Aanisah Nuur, Sulistiawati Sulistiawati, Djabir Yulia Yusrini, Asri Rangga Meidianto, Sumarheni Sumarheni, Chabib Lutfi, Hamzah Hasyrul, Permana Andi Dian
Department of Pharmacy, Faculty of Science, Tadulako University, Palu94118, Indonesia.
Faculty of Pharmacy, Hasanuddin University, Makassar90245, Indonesia.
Langmuir. 2023 Feb 7;39(5):1838-1851. doi: 10.1021/acs.langmuir.2c02754. Epub 2023 Jan 26.
Safflower ( L.) is a potent natural antioxidant because of active compounds such as quercetin (QU) and luteolin (LU). These components prevent damage to the skin caused by free radicals from UV rays. However, due to the poor solubility and transdermal permeation, the effectiveness of the compounds in showing their activity was limited. In this study, we develop solid lipid nanoparticle (SLN)-based hydrogel formulations to enhance the solubility and penetration of two bioactive compounds found in safflower petals extract (SPE). The hot emulsification-ultrasonication method was used to produce SLNs, and to obtain high antioxidant activity, 100% v/v ethanol was used in the extraction procedure. The results showed that this approach could encapsulate >80% of both QU and LU. Moreover, Fourier transform infrared (FTIR), differential scanning calorimetry (DSC), and powder X-ray diffraction (PXRD) spectra indicated that most of the QU and LU were trapped in a lipid matrix and dispersed homogeneously at the molecular level, increasing the solubility. Additionally, SLN-hydrogel composites are able to release two lipophilic bioactive compounds for 24 h, which also demonstrated increased skin retention and penetrability of the QU and LU up to 19-fold. In vitro blood biocompatibility showed that no hemolytic toxicity was observed below 500 μg/mL. Accordingly, the formulation was considered safe for use. Sun protective factor (SPF) test shows a value above 15, showing an excellent promising application as the photoprotective agent to prevent symptoms associated with photoinduced skin aging.
红花(Carthamus tinctorius L.)因其含有槲皮素(QU)和木犀草素(LU)等活性化合物而成为一种有效的天然抗氧化剂。这些成分可防止紫外线产生的自由基对皮肤造成损伤。然而,由于其溶解性和透皮渗透性较差,这些化合物发挥活性的效果受到限制。在本研究中,我们开发了基于固体脂质纳米粒(SLN)的水凝胶制剂,以提高红花花瓣提取物(SPE)中两种生物活性化合物的溶解度和渗透性。采用热乳化-超声法制备SLN,为获得高抗氧化活性,提取过程中使用了100% v/v乙醇。结果表明,该方法可包封80%以上的QU和LU。此外,傅里叶变换红外光谱(FTIR)、差示扫描量热法(DSC)和粉末X射线衍射(PXRD)光谱表明,大部分QU和LU被困在脂质基质中,并在分子水平上均匀分散,从而提高了溶解度。此外,SLN-水凝胶复合材料能够在24小时内释放两种亲脂性生物活性化合物,这也表明QU和LU在皮肤中的滞留和渗透能力提高了19倍。体外血液生物相容性表明,在500μg/mL以下未观察到溶血毒性。因此,该制剂被认为使用安全。防晒系数(SPF)测试显示值高于15,作为预防光诱导皮肤老化相关症状的光保护剂具有极好的应用前景。