Qin Benkai, Liu Lei, Pan Yangyang, Zhu Yingchun, Wu Xiaohe, Song Shiyong, Han Guang
Institute of Pharmacy, Pharmacy College of Henan University , Jinming, Kaifeng, Henan 475001, China.
J Agric Food Chem. 2017 Apr 26;65(16):3360-3367. doi: 10.1021/acs.jafc.7b00165. Epub 2017 Apr 18.
Coenzyme Q (CoQ) is widely used in preventive or curative treatment of cardiovascular diseases. However, CoQ exhibits an extremely low solubility in aqueous medium as well as a poor oral bioavailability. Therefore, solanesyl poly(ethylene glycol) succinate (SPGS) and CoQ were formulated as CoQ-SPGS micelles with a high content of CoQ to improve the bioavailability of CoQ in rat. Findings indicate that, in the CoQ-SPGS micelles, SPGS is self-assembled into stable nanosized micelles with a CoQ loading capacity of more than 39%. The CoQ-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 CoQ, there was three-fold enhancement of oral bioavailability for CoQ-loaded SPGS micelles depending on varying molecular weight of SPGS. In the encapsulation of CoQ by SPGS micelles, the self-assembled nanocarriers with strong muco-adhesive properties lead to increases in the solubility and oral absorption of lipophilic CoQ nanoparticles.
辅酶Q(CoQ)被广泛用于心血管疾病的预防或治疗。然而,CoQ在水性介质中的溶解度极低,口服生物利用度也很差。因此,将茄尼基聚(乙二醇)琥珀酸酯(SPGS)和CoQ制成CoQ含量高的CoQ-SPGS胶束,以提高CoQ在大鼠体内的生物利用度。研究结果表明,在CoQ-SPGS胶束中,SPGS自组装成稳定的纳米级胶束,CoQ负载量超过39%。CoQ-SPGS胶束在模拟阳光下具有增强的光稳定性。体内实验表明,与CoQ粗悬浮液相比,根据SPGS分子量的不同,负载CoQ的SPGS胶束的口服生物利用度提高了三倍。在SPGS胶束包封CoQ的过程中,具有强粘膜粘附特性的自组装纳米载体导致亲脂性CoQ纳米颗粒的溶解度和口服吸收增加。