载入微胶束以调节其水溶性的非甾体抗炎药物。
Non-Steroidal Anti-Inflammatory Drugs Loaded to Micelles for the Modulation of Their Water Solubility.
机构信息
Inorganic Chemistry Laboratory, Department of Chemistry, University of Ioannina, 45110 Ioannina, Greece.
Physical Chemistry Laboratory, Department of Chemistry, University of Ioannina, 45110 Ioannina, Greece.
出版信息
Int J Mol Sci. 2023 Oct 13;24(20):15152. doi: 10.3390/ijms242015152.
The low water solubility of aspirin (ASPH) is well known, creating research challenges regarding both its composition and its delivery. Therefore, the development of new aspirin-based formulations that are water soluble is a research, technological, and financial issue. With the aim to improve the water solubility of ASPH, the micelle of formula (SLS = Sodium Lauryl Sulfate) was formed. The Critical Micelle Concentration (CMC) of SLS in the presence of ASPH was determined by ultrasonic velocity, complementary, and transient birefringence measurements. The was characterized by the melting point (m.p.), attenuated total reflection spectroscopy (FT-IR-ATR), and X-ray fluorescence spectroscopy (XRF) in a solid state and in a solution by ultraviolet-visible (UV-Vis) and H NMR spectroscopies. The SLS/ASPH molar ratio was determined to be 5/1 in . The inhibitory activity of towards lipoxygenase (LOX), an enzyme that takes part in the inflammation mechanism, was studied. The inhibitory activity of against LOX is 3.5-fold stronger than that of free SLS. The in vitro toxicity of the was tested on immortalized human keratinocyte (HaCaT) cells.
阿司匹林（ASPH）的水溶性低是众所周知的，这给其组成和输送都带来了研究上的挑战。因此，开发新的水溶性阿司匹林制剂是一个研究、技术和财务问题。为了提高 ASPH 的水溶性，形成了（SLS = 十二烷基硫酸钠）的胶束。通过超声速度、互补和瞬态双折射测量来确定 SLS 在存在 ASPH 时的临界胶束浓度（CMC）。通过熔点（m.p.）、衰减全反射光谱（FT-IR-ATR）和 X 射线荧光光谱（XRF）在固态和溶液中进行表征，通过紫外可见（UV-Vis）和 H NMR 光谱进行。在 中确定 SLS/ASPH 的摩尔比为 5/1。研究了 对参与炎症机制的脂氧合酶（LOX）的抑制活性。与游离 SLS 相比， 对 LOX 的抑制活性强 3.5 倍。在永生化人角质形成细胞（HaCaT）细胞上测试了 的体外毒性。
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