Department of Bioengineering, University of Illinois, Chicago, Illinois 60607-7052.
Advanced Materials and Nanobiotechnology Laboratory, Department of Biomedical and Pharmaceutical Sciences, Center for Targeted Drug Delivery, Chapman University, Irvine, California 92618-1908.
Biointerphases. 2019 May 20;14(3):031001. doi: 10.1116/1.5090396.
One of the main goals of materials science in the 21st century is the development of materials with rationally designed properties as substitutes for traditional pharmacotherapies. At the same time, there is a lack of understanding of the exact material properties that induce therapeutic effects in biological systems, which limits their rational optimization for the related medical applications. This study sets the foundation for a general approach for elucidating nanoparticle properties as determinants of antibacterial activity, with a particular focus on calcium phosphate nanoparticles. To that end, nine physicochemical effects were studied and a number of them were refuted, thus putting an end to frequently erred hypotheses in the literature. Rather than having one key particle property responsible for eliciting the antibacterial effect, a complex synergy of factors is shown to be at work, including (a) nanoscopic size; (b) elevated intracellular free calcium levels due to nanoparticle solubility; (c) diffusivity and favorable electrostatic properties of the nanoparticle surface, primarily low net charge and high charge density; and (d) the dynamics of perpetual exchange of ultrafine clusters across the particle/solution interface. On the positive side, this multifaceted mechanism is less prone to induce bacterial resistance to the therapy and can be a gateway to the sphere of personalized medicine. On a more problematic side, it implies a less intense effect compared to single-target molecular therapies and a difficulty of elucidating the exact mechanisms of action, while also making the rational design of theirs for this type of medical application a challenge.
二十一世纪材料科学的主要目标之一是开发具有合理设计性能的材料,以替代传统的药物疗法。同时,人们对确切的材料特性缺乏了解,这些特性会在生物系统中诱导治疗效果,从而限制了它们在相关医疗应用中的合理优化。本研究为阐明纳米颗粒特性作为抗菌活性决定因素的一般方法奠定了基础,特别关注磷酸钙纳米颗粒。为此,研究了九种物理化学效应,并驳斥了其中的一些效应,从而结束了文献中经常出现的错误假设。引起抗菌作用的并非是一个关键的颗粒特性,而是多种因素的协同作用,包括:(a) 纳米级尺寸;(b) 由于纳米颗粒的溶解度而导致细胞内游离钙水平升高;(c) 纳米颗粒表面的扩散性和有利的静电特性,主要是低净电荷和高电荷密度;以及 (d) 超细颗粒在颗粒/溶液界面上不断交换的动力学。从积极的方面来看,这种多方面的机制不太可能引起细菌对治疗的耐药性,并且可以成为个性化药物领域的一个切入点。更成问题的是,与单靶点分子疗法相比,它的效果较弱,阐明确切的作用机制也具有一定难度,同时也使得针对此类医疗应用进行合理设计具有一定挑战性。