Sainakham Mathukorn, Promma Bouachompoo, Ngernthong Arthima, Kiattisin Kanokwan, Boonpisuttinant Korawinwich, Wuttikul Krisada, Jantrawut Pensak, Ruksiriwanich Warintorn
Department of Pharmaceutical Sciences, Faculty of Pharmacy, Chiang Mai University, Chiang Mai, 50200, Thailand.
Cluster of Valorization and Bio-Green Transformation for Translational Research Innovation of Raw Materials and Products, Chiang Mai University, Chiang Mai, 50200, Thailand.
Heliyon. 2024 Jul 15;10(14):e34665. doi: 10.1016/j.heliyon.2024.e34665. eCollection 2024 Jul 30.
In the present, whitening products are most popular in the cosmetics market, and nanoemulsions are effective drug delivery systems through the skin. The objective of this study was to investigate multiple nanoemulsion formulations for lightning skin effects. The method of this study was the selection of active compounds based on synergistic tyrosinase inhibition activity, formulation preparation by low and high energy methods, physicochemical property determination, stability test, cell toxicity, and anti-melanogenesis in cell culture. From the results, it was found that tyrosinase inhibition with substrate l-tyrosine from the mixture of curcumin and alpha-arbutin gave the highest activity with an IC of 63.58 ± 4.99 μM, showed a synergistic effect at a CI value of 0.99, and selected these compounds to develop formulations by the low energy method. However, the most formulations prepared by this method were unstable and phase separated, while the high energy method gave the most formulations with good properties, which were selected for further investigation. The best formulation was 2DS which showed internal droplet morphology in the range of nanometers under a TEM microscope. For 3 months stability test, the formulations had no phase separation and gave the slightly changed values of particle size, polydispersity index (PDI), zeta potentials, and pH values. In addition, multiple nanoemulsions also enhanced the stability of active compounds, with the highest percentage of remaining content of curcumin and arbutin at 94.69 and 90.45 %, respectively at 4 °C for 3 months. In a cell culture test on BF, 2DS at 0.05 g/ml gave no cell cytotoxicity and anti-melanogenesis at 57.75 ± 5.74 %, the same potency as kojic acid at a concentration of 20 μg/ml. Therefore, this study will be useful to prepare multiple nanoemulsions for further development into novel health care products.
目前，美白产品在化妆品市场中最为流行，而纳米乳剂是有效的经皮给药系统。本研究的目的是研究多种纳米乳剂配方对皮肤美白的效果。本研究方法包括基于协同酪氨酸酶抑制活性选择活性化合物、通过低能和高能方法制备配方、测定理化性质、进行稳定性测试、细胞毒性测试以及细胞培养中的抗黑色素生成测试。结果发现，姜黄素和α - 熊果苷混合物对以L - 酪氨酸为底物的酪氨酸酶抑制活性最高，IC50为63.58 ± 4.99 μM，CI值为0.99时显示出协同效应，并选择这些化合物通过低能方法开发配方。然而，用这种方法制备的大多数配方不稳定且会发生相分离，而高能方法制备的大多数配方性质良好，被选用于进一步研究。最佳配方是2DS，在透射电子显微镜下显示内部液滴形态在纳米范围内。经过3个月的稳定性测试，这些配方没有相分离，粒径、多分散指数（PDI）、zeta电位和pH值的变化很小。此外，多种纳米乳剂还提高了活性化合物的稳定性，在4℃下放置3个月时，姜黄素和熊果苷的最高剩余含量分别为94.69%和90.45%。在BF细胞培养试验中，0.05 g/ml的2DS没有细胞毒性，抗黑色素生成率为57.75 ± 5.74%，与浓度为20 μg/ml的曲酸效力相同。因此，本研究对于制备多种纳米乳剂以进一步开发新型保健品具有重要意义。
