Guillot Antonio José, Jornet-Mollá Enrique, Landsberg Natalia, Milián-Guimerá Carmen, Montesinos M Carmen, Garrigues Teresa M, Melero Ana
Department of Pharmacy and Pharmaceutical Technology and Parasitology, Faculty of Pharmacy, University of Valencia, Avda. Vicent Andrés Estellés s/n, 46100 Burjassot, Spain.
Department of Pharmacology, Faculty of Pharmacy, University of Valencia, Avda. Vicent Andrés Estellés s/n, 46100 Burjassot, Spain.
Pharmaceutics. 2021 Mar 20;13(3):418. doi: 10.3390/pharmaceutics13030418.
Atopic dermatitis (AD) and psoriasis are the most common chronic inflammatory skin disorders, which importantly affect the quality of life of patients who suffer them. Among other causes, nitric oxide has been reported as part of the triggering factors in the pathogenesis of both conditions. Cyanocobalamin (vitamin B) has shown efficacy as a nitric oxide scavenger and some clinical trials have given positive outcomes in its use for treating skin pathologies. Passive skin diffusion is possible only for drugs with low molecular weights and intermediate lipophilicity. Unfortunately, the molecular weight and hydrophilicity of vitamin B do not predict its effective diffusion through the skin. The aim of this work was to design new lipid vesicles to encapsulate the vitamin B to enhance its skin penetration. Nine prototypes of vesicles were generated and characterized in terms of size, polydispersity, surface charge, drug encapsulation, flexibility, and stability with positive results. Additionally, their ability to release the drug content in a controlled manner was demonstrated. Finally, we found that these lipid vesicle formulations facilitated the penetration of cyanocobalamin to the deeper layers of the skin. The present work shows a promising system to effectively administer vitamin B topically, which could be of interest in the treatment of skin diseases such as AD and psoriasis.
特应性皮炎(AD)和银屑病是最常见的慢性炎症性皮肤病,严重影响患者的生活质量。在诸多病因中,一氧化氮被报道为这两种疾病发病机制中的触发因素之一。氰钴胺素(维生素B)已显示出作为一氧化氮清除剂的功效,一些临床试验在其用于治疗皮肤疾病方面取得了积极成果。被动皮肤扩散仅适用于低分子量和中等亲脂性的药物。不幸的是,维生素B的分子量和亲水性无法预测其通过皮肤的有效扩散情况。这项工作的目的是设计新的脂质体来包裹维生素B,以增强其皮肤渗透性。制备了九个脂质体原型,并在大小、多分散性、表面电荷、药物包封、柔韧性和稳定性方面进行了表征,结果良好。此外,还证明了它们以可控方式释放药物成分的能力。最后,我们发现这些脂质体制剂促进了氰钴胺素渗透到皮肤深层。目前的工作展示了一种有望有效局部施用维生素B的系统,这可能对治疗AD和银屑病等皮肤病具有重要意义。