Departamento de Química Farmacológica y Toxicológica, Facultad de Ciencias Químicas y Farmacéuticas, Universidad de Chile, Chile; Advanced Center of Chronic Diseases (ACCDiS), Chile; Departamento de Ciencias y Tecnología Farmacéuticas, Facultad de Ciencias Químicas y Farmacéuticas, Universidad de Chile, Chile; Université Grenoble Alpes, CNRS, Grenoble INP, Intitut Néel, France.
Université Grenoble Alpes, CNRS, Grenoble INP, Intitut Néel, France.
Int J Pharm. 2024 Sep 5;662:124507. doi: 10.1016/j.ijpharm.2024.124507. Epub 2024 Jul 22.
Epigallocatechin-3-gallate (EGCG) exhibits several pharmacological activities with potential benefits for human health, however, it has low oral bioavailability. A promising approach is to transport EGCG in a nanostructured system to protect it until it reaches the site of action and also allow combining chemotherapy with phototherapy to improve its therapeutic efficiency. The aim of this work was to synthesize GNR@mSiO-NH/EGCG and characterize the adsorption process, its antioxidant activity, properties and photothermal stability, for its potential use in chemo-photothermal therapy. The nanosystem presented good encapsulation efficiency (19.2 %) and EGCG loading capacity (6.0 %). The DPPH• free radical scavenging capacity (RSA) and chelating activity of the nanosystem was 60.7 ± 6.9 % and 71.0 ± 6.4 % at an EGCG equivalent concentration of 1 µg/mL and 30 µg/mL, respectively. The core-shell NPs presented a good photothermal transduction efficiency of 17 %. EGCG free, as well as its RSA and chelating activity, remained stable after NIR irradiation (808 nm, 7 W/cm). The morphology of GNR@mSiO remained intact after being irradiated with NIR, however, ultrasmall gold NPs could be observed, probably a product of photocracking of GNR. In summary, the nanosystem has good antioxidant activity, photothermal stability, and photothermal transduction ability making it potentially useful for chemo-photothermal therapy.
没食子酸表没食子儿茶素酯(EGCG)具有多种药理学活性,对人类健康有益,但口服生物利用度低。一种有前途的方法是将 EGCG 输送到纳米结构系统中,以保护它直到到达作用部位,并允许将化学疗法与光疗结合使用,以提高其治疗效率。本工作的目的是合成 GNR@mSiO-NH/EGCG 并对其吸附过程、抗氧化活性、性质和光热稳定性进行表征,以将其潜在用于化学-光热治疗。该纳米系统具有良好的包封效率(19.2%)和 EGCG 载药量(6.0%)。纳米系统的 DPPH•自由基清除能力(RSA)和螯合活性在 EGCG 当量浓度为 1μg/mL 和 30μg/mL 时分别为 60.7±6.9%和 71.0±6.4%。核壳 NPs 具有良好的光热转换效率为 17%。在近红外辐射(808nm,7W/cm)后,EGCG 游离物以及其 RSA 和螯合活性仍然稳定。在近红外辐射后,GNR@mSiO 的形态保持完整,但可以观察到超小的金 NPs,可能是 GNR 光解的产物。总之,该纳米系统具有良好的抗氧化活性、光热稳定性和光热转换能力,使其有可能用于化学-光热治疗。