocarriers with strong muco-adhesive properties lead to increases in the solubility and oral absorption of lipophilic CoQ₁₀ nanoparticles.

Keywords: bioavailability; coenzyme Q10; micelles; photostability; solanesol; water dispersibility.