PDF(Pubmed)
Abstract：
UNASSIGNED: Improving the treatment of psoriasis is a serious challenge today. Psoriasis is an immune-mediated skin condition affecting 125 million people worldwide. It is commonly treated with cyclosporine-A (CsA) and dithranol (DTH). CsA suppresses the activation of T-cells, immune cells involved in forming psoriatic lesions. Meanwhile, DTH is a potent anti-inflammatory and anti-proliferative drug that effectively reduces the severity of psoriasis symptoms such as redness, scaling, and skin thickness. CsA and DTH belong to BCS class II with limited oral bioavailability. We aim to develop a drug delivery system for topical co-delivery of CsA and DTH, exploring its therapeutic potential.
UNASSIGNED: Firstly, we developed a niosomal drug delivery system based on ceramide IIIB to form Cerosomes. Cerosomes were prepared from a mixture of Ceramide, hyaluronic acid, and edge activator using a thin-film hydration technique. To co-deliver CsA and DTH topically for the treatment of psoriasis. These two hydrophobic drugs encapsulated into our synthesized positively charged particle cerosomes.
UNASSIGNED: Cerosomes had an average particle size of (222.36 nm± 0.36), polydispersity index of (0.415±0.04), Entrapment Efficiency of (96.91%± 0.56), and zeta potential of (29.36±0.38mV) for selected formula. In vitro, In silico, in vivo, permeation, and histopathology experiments have shown that cerosomes enhanced the skin penetration of both hydrophobic drugs by 66.7% compared to the CsA/DTH solution. Imiquimod (IMQ) induced psoriatic mice model was topically treated with our CsA/DTH cerosomes. We found that our formulation enhances the skin penetration of both drugs and reduces psoriasis area and severity index (PASI score) by 2.73 times and 42.85%, respectively, compared to the CsA/DTH solution. Moreover, it reduces the levels of proinflammatory cytokines, TNF-α, IL-10, and IL-6 compared to CsA/DTH solution administration.
UNASSIGNED: The Cerosomes nano-vesicle-containing CsA/DTH represents a more promising topical treatment for psoriasis, giving new hope to individuals with psoriasis, compared to commercial and other conventional alternatives.
UNASSIGNED: Firstly, we developed a niosomal drug delivery system based on ceramide IIIB to form Cerosomes. Cerosomes were prepared from a mixture of Ceramide, hyaluronic acid, and edge activator using a thin-film hydration technique. To co-deliver CsA and DTH topically for the treatment of psoriasis. These two hydrophobic drugs encapsulated into our synthesized positively charged particle cerosomes.
UNASSIGNED: Cerosomes had an average particle size of (222.36 nm± 0.36), polydispersity index of (0.415±0.04), Entrapment Efficiency of (96.91%± 0.56), and zeta potential of (29.36±0.38mV) for selected formula. In vitro, In silico, in vivo, permeation, and histopathology experiments have shown that cerosomes enhanced the skin penetration of both hydrophobic drugs by 66.7% compared to the CsA/DTH solution. Imiquimod (IMQ) induced psoriatic mice model was topically treated with our CsA/DTH cerosomes. We found that our formulation enhances the skin penetration of both drugs and reduces psoriasis area and severity index (PASI score) by 2.73 times and 42.85%, respectively, compared to the CsA/DTH solution. Moreover, it reduces the levels of proinflammatory cytokines, TNF-α, IL-10, and IL-6 compared to CsA/DTH solution administration.
UNASSIGNED: The Cerosomes nano-vesicle-containing CsA/DTH represents a more promising topical treatment for psoriasis, giving new hope to individuals with psoriasis, compared to commercial and other conventional alternatives.
摘要：
■改善牛皮癣的治疗是当今的严峻挑战。牛皮癣是一种免疫介导的皮肤病，影响全球1.25亿人。它通常用环孢菌素A(CsA)和地蒽酚(DTH)治疗。CsA抑制T细胞的活化,参与形成银屑病病变的免疫细胞。同时,DTH是一种有效的抗炎和抗增殖药物，可有效降低牛皮癣症状的严重程度，如发红，缩放，和皮肤厚度。CsA和DTH属于BCSII类,具有有限的口服生物利用度。我们的目标是开发一种用于CsA和DTH局部共递送的药物递送系统，探索其治疗潜力。
■首先，我们开发了一种基于神经酰胺IIIB的脂质体给药系统以形成Cerosome.Cerosome由神经酰胺的混合物制备，透明质酸，和边缘活化剂使用薄膜水化技术。共同局部递送CsA和DTH用于治疗银屑病。这两种疏水性药物包封到我们合成的带正电荷的颗粒cerosome中。
■Cerosome的平均粒径为（222.36nm±0.36），多分散指数为(0.415±0.04)，捕获效率（96.91%±0.56），所选配方的zeta电位为(29.36±0.38mV)。体外，在硅片中，在体内，渗透，和组织病理学实验表明，与CsA/DTH溶液相比，cerosome将两种疏水性药物的皮肤渗透增强了66.7％。用我们的CsA/DTHcerosome局部处理咪喹莫特(IMQ)诱导的银屑病小鼠模型。我们发现我们的配方可增强两种药物的皮肤渗透，并将牛皮癣面积和严重程度指数（PASI评分）降低2.73倍和42.85％，分别,与CsA/DTH解决方案相比。此外，它降低了促炎细胞因子的水平，TNF-α,IL-10和IL-6与CsA/DTH溶液施用相比。
含Cerosomes纳米囊泡的CsA/DTH代表了一种更有希望的牛皮癣局部治疗方法，给牛皮癣患者带来新的希望，与商业和其他常规替代品相比。
■首先，我们开发了一种基于神经酰胺IIIB的脂质体给药系统以形成Cerosome.Cerosome由神经酰胺的混合物制备，透明质酸，和边缘活化剂使用薄膜水化技术。共同局部递送CsA和DTH用于治疗银屑病。这两种疏水性药物包封到我们合成的带正电荷的颗粒cerosome中。
■Cerosome的平均粒径为（222.36nm±0.36），多分散指数为(0.415±0.04)，捕获效率（96.91%±0.56），所选配方的zeta电位为(29.36±0.38mV)。体外，在硅片中，在体内，渗透，和组织病理学实验表明，与CsA/DTH溶液相比，cerosome将两种疏水性药物的皮肤渗透增强了66.7％。用我们的CsA/DTHcerosome局部处理咪喹莫特(IMQ)诱导的银屑病小鼠模型。我们发现我们的配方可增强两种药物的皮肤渗透，并将牛皮癣面积和严重程度指数（PASI评分）降低2.73倍和42.85％，分别,与CsA/DTH解决方案相比。此外，它降低了促炎细胞因子的水平，TNF-α,IL-10和IL-6与CsA/DTH溶液施用相比。
含Cerosomes纳米囊泡的CsA/DTH代表了一种更有希望的牛皮癣局部治疗方法，给牛皮癣患者带来新的希望，与商业和其他常规替代品相比。
