PEGylated Solanesol for Oral Delivery of Coenzyme Q10

• DOI: 10.1021/acs.jafc.7b00165
• Publication Date: 2017-04-18T18:49:51Z
• Authors: Benkai Qin; Lei Liu; Yangyang Pan; Yingchun Zhu; Xiaohe Wu; Shiyong Song; Guang Han
• Keywords: Drug Carriers; 0303 health sciences; Terpenes; Ubiquinone; Biological Availability; Polyethylene Glycols; Rats; 3. Good health; Rats, Sprague-Dawley; 03 medical and health sciences; Drug Delivery Systems; Solubility; Animals; Nanoparticles; Female; Micelles

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.