School of Cosmetic Science, Mae Fah Luang University, 333, Moo.1, Thasud, Muang, Chiang Rai 57100, Thailand.
Cosmetic and Beauty Innovations for Sustainable Development (CBIS) Research Group, Mae Fah Luang University, 333, Moo.1, Thasud, Muang, Chiang Rai 57100, Thailand.
Molecules. 2023 Sep 27;28(19):6830. doi: 10.3390/molecules28196830.
Encapsulation of bioactive compounds in the liposome system provides several advantages, such as enhancing the stability and lowering the toxicity of active compounds. Coffee berry extract (CBE) has previously been established to have in vitro anti-aging properties and to retard the aging of human skin. The purposes of this study were to encapsulate CBE in nanoliposomes and to assess its stability and in vitro anti-aging potential in human dermal fibroblasts (HDF), as well as in healthy human skin. In the HDF model, anti-aging potential was determined by nitric oxide (NO) and collagenase inhibition assays and a superoxide dismutase (SOD) activity assay, whereas in healthy human skin (in vivo), the skin elasticity and brightness were examined. First, liposomal CBE (L-CBE) was created with a particle size of 117.33 ± 2.91 nm, a polydispersity index (PDI) of 0.36 ± 0.03, and a zeta potential of -56.13 ± 1.87 mV. The percentages of encapsulation efficacy (%EE) and loading efficacy (%LE) were 71.26 ± 3.12% and 2.18 ± 0.18%, respectively. After undergoing a 12-week stability test, the L-CBE retained more phenolic content than the free CBE when stored at 4 °C, room temperature, and 45 °C. Compared to free CBE, the L-CBE demonstrated a more consistent, elevated, and prolonged release of phenolics from the lipid system. In human dermal fibroblasts, L-CBE showed lower toxicity, and at its maximum nontoxic concentration (10 mg/mL), it exhibited slightly higher anti-aging effects than CBE, including NO inhibition, enhanced SOD activity, and anti-collagenase activities. In clinical trials (30 volunteer subjects), none of the participants' skin was irritated when the L-CBE, the CBE, or base creams were applied. After 2 weeks of application, the L-CBE and CBE creams both demonstrated an improvement in skin elasticity and a reduction in melanin levels, and after 4 weeks, L-CBE cream showed a significantly greater improvement in skin elasticity and lightening. The results demonstrate that the encapsulation of the CBE in liposomal systems could increase its stability and skin penetration, reduce its toxicity, and maintain its anti-aging effect, which is powerful enough to be exploited in anti-aging and whitening agents for application in cosmetics and cosmeceuticals.
将生物活性化合物包封在脂质体系统中具有多种优势,例如可以提高活性化合物的稳定性和降低其毒性。咖啡浆果提取物(CBE)已被证实具有体外抗衰老特性,并能延缓人体皮肤衰老。本研究的目的是将 CBE 包封在纳米脂质体中,并评估其在人真皮成纤维细胞(HDF)和健康人皮肤上的稳定性和体外抗衰老潜力。在 HDF 模型中,通过一氧化氮(NO)和胶原酶抑制试验以及超氧化物歧化酶(SOD)活性测定来确定抗衰老潜力,而在健康人皮肤上(体内),则检测皮肤弹性和亮度。首先,制备粒径为 117.33±2.91nm、多分散指数(PDI)为 0.36±0.03、Zeta 电位为-56.13±1.87mV 的脂质体 CBE(L-CBE)。包封效率(%EE)和载药效率(%LE)分别为 71.26±3.12%和 2.18±0.18%。经过 12 周的稳定性测试,L-CBE 在 4°C、室温、45°C 下储存时比游离 CBE 保留更多的酚类物质。与游离 CBE 相比,L-CBE 从脂质体系统中表现出更一致、更高、更持久的酚类释放。在人真皮成纤维细胞中,L-CBE 表现出较低的毒性,在其最大非毒性浓度(10mg/mL)下,其表现出的抗衰老效果略高于 CBE,包括 NO 抑制、增强 SOD 活性和抗胶原酶活性。在临床试验(30 名志愿者)中,应用 L-CBE、CBE 或基础霜时,没有参与者的皮肤受到刺激。应用 2 周后,L-CBE 和 CBE 霜均显示出皮肤弹性的改善和黑色素水平的降低,4 周后,L-CBE 霜显示出皮肤弹性的显著改善和提亮。结果表明,将 CBE 包封在脂质体系统中可以提高其稳定性和皮肤渗透性,降低其毒性,并保持其抗衰老作用,足以用于化妆品和药妆品中的抗衰老和美白剂。