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使用 PFG-NMR 测定的平移扩散系数预测小分子在有序纳米结构化脂质双连续立方相内的释放特性。

Predicting the release profile of small molecules from within the ordered nanostructured lipidic bicontinuous cubic phase using translational diffusion coefficients determined by PFG-NMR.

机构信息

School of Chemistry, University of Melbourne, VIC 3010, Australia and Bio21 Institute, University of Melbourne, VIC 3010, Australia.

Bio21 Institute, University of Melbourne, VIC 3010, Australia.

出版信息

Nanoscale. 2017 Feb 16;9(7):2471-2478. doi: 10.1039/c6nr07382d.

Abstract

The ordered nanostructured lipidic bicontinuous cubic phase has demonstrated potential as a drug release material, due to its ability to encapsulate a wide variety of compounds, which may undergo sustained, diffusion controlled release over time. Control of drug release has been shown to depend on the nanostructural parameters of the lipid mesophase. Herein, the diffusion and release of two amino acids, encapsulated within a range of different lipidic cubic mesophases are investigated. Pulsed-field gradient NMR was used to determine the diffusion coefficient of the encapsulated amino acid, which was found to be correlated with the nanoscale diameter of the water channels within the cubic mesophase. This information was used to predict the release profiles of encapsulated compounds from within the cubic mesophase, which was verified by directly measuring the release of each amino acid in vitro. Predicted release profiles tracked reasonably close to the measured release profiles, indicating that NMR determined diffusion measurements can be used to predict release profiles.

摘要

有序纳米结构脂质双连续立方相由于能够包裹各种化合物,有望成为一种药物释放材料,这些化合物可能会随着时间的推移持续进行扩散控制释放。研究表明,药物释放的控制取决于脂质中间相的纳米结构参数。在此,研究了两种氨基酸在一系列不同的脂质立方中间相中的扩散和释放。使用脉冲梯度 NMR 来确定包裹氨基酸的扩散系数,发现其与立方中间相中的水通道的纳米级直径相关。该信息用于预测立方中间相内包裹化合物的释放曲线,通过直接测量每种氨基酸在体外的释放来验证。预测的释放曲线与测量的释放曲线相当吻合,表明 NMR 确定的扩散测量可以用于预测释放曲线。

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