目的:本研究旨在准备,表征,并在体外和体内评估了一种新型的纳米结构脂质载体(NLCs)制剂,该制剂含有两种甘草(甘草)提取物,用于治疗色素沉着过度。
方法:两个分数,一种富含甘草苷(FEG),另一种富含甘草苷(FEL),通过用乙酸乙酯(EtOAc)分配甘草根的甲醇(MeOH)提取物和用丁醇(n-BuOH)和水分配EtOAc级分获得。通过高效液相色谱(HPLC)测定馏分中的光甘草苷(Glab)和甘草苷(LQ)的量。FEG和FEL装载在不同的NLC配方中,使用动态光散射(DLS)研究了表面表征和长期稳定性。选择最佳配方进行进一步的表面表征,包括透射电子显微镜(TEM),差示扫描量热法(DSC),和傅立叶变换红外(FTIR)光谱。此外,包封效率百分比(EE%),体外药物释放,体内皮肤渗透,对B16F10黑色素瘤细胞的细胞毒性,对黑色素产生的影响,测试所选制剂的抗酪氨酸酶活性。
结果:基于HPLC结果,FEG含有34.501mg/g的Glab,和FEL含有31.714mg/g的LQ。在20种不同的配方中,NLC20(LG-NLC)显示出理想的DLS结果,Z平均尺寸为185.3±1.08nm,多分散指数(PDI)为0.229±0.35,ζ电位为-16.2±1.13mV。它表明良好的球形,高EE%(Glab为79.01%,LQ为69.27%),两阶段释放模式(初始爆发释放,然后持续释放),有效的体内皮肤渗透,和强大的抗酪氨酸酶活性。LG-NLC具有可接受的物理化学稳定性长达9个月并且是非细胞毒性的。
结论:LG-NLC配方显示了理想的表面表征,良好的理化稳定性,有效的药物释放模式和体内渗透,高EE%。因此,它可以是用于递送甘草提取物治疗色素沉着过度的合适的纳米系统。
OBJECTIVE: This study aimed to prepare, characterize, and in vitro and in vivo evaluate a novel nanostructured lipid carriers (NLCs) formulation containing two fractions of Glycyrrhiza glabra L. (licorice) extract for the treatment of hyperpigmentation.
METHODS: 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%), in vitro drug release, in vivo skin penetration, cytotoxicity on B16F10 melanoma cells, effect on melanin production, and anti- tyrosinase activity were tested for the selected formulation.
RESULTS: 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 in vivo skin penetration, and strong anti-tyrosinase activity. LG-NLCs had acceptable physiochemical stability for up to 9 months and were non-cytotoxic.
CONCLUSIONS: The LG-
NLC formulation has revealed desirable surface characterization, good physiochemical stability, efficient drug release pattern and in vivo penetration, and high EE%. Therefore, it can be a suitable nanosystem for the delivery of licorice extract in the treatment of hyperpigmentation.