Bosch Antonio M, Assenza Salvatore
Departamento de Física Teórica de la Materia Condensada, Universidad Autónoma de Madrid, 28049 Madrid, Spain.
Condensed Matter Physics Center (IFIMAC), Universidad Autónoma de Madrid, 28049 Madrid, Spain.
Pharmaceutics. 2023 Feb 8;15(2):573. doi: 10.3390/pharmaceutics15020573.
Lipid mesophases are being intensively studied as potential candidates for drug-delivery purposes. Extensive experimental characterization has unveiled a wide palette of release features depending on the nature of the host lipids and of the guest molecule, as well as on the environmental conditions. However, only a few simulation works have addressed the matter, which hampers a solid rationalization of the richness of outcomes observed in experiments. Particularly, to date, there are no theoretical works addressing the impact of hydropathy on the transport of a molecule within lipid mesophases, despite the significant fraction of hydrophobic molecules among currently-available drugs. Similarly, the high heterogeneity of water mobility in the nanoscopic channels within lipid mesophases has also been neglected. To fill this gap, we introduce here a minimal model to account for these features in a lamellar geometry, and systematically study the role played by hydropathy and water-mobility heterogeneity by Brownian-dynamics simulations. We unveil a fine interplay between the presence of free-energy barriers, the affinity of the drug for the lipids, and the reduced mobility of water in determining the net molecular transport. More in general, our work is an instance of how multiscale simulations can be fruitfully employed to assist experiments in release systems based on lipid mesophases.
脂质中间相作为药物递送目的的潜在候选物正在被深入研究。广泛的实验表征揭示了一系列取决于主体脂质和客体分子的性质以及环境条件的释放特性。然而,只有少数模拟工作涉及这个问题,这妨碍了对实验中观察到的丰富结果进行坚实的合理化解释。特别是,迄今为止,尽管目前可用的药物中有很大一部分是疏水分子,但尚无理论工作探讨亲水性对脂质中间相内分子运输的影响。同样,脂质中间相纳米通道内水流动性的高度异质性也被忽视了。为了填补这一空白,我们在此引入一个最小模型来解释层状几何结构中的这些特征,并通过布朗动力学模拟系统地研究亲水性和水流动性异质性所起的作用。我们揭示了自由能垒的存在、药物对脂质的亲和力以及水流动性降低在决定分子净运输方面的微妙相互作用。更一般地说,我们的工作是一个实例,展示了多尺度模拟如何能够有效地用于辅助基于脂质中间相的释放系统的实验。