Department of Functional Molecular Chemistry, Kobe Pharmaceutical University, 4-19-1 Motoyamakitamachi, Higashinada-ku, Kobe 658-8558, Hyogo, Japan.
Int J Pharm. 2010 Jun 30;393(1-2):104-11. doi: 10.1016/j.ijpharm.2010.04.013. Epub 2010 Apr 18.
The encapsulation of mononucleotides and DNA into Mg-Al layered double hydroxide (LDH, also known as hydrotalcite) by intercalation reaction, and release profile of mononucleotides and DNA was examined. Screening of the intercalation conditions (mononucleotide concentration, reaction temperature, reaction time, and pH) was carried out in order to determine precisely the optimal conditions. Intercalation of all examined mononucleotides and DNA into the chloride form of LDH was found to be possible using the ion-exchange method. The amount of mononucleotide taken up was 0.6-1.5 mmol per 1 g LDH. Intercalation compounds were examined using XRD and solid-state NMR. The interlayer distance of 5'-mononucleotide-intercalated LDH was found to be 14.0-15.3A, while that of 3'-mononucleotide-intercalated LDH was 17.4-17.7A. Intercalation of double-helix DNA of less than 500 base pairs was verified, with an uptake of 1.8 mmol per 1 g LDH (based on mononucleotide units). The intercalation mechanism and release profile in aqueous K(2)CO(3) solution were also investigated. Complete release of the nucleotides was found to take place. The encapsulation makes possible to protect mononucleotides and DNA, and promise the carrier of them to gene.
通过插层反应将单核苷酸和 DNA 包封到 Mg-Al 层状双氢氧化物（LDH，也称为水滑石）中，并检查了单核苷酸和 DNA 的释放情况。为了精确确定最佳条件，对插层条件（单核苷酸浓度、反应温度、反应时间和 pH）进行了筛选。使用离子交换法发现所有检查的单核苷酸和 DNA 都可以插入 LDH 的氯化物形式中。每个 LDH 吸收的单核苷酸量为 0.6-1.5mmol。使用 XRD 和固态 NMR 检查了插层化合物。发现 5'-单核苷酸插层 LDH 的层间距为 14.0-15.3Å，而 3'-单核苷酸插层 LDH 的层间距为 17.4-17.7Å。证实了小于 500 个碱基对的双链 DNA 的插入，每个 LDH 吸收 1.8mmol（基于单核苷酸单位）。还研究了在水性 K(2)CO(3)溶液中的插层机制和释放情况。发现核苷酸完全释放。封装使得保护单核苷酸和 DNA 成为可能，并为它们的基因载体提供了承诺。
