Lestari Uce, Muhaimin Muhaimin, Chaerunisaa Anis Yohana, Sujarwo Wawan
Doctoral Program of Pharmacy, Faculty of Pharmacy, Universitas Padjadjaran, Jalan Raya Bandung-Sumedang Km 21, Jatinangor 45363, Indonesia.
Department of Pharmacy, Faculty of Medicine and Health Sciences, Universitas Jambi, Jalan Jambi-Muara Bulian Km 15, Mendalo Indah 36361, Indonesia.
Pharmaceuticals (Basel). 2025 Feb 20;18(3):288. doi: 10.3390/ph18030288.
Natural polymer nanoparticles have potential as delivery systems, can enhance pharmacological activity, and can improve stability in the cosmetic field. In this research, we implemented a development approach for chitosan-alginate and chitosan-pectin nanoparticles. This study aimed to investigate effect of formulation, process variables, in vitro antiaging evaluation, and metabolite profiling of leaf extracts. : Polymeric nanoparticles have been prepared using the ionic gelation method (Temperature = 40 °C, time = 1 h and speed = 1000 rpm), in vitro antiaging evaluation using the Neutrophil Elastase Inhibitor Screening Kit method, and analysis of metabolite profiling with UHPLC-HRMS. : Research results found that the SLE and EAFSL nanoparticles that have good and stable characteristics before and after storage in a climatic chamber after 3 months are FIIA-NPSLE (0.75% chitosan and 1.25% Alginate), FIP-NPSLE (1% chitosan and 0.5% Pectin), FIIA-NPEAFSL (0.75% chitosan and 1.25% Alginate), and FIIIP-NPEAFSL (0.125% chitosan and 0.375% Alginate). Chitosan-alginate polymers, such as FIIA-NPEAFSL, have higher inhibition of the elastase enzyme than FIIA-NPSLE, with a % inhibition (IC) of FIIA-NPEAFSL being 87.30%, while the IC of FIIA-NPSLE is 39.40%. Meanwhile, using chitosan-pectin polymers, such as FIP-NPSLE, results in lower inhibition of the elastase enzyme compared to the chitosan-alginate polymer, with an IC of 27.28% while IC FIIIP-NPEAFSL is 39.53%. SLE and EAFSL nanoparticles with chitosan-alginate and chitosan-pectin polymers resulted in a significant PDI during storage from 1.3 to 1.9, and zeta potential values were very low, ranging from -11 mV to -27 mV. Metabolite profiling using UHPLC-HRMS on leaf extracts revealed that the main compounds contained were glycitein, quercetin, quercetin-3β-D-glucoside, kaempferol, and ellagic acid, which has potential as an antiaging agent. : It can be concluded that using chitosan, alginate, and pectin in the process of encapsulating extracts into nanoparticles with the same process variables affect evaluation of antiaging activity in elastase enzymes. Further research will develop these nanoparticles into nanohydrogels with antiaging activity.
天然聚合物纳米颗粒有作为递送系统的潜力，可增强药理活性，并能提高在化妆品领域的稳定性。在本研究中，我们实施了一种壳聚糖 - 海藻酸盐和壳聚糖 - 果胶纳米颗粒的开发方法。本研究旨在研究配方、工艺变量、体外抗老化评估以及叶提取物的代谢物谱分析的影响。：已使用离子凝胶法（温度 = 40 °C，时间 = 1 h，速度 = 1000 rpm）制备了聚合物纳米颗粒，使用中性粒细胞弹性蛋白酶抑制剂筛选试剂盒方法进行体外抗老化评估，并使用超高效液相色谱 - 高分辨质谱分析代谢物谱。：研究结果发现，在气候箱中储存3个月前后具有良好且稳定特性的SLE和EAFSL纳米颗粒是FIIA - NPSLE（0.75%壳聚糖和1.25%海藻酸盐）、FIP - NPSLE（1%壳聚糖和0.5%果胶）、FIIA - NPEAFSL（0.75%壳聚糖和1.25%海藻酸盐）以及FIIIP - NPEAFSL（0.125%壳聚糖和0.375%海藻酸盐）。壳聚糖 - 海藻酸盐聚合物，如FIIA - NPEAFSL，对弹性蛋白酶的抑制作用高于FIIA - NPSLE，FIIA - NPEAFSL的抑制率（IC）为87.30%，而FIIA - NPSLE的IC为39.40%。同时，使用壳聚糖 - 果胶聚合物，如FIP - NPSLE，与壳聚糖 - 海藻酸盐聚合物相比，对弹性蛋白酶的抑制作用较低，IC为27.28%，而FIIIP - NPEAFSL的IC为39.53%。含有壳聚糖 - 海藻酸盐和壳聚糖 - 果胶聚合物的SLE和EAFSL纳米颗粒在储存期间导致显著的多分散指数（PDI）从1.3变为1.9，并且zeta电位值非常低，范围从 - 11 mV到 - 27 mV。使用超高效液相色谱 - 高分辨质谱对叶提取物进行代谢物谱分析表明，所含主要化合物为黄豆黄素、槲皮素、槲皮素 - 3β - D - 葡萄糖苷、山奈酚和鞣花酸，它们具有作为抗老化剂的潜力。：可以得出结论，在将提取物包封到纳米颗粒的过程中使用壳聚糖、海藻酸盐和果胶，在相同工艺变量下会影响弹性蛋白酶中抗老化活性的评估。进一步的研究将把这些纳米颗粒开发成具有抗老化活性的纳米水凝胶。
