Shin Jae-Yoon, Shin Jae-Il, Kim Jun-Seob, Yang Yoo-Soo, Hwang Yunha, Yang Joo-Sung, Shin Dongwoo, Seo Jin-Ho, Jin Yong-Su, Park Yong-Cheol, Hwang Jae-Sung, Kweon Dae-Hyuk
School of Biotechnology and Bioengineering, Sungkyunkwan University, Suwon, Gyeongido 440-746, Republic of Korea.
Biochem Biophys Res Commun. 2009 Oct 16;388(2):217-21. doi: 10.1016/j.bbrc.2009.07.140. Epub 2009 Jul 30.
There are tremendous drug candidates that suffer from insolubility in water. In the present study, it is shown that Coenzyme Q10 (CoQ10), a model water-insoluble compound, can be nanoparticulated into a water-soluble form using apolipoprotein A-I (apoA-I). Similar to the way that apoA-I forms nascent discoidal high density lipoprotein (ndHDL) particles by bordering acyl chain tails of phospholipids, CoQ10 could be enclosed into the circle of a disk made of apoA-Is. The resulting nanostructure of CoQ10 and apoA-I was water-soluble with a size of approximately 12 nm in diameter and was physically more robust than liposome. We expect that the strategy suggested in this study can be exploited to assemble nano-sized, water-soluble structures of various water-insoluble drug candidates.
有大量的候选药物存在水不溶性问题。在本研究中,结果表明,辅酶Q10(CoQ10),一种典型的水不溶性化合物,可以利用载脂蛋白A-I(apoA-I)纳米化为水溶性形式。类似于apoA-I通过毗连磷脂的酰基链尾部形成新生盘状高密度脂蛋白(ndHDL)颗粒的方式,CoQ10可以被包裹在由apoA-I构成的盘状物的环内。所得的CoQ10和apoA-I的纳米结构是水溶性的,直径约为12纳米,并且在物理性质上比脂质体更稳定。我们期望本研究中提出的策略能够用于组装各种水不溶性候选药物的纳米级水溶性结构。