Department of Pharmacognosy, Faculty of Pharmacy, Tehran University of Medical Sciences, Tehran, Iran.
Department of Pharmaceutics, School of Pharmacy, Mashhad University of Medical Sciences, Mashhad, Iran.
Curr Pharm Des. 2024;30(40):3213-3232. doi: 10.2174/0113816128327512240730102545.
This study aimed to prepare, characterize, and and evaluate a novel nanostructured lipid carriers (NLCs) formulation containing two fractions of L. (licorice) extract for the treatment of hyperpigmentation.
Two fractions, one enriched with glabridin (FEG) and the other enriched with liquiritin (FEL), were obtained by partitioning the methanol (MeOH) extract of licorice roots with ethyl acetate (EtOAc) and partitioning the EtOAc fraction with butanol (n-BuOH) and water. The quantities of glabridin (Glab) and liquiritin (LQ) in the fractions were determined by high-performance liquid chromatography (HPLC). FEG and FEL were loaded in different NLC formulations, and surface characterization and long-term stability were studied using Dynamic Light Scattering (DLS). The best formulation was chosen for further surface characterization, including Transmission Electron Microscopy (TEM), Differential Scanning Calorimetry (DSC), and Fouriertransform infrared (FTIR) spectroscopy. Moreover, entrapment efficiency percentage (EE%), drug release, skin penetration, cytotoxicity on B16F10 melanoma cells, effect on melanin production, and anti- tyrosinase activity were tested for the selected formulation.
Based on HPLC results, FEG contained 34.501 mg/g of Glab, and FEL contained 31.714 mg/g of LQ. Among 20 different formulations, NLC 20 (LG-NLCs) showed desirable DLS results with a Z-average size of 185.3 ± 1.08 nm, polydispersity index (PDI) of 0.229 ± 0.35, and zeta potential of -16.2 ± 1.13 mV. It indicated good spherical shape, high EE% (79.01% for Glab and 69.27% for LQ), two-stage release pattern (an initial burst release followed by sustained release), efficient skin penetration, and strong anti-tyrosinase activity. LG-NLCs had acceptable physiochemical stability for up to 9 months and were non-cytotoxic.
The LG-NLC formulation has revealed desirable surface characterization, good physiochemical stability, efficient drug release pattern and penetration, and high EE%. Therefore, it can be a suitable nanosystem for the delivery of licorice extract in the treatment of hyperpigmentation.
本研究旨在制备、表征和评估一种新型纳米结构脂质载体（NLCs）制剂，该制剂含有甘草提取物的两种馏分，用于治疗色素沉着过度。
通过用乙酸乙酯（EtOAc）对甘草根的甲醇（MeOH）提取物进行分区以及用正丁醇（n-BuOH）和水对 EtOAc 馏分进行分区，得到两种馏分，一种馏分富含甘草苷（FEG），另一种馏分富含甘草素（FEL）。通过高效液相色谱法（HPLC）测定馏分中甘草苷（Glab）和甘草素（LQ）的含量。将 FEG 和 FEL 载入不同的 NLC 制剂中，并通过动态光散射（DLS）研究表面特性和长期稳定性。选择最佳制剂进行进一步的表面特性研究，包括透射电子显微镜（TEM）、差示扫描量热法（DSC）和傅里叶变换红外光谱（FTIR）光谱。此外，还对所选制剂进行了包封效率百分比（EE%）、药物释放、皮肤渗透、对 B16F10 黑素瘤细胞的细胞毒性、对黑色素生成的影响和对酪氨酸酶活性的测试。
根据 HPLC 结果，FEG 中含有 34.501mg/g 的甘草苷，FEL 中含有 31.714mg/g 的甘草素。在 20 种不同的制剂中，NLC20（LG-NLCs）显示出理想的 DLS 结果，Z 均粒径为 185.3±1.08nm，多分散指数（PDI）为 0.229±0.35，zeta 电位为-16.2±1.13mV。表明具有良好的球形形状、高 EE%（甘草苷为 79.01%，甘草素为 69.27%）、两阶段释放模式（初始突释后持续释放）、高效皮肤渗透和强的酪氨酸酶抑制活性。LG-NLCs 在长达 9 个月的时间内具有良好的物理化学稳定性，且无细胞毒性。
LG-NLC 制剂表现出理想的表面特性、良好的物理化学稳定性、高效的药物释放模式和渗透以及高 EE%。因此，它可以成为甘草提取物在治疗色素沉着过度中的一种合适的纳米系统。
