Department of Pharmaceutics, National Institute of Pharmaceutical Education and Research, Hyderabad, Telangana, India.
Department of Chemical Sciences, National Institute of Pharmaceutical Education and Research, Hyderabad, Telangana, India.
AAPS PharmSciTech. 2023 May 25;24(5):126. doi: 10.1208/s12249-023-02581-0.
The current research was aimed to synthesize a phytomolecule, naringenin (NRG)-mediated silver nanoparticles (NRG-SNPs) to study their antifungal potential against Candida albicans (C. albicans) and Candida glabrata (C. glabrata). The NRG-SNPs were synthesized by using NRG as a reducing agent. The synthesis of NRG-SNPs was confirmed by a color change and surface plasmon resonance (SPR) peak at 425 nm. Furthermore, the NRG-SNPs were analyzed for size, PDI, and zeta potential, which were found to be 35 ± 0.21 nm, 0.19 ± 0.03, and 17.73 ± 0.92 mV, respectively. In silico results demonstrated that NRG had a strong affinity towards the sterol 14α-demethylase. The docking with ceramide revealed the skin permeation efficiency of the NRG-SNPs. Next, the NRG-SNPs were loaded into the topical dermal dosage form (NRG-SNPs-TDDF) by formulating a gel using Carbopol Ultrez 10 NF. The MIC of NRG solution and TSC-SNPs against C. albicans was found to be 50 µg/mL and 4.8 µg/mL, respectively, significantly (P < 0.05) higher than 0.3625 µg/mL of NRG-SNPs-TDDF. Correspondingly, MIC results were calculated against C. glabrata and the results of NRG, TSC-SNPs, NRG-SNPs-TDDF, and miconazole nitrate were found to be 50 µg/mL, 9.6 µg/mL, 0.3625 µg/mL, and 3-µg/mL, respectively. Interestingly, MIC of NRG-SNPs-TDDF was significantly (P < 0.05) lower than MIC of miconazole nitrate against C. glabrata. The FICI (fractional inhibitory concentration index) value against both the C. albicans and C. glabrata was found to be 0.016 and 0.011, respectively, which indicated the synergistic antifungal activity of NRG-SNPs-TDDF. Thus, NRG-SNPs-TDDF warrants further in depth in vivo study under a set of stringent parameters for translating in to a clinically viable antifungal product.
本研究旨在合成一种植物分子柚皮素（NRG）介导的银纳米粒子（NRG-SNPs），以研究其对白色念珠菌（C. albicans）和光滑念珠菌（C. glabrata）的抗真菌潜力。NRG-SNPs 的合成是使用 NRG 作为还原剂来实现的。NRG-SNPs 的合成通过颜色变化和表面等离子体共振（SPR）峰在 425nm 处得到证实。此外，对 NRG-SNPs 的粒径、PDI 和 zeta 电位进行了分析，结果分别为 35±0.21nm、0.19±0.03 和 17.73±0.92mV。计算结果表明，NRG 与甾醇 14α-脱甲基酶具有很强的亲和力。与神经酰胺的对接揭示了 NRG-SNPs 的皮肤渗透效率。接下来，通过使用 Carbopol Ultrez 10 NF 配制凝胶，将 NRG-SNPs 载入局部皮肤给药剂型（NRG-SNPs-TDDF）。NRG 溶液和 TSC-SNPs 对 C. albicans 的 MIC 分别为 50μg/mL 和 4.8μg/mL，明显（P<0.05）高于 NRG-SNPs-TDDF 的 0.3625μg/mL。相应地，对 C. glabrata 进行了 MIC 计算，结果表明 NRG、TSC-SNPs、NRG-SNPs-TDDF 和硝酸咪康唑的 MIC 分别为 50μg/mL、9.6μg/mL、0.3625μg/mL 和 3μg/mL。有趣的是，NRG-SNPs-TDDF 对 C. glabrata 的 MIC 明显（P<0.05）低于硝酸咪康唑的 MIC。对 C. albicans 和 C. glabrata 的 FICI（抑菌浓度指数）值分别为 0.016 和 0.011，表明 NRG-SNPs-TDDF 具有协同抗真菌活性。因此，NRG-SNPs-TDDF 值得在更严格的参数下进一步深入的体内研究，以转化为一种临床可行的抗真菌产品。
