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用于辅酶Q口服递送的聚乙二醇化茄尼醇

PEGylated Solanesol for Oral Delivery of Coenzyme Q.

作者信息

Qin Benkai, Liu Lei, Pan Yangyang, Zhu Yingchun, Wu Xiaohe, Song Shiyong, Han Guang

机构信息

Institute of Pharmacy, Pharmacy College of Henan University , Jinming, Kaifeng, Henan 475001, China.

出版信息

J Agric Food Chem. 2017 Apr 26;65(16):3360-3367. doi: 10.1021/acs.jafc.7b00165. Epub 2017 Apr 18.

Abstract

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.

摘要

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。

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