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基于片上光流控的单颗粒法用于快速筛选生物活性物质的微尺度平衡溶解度。

On-chip optofluidic single-particle method for rapid microscale equilibrium solubility screening of biologically active substances.

机构信息

Division of Pharmaceutical Chemistry and Technology, University of Helsinki, P.O. Box 56, FI-00014 Helsinki, Finland.

出版信息

Anal Chem. 2015;87(10):5041-5. doi: 10.1021/acs.analchem.5b01033. Epub 2015 Apr 30.

DOI:10.1021/acs.analchem.5b01033
PMID:25913110
Abstract

Solubility is the primary physicochemical property determining the absorption and bioavailability of substances. Here, we present an optofluidic single-particle technique for microscale equilibrium solubility determination, based on on-chip hydrodynamic particle trapping and optical particle size monitoring. The method combines the rapidity, universality, and substance sparing nature of physical analysis, with the accuracy traditionally associated with chemical analysis. Applying the diffusion layer theory, we determined the equilibrium solubility from individual pure substance microparticles of as little as 14 μg in initial mass, in a matter of seconds to minutes. The reduction in time and substance consumption, when compared to the golden standard method, is above 2 orders of magnitude. With a simultaneous improvement above 3-fold in accuracy of the solubility data, the applicability of optofluidics based analytics for small-scale high-throughput quantitative solubility and biological activity screening is demonstrated.

摘要

溶解度是决定物质吸收和生物利用度的主要物理化学性质。在这里,我们提出了一种基于片上流体动力学粒子捕获和光学粒子尺寸监测的微尺度平衡溶解度测定的光流控单粒子技术。该方法结合了物理分析的快速性、普遍性和节省物质的特点,以及传统上与化学分析相关的准确性。应用扩散层理论,我们从初始质量仅为 14μg 的单个纯物质微粒子中,在几秒钟到几分钟内确定了平衡溶解度。与金标准方法相比,时间和物质消耗的减少超过 2 个数量级。由于溶解度数据的准确性提高了 3 倍以上,因此证明了基于光流控分析的适用于小规模高通量定量溶解度和生物活性筛选的适用性。

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