Faculty of Pharmaceutical Sciences, Sojo University, Kumamoto 860-0082, Japan.
Faculty of Pharmaceutical Sciences, Sojo University, Kumamoto 860-0082, Japan; DDS Research Institute, Sojo University, Kumamoto 860-0082, Japan.
J Pharm Sci. 2018 Jan;107(1):436-445. doi: 10.1016/j.xphs.2017.08.003. Epub 2017 Aug 18.
Liposomes are clinically used in drug delivery, but loading hydrophobic substances is limited to the hydrophobic space of a lipid membrane, despite the fact that it is favorable to encapsulate substances into the inner aqueous core of liposome, from a drug stability of view. We report herein on the preparation of a liposome with bovine serum albumin encapsulated (BSA-liposome). Using this system, it is possible to encapsulate hydrophobic drugs in the inner aqueous core of the liposome based on the hypothesis that the water solubility of hydrophobic drugs is increased when bound to albumin. The physicochemical properties of the prepared BSA-liposomes could be easily regulated and the loading of hydrophobic drugs in the inner aqueous core of the liposome was dramatically improved by virtue of the drug-binding properties of albumin. An in vivo safety and pharmacokinetic study showed that BSA-liposomes possess favorable properties as a drug carrier, including biocompatibility and a stealth effect. This new type of hydrophobic drug carrier, an albumin-liposome, has the potential for use in delivering numerous hydrophobic drugs that typically bind to albumin.
脂质体在药物传递中得到了临床应用，但将疏水性物质载入脂质体中受到脂质膜疏水区的限制，尽管从药物稳定性的角度来看，将物质包封在脂质体的内水核中是有利的。我们在此报告了一种包载牛血清白蛋白（BSA）的脂质体（BSA-脂质体）的制备。基于疏水药物与白蛋白结合后水溶性增加的假设，利用该系统可以将疏水性药物包封在脂质体的内水核中。通过白蛋白的药物结合特性，可以轻松调节所制备的 BSA-脂质体的理化性质，并显著提高疏水性药物在脂质体的内水核中的载药量。体内安全性和药代动力学研究表明，BSA-脂质体作为药物载体具有良好的特性，包括生物相容性和隐形效果。这种新型的疏水性药物载体，即白蛋白脂质体，有望用于传递许多通常与白蛋白结合的疏水性药物。
