Department of Pharmaceutics, National Institute of Pharmaceutical Education and Research (NIPER), Hyderabad 500037, India.
Department of Pharmaceutics, National Institute of Pharmaceutical Education and Research (NIPER), Hyderabad 500037, India.
J Photochem Photobiol B. 2017 Sep;174:44-57. doi: 10.1016/j.jphotobiol.2017.07.007. Epub 2017 Jul 12.
Vitiligo is a de-pigmenting skin disorder characterized by white patches on skin due to partial or complete loss of melanocytes. Psoralen in combination with ultraviolet-A (PUVA) acts by stimulation of melanin content and tyrosinase activity in melanocytes. Resveratrol, a sirtuin activator and a potential anti-oxidant reduce oxidative stress which is one of the triggering factors for initiation of vitiligo. Despite their therapeutic activity, weak percutaneous permeability of psoralen and poor solubility of resveratrol hinders their effective topical administration. The aim of present study is to formulate ultradeformable liposomes (UDL) co-loaded with psoralen and resveratrol for evaluation of PUVA and anti-oxidant combination in vitiligo treatment. For this purpose, UDL composed of DC-Chol, cholesterol and sodium deoxy cholate were prepared for their co-delivery. Liposomal carriers were characterized and evaluated for their efficacy using B16F10 cell line. Free radical scavenging potential was also determined for these carriers by in vitro anti-oxidant assays. Optimal co-loaded UDL with particle size ranging from 120 to 130nm, zeta potential of +46.2mV, entrapment efficiency of 74.09% (psoralen) and 76.91% (resveratrol) were obtained. Compared to control, co-loaded UDL showed significant stimulation of melanin and tyrosinase activity with major contribution of psoralen. Further, co-loaded UDL also exhibited potential free radical scavenging activity where resveratrol played a key role. Hence, psoralen and resveratrol co-loaded UDL acts in vitiligo through dual mechanisms of action viz., stimulation of melanin and tyrosinase activity as well as by anti-oxidant activity. These findings indicate that psoralen and resveratrol co-loaded UDL has the promising therapeutic potential for the treatment of vitiligo.
白癜风是一种色素脱失性皮肤病,其特征是皮肤出现白色斑块,这是由于黑色素细胞部分或完全丧失所致。补骨脂素与紫外线 A(PUVA)联合作用通过刺激黑色素细胞中的黑色素含量和酪氨酸酶活性来发挥作用。白藜芦醇是一种组蛋白去乙酰化酶激活剂和潜在的抗氧化剂,可以减少氧化应激,氧化应激是白癜风发病的触发因素之一。尽管补骨脂素和白藜芦醇具有治疗活性,但它们的经皮渗透性弱且溶解度差,这阻碍了它们的有效局部给药。本研究的目的是制备共载有补骨脂素和白藜芦醇的超变形脂质体(UDL),以评估 PUVA 和抗氧化剂联合治疗白癜风的效果。为此,制备了由 DC-Chol、胆固醇和脱氧胆酸钠组成的 UDL 以实现共递药。对脂质体载体进行了表征和评估,并使用 B16F10 细胞系评估其功效。还通过体外抗氧化测定法确定了这些载体的自由基清除潜力。获得了粒径范围为 120-130nm、表面电势为+46.2mV、包封效率分别为 74.09%(补骨脂素)和 76.91%(白藜芦醇)的最佳共载 UDL。与对照组相比,共载 UDL 显著刺激黑色素和酪氨酸酶活性,这主要得益于补骨脂素。此外,共载 UDL 还表现出潜在的自由基清除活性,其中白藜芦醇发挥了关键作用。因此,共载有补骨脂素和白藜芦醇的 UDL 通过刺激黑色素和酪氨酸酶活性以及抗氧化活性的双重作用作用于白癜风。这些发现表明,共载有补骨脂素和白藜芦醇的 UDL 具有治疗白癜风的潜在治疗潜力。