Beirampour Negar, Mallandrich Mireia, Bustos-Salgado Paola, Domínguez-Villegas Valeri, Garrós Núria, Mohammadi-Meyabadi Roya, Clares-Naveros Beatriz, Romero-Olid Maria Nuria, Pérez-Cano Francisco J, Girbal Marina, Rodríguez-Lagunas Maria José, Suñer-Carbó Joaquim, Calpena Ana Cristina
Departament de Farmàcia i Tecnologia Farmacèutica, i Fisicoquímica, Facultat de Farmàcia i Ciències de l'Alimentació, Universitat de Barcelona, Av. Joan XXIII 27-31, 08028 Barcelona, Spain.
Institut de Nanociència i Nanotecnologia, Universitat de Barcelona (UB), 08028 Barcelona, Spain.
Pharmaceutics. 2025 Apr 5;17(4):475. doi: 10.3390/pharmaceutics17040475.
Alopecia areata is an autoimmune disorder that causes hair loss in clumps about the size and shape of a quarter. The estimated prevalence of the disorder is approximately 1 in 1000 people, with a lifetime risk of approximately 2 percent. One of the systemic therapies for alopecia areata consists of the use of glucocorticoids or immunosuppressants. Baricitinib (BCT) is a Janus kinase (JAK) 1 and 2 selective inhibitor used as an immunosuppressant drug. In this study, three olive oil BCT formulations (Oil A, Oil B, and Oil C, which differ in their content in squalene, tocopherol, tyrosol, and hydroxytyrosol) have been developed for topical delivery. The formulations were physicochemically characterized and the in vitro drug release and ex vivo permeation through human skin tissues were assessed. The results showed nearly identical viscosity across all three formulations, exhibiting Newtonian behavior. The mathematical modeling used to describe the drug release profiles was the one-site binding hyperbola for all formulations. Oil-based formulations showed a slow BCT penetration into human skin. Skin integrity remained intact during the experiments, with no signs of irritation or alterations observed. In addition, all the formulations proved their efficacy in vivo. Among the formulations, Oil A demonstrated the highest ability retention capacity ( = 1875 ± 124.32 ng/cm) in the skin, making it an excellent candidate for further investigation in the treatment of alopecia areata.
斑秃是一种自身免疫性疾病，会导致头发成簇脱落，脱落区域大小和形状约为25美分硬币。该疾病的估计患病率约为千分之一，终生患病风险约为2%。斑秃的全身治疗方法之一是使用糖皮质激素或免疫抑制剂。巴瑞替尼（BCT）是一种用作免疫抑制药物的Janus激酶（JAK）1和2选择性抑制剂。在本研究中，已开发出三种橄榄油BCT制剂（油A、油B和油C，它们在角鲨烯、生育酚、酪醇和羟基酪醇的含量上有所不同）用于局部给药。对这些制剂进行了物理化学表征，并评估了其体外药物释放和通过人体皮肤组织的离体渗透情况。结果显示，所有三种制剂的粘度几乎相同，呈现牛顿流体行为。用于描述药物释放曲线的数学模型对所有制剂均为单点结合双曲线。油基制剂显示出巴瑞替尼向人体皮肤的缓慢渗透。在实验过程中皮肤完整性保持完好，未观察到刺激或改变的迹象。此外，所有制剂在体内均证明了其有效性。在这些制剂中，油A在皮肤中的保留能力最高（=1875±124.32纳克/平方厘米），使其成为进一步研究治疗斑秃的优秀候选药物。
