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Liposomes augment biological benefits of curcumin for multitargeted skin therapy
European Journal of Pharmaceutics and Biopharmaceutics ( IF 4.9 ) Pub Date : 2019-09-19 , DOI: 10.1016/j.ejpb.2019.09.016
Selenia Ternullo , Eivind Gagnat , Kjersti Julin , Mona Johannessen , Purusotam Basnet , Željka Vanić , Nataša Škalko-Basnet

Curcumin, a multi-targeting pharmacologically active compound, is a promising molecule for the treatment of skin inflammation and infection in chronic wounds. However, its hydrophobic nature remains to be a challenge in development of its pharmaceutical products, including dermatopharmaceuticals. Here we propose deformable liposomes (DLs) as a mean to overcome the curcumin limitations in skin treatment. We explored the properties and biological effects of curcumin containing DLs (curcumin-DLs) with varying surface charge by preparing the neutral (NDLs), cationic (CDLs) and anionic (ADLs) nanocarriers. The vesicles of mean diameter 200–300 nm incorporated high curcumin load mirroring the type of employed surfactant. Curcumin-CDLs provided the most sustained ex vivo penetration of curcumin through the full thickness human skin. Although the curcumin-CDLs were the most potent regarding the in vitro anti-inflammatory activity, all curcumin-DLs were superior to curcumin in solution (control). No cytotoxicity in human skin fibroblasts was detected. All DLs significantly inhibited bacterial Staphylococcus aureus and Streptococcus pyogenes growth in vitro. The curcumin-CDLs were found superior to other DLs. The incorporation of curcumin in DLs enabled both its sustained skin penetration and enhancement of its biological properties. Cationic nanocarriers enhanced the activities of curcumin to the greatest extent.



中文翻译:

脂质体增强姜黄素在多目标皮肤治疗中的生物学益处

姜黄素是一种多靶点的药理活性化合物,是一种有前途的分子,可用于治疗慢性伤口的皮肤炎症和感染。然而,其疏水性质仍然是其药物产品(包括皮肤药物)开发中的挑战。在这里,我们提出可变形脂质体(DLs)作为克服姜黄素在皮肤治疗中的局限性的手段。我们通过制备中性(NDL),阳离子(CDL)和阴离子(ADL)纳米载体,探索了具有不同表面电荷的含姜黄素的DL(curcumin-DLs)的性质和生物学效应。平均直径为200-300 nm的囊泡掺入了高姜黄素载量,反映了所用表面活性剂的类型。姜黄素-CDLs提供了最持久的离体姜黄素穿过人体全层的渗透。尽管就体外抗炎活性而言,姜黄素-CDL最有效,但所有姜黄素-DL在溶液中(对照)均优于姜黄素。在人皮肤成纤维细胞中未检测到细胞毒性。所有的DLs在体外均显着抑制细菌金黄色葡萄球菌化脓性链球菌的生长。发现姜黄素-CDL优于其他DL。姜黄素在DLs中的结合使其能够持续渗透皮肤并增强其生物学特性。阳离子纳米载体最大程度地增强了姜黄素的活性。

更新日期:2019-09-19
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