Oxidative stress is caused by reactive oxygen species (ROS) and is related to skin cancer and aging. Although anthocyanin is an effective antioxidant, has poor skin permeability and is vulnerable to temperature and pH, a suitable formulation is required. We prepared a pH-gradient loading method to prepare anthocyanin-loaded liposomes because liposomes prepared by the remote loading method exhibit high loading efficiency without anthocyanin damage. The liposome formulation could enhance anthocyanin stability, antioxidation activity and skin permeability. To compare these features, nonformulated anthocyanin (NFA) and anthocyanin-loaded liposomes prepared by the passive loading method were used as control groups. Anthocyanin-loaded HSPC liposomes prepared by the remote loading method (RAH liposomes) exhibited markedly enhanced loading efficiency (71.2%) and anthocyanin stability (85.4%) compared with control groups. The antioxidation activity of RAH liposomes was 2.1- and 1.7-fold greater than NFA and passive loading of anthocyanin in HSPC liposomes (PAH liposomes), respectively. The skin permeability of RAH liposomes was enhanced 2.9- and 2.2-fold compared with NFA and PAH liposomes, respectively. RAH liposomes maintained anthocyanin stability under in vitro physiological conditions for 14 days and exhibited enhanced ROS scavenging activity and skin permeability. Therefore, RAH liposomes represent a platform for effective anthocyanin loading and exhibited promising application for pharmaco-cosmetics.

中文翻译：

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通过pH梯度上样法制备的花青素负载脂质体可增强花青素的稳定性，抗氧化作用和皮肤渗透性

氧化应激是由活性氧（ROS）引起的，与皮肤癌和衰老有关。尽管花色苷是有效的抗氧化剂，皮肤渗透性差，并且容易受温度和pH的影响，但仍需要合适的制剂。我们准备了一种pH梯度加载方法来制备花青素负载的脂质体，因为通过远程加载方法制备的脂质体显示出高的负载效率而不会破坏花色苷。脂质体制剂可以增强花青苷的稳定性，抗氧化活性和皮肤渗透性。为了比较这些特征，将通过被动加载方法制备的未配制花色苷（NFA）和负载花色苷的脂质体用作对照组。通过远程加载方法制备的花青素负载HSPC脂质体（RAH脂质体）显示出显着提高的加载效率（71。2％）和花青素稳定性（85.4％）。RAH脂质体的抗氧化活性分别是NFA和HSPC脂质体（PAH脂质体）中花色苷被动负载的2.1倍和1.7倍。与NFA和PAH脂质体相比，RAH脂质体的皮肤渗透性分别提高了2.9倍和2.2倍。RAH脂质体在体外生理条件下维持花色苷稳定性14天，并具有增强的ROS清除活性和皮肤通透性。因此，RAH脂质体代表了有效花色苷负载的平台，并显示出有望用于药物化妆品的应用。HSPC脂质体（PAH脂质体）中的NFA和花色苷的被动负载分别比后者高7倍。与NFA和PAH脂质体相比，RAH脂质体的皮肤渗透性分别提高了2.9倍和2.2倍。RAH脂质体在体外生理条件下维持花色苷稳定性14天，并具有增强的ROS清除活性和皮肤通透性。因此，RAH脂质体代表了有效花色苷负载的平台，并显示出有望用于药物化妆品的应用。HSPC脂质体（PAH脂质体）中的NFA和花色苷的被动负载分别比NFA大7倍。与NFA和PAH脂质体相比，RAH脂质体的皮肤渗透性分别提高了2.9倍和2.2倍。RAH脂质体在体外生理条件下维持花色苷稳定性14天，并具有增强的ROS清除活性和皮肤通透性。因此，RAH脂质体代表了有效花色苷负载的平台，并显示出有望用于药物化妆品的应用。RAH脂质体在体外生理条件下维持花色苷稳定性14天，并具有增强的ROS清除活性和皮肤通透性。因此，RAH脂质体代表了有效花色苷负载的平台，并显示出有望用于药物化妆品的应用。RAH脂质体在体外生理条件下维持花色苷稳定性14天，并具有增强的ROS清除活性和皮肤通透性。因此，RAH脂质体代表了有效花色苷负载的平台，并显示出有望用于药物化妆品的应用。