Maliba Pharmacy College, Uka Tarsadia University, Surat, 394350, India.
Maliba Pharmacy College, Uka Tarsadia University, Surat, 394350, India.
Colloids Surf B Biointerfaces. 2020 Feb;186:110681. doi: 10.1016/j.colsurfb.2019.110681. Epub 2019 Nov 28.
Psoriasis is a widespread chronic disease affecting 1-3 % of total population. In major cases (>80 %), it is treated by topical application of corticosteroids. However, the topical route is very challenging due to physico-chemical nature of diseased stratum corneum and so no single treatment works for every patient. The oral route showed severe side effects due to systemic immunosuppression, which can be avoided by topical route. The aim of the research work was to investigate cyclosporine loaded microemulsion based gel for effective cyclosporine permeation and retention in the skin tissue for psoriasis treatment. The pseudo ternary phase diagram at three S ratios (2:1, 1:1, and 1:2; Tween 80: isopropyl alcohol) were constructed using isopropyl myristate as oil phase. The S at 2:1 ratio showed large microemulsion area. The transmission electron microscope images showed spherical non-aggregated oil globules with the size < 50 nm. The selected microemulsion (Cy-2-ME12O55SM) was incorporated in Carbopol 940 gel for topical application. The ex vivo diffusion study showed improved permeation (>24 h) with microemulsion-gel in comparison to cyclosporine suspension. The microemulsion-gel was non-irritating on the rabbit skin. In drug retention studies, microemulsion-gel showed high drug retention (trapping, 38.92 %) in the skin tissue, which was due to destabilization of microemulsion after penetration in the skin layer causing precipitation of cyclosporine. The depot effect due to cyclosporine precipitates could be helpful for sustained effect of cyclosporine for the effective treatment of psoriasis.
银屑病是一种广泛存在的慢性疾病,影响总人口的 1-3%。在大多数情况下(>80%),它通过局部应用皮质类固醇来治疗。然而,由于病变角质层的物理化学性质,局部途径非常具有挑战性,因此没有单一的治疗方法适用于每个患者。口服途径由于全身免疫抑制而显示出严重的副作用,这可以通过局部途径避免。本研究工作的目的是研究环孢素负载微乳凝胶,以有效渗透和保留环孢素在皮肤组织中,用于治疗银屑病。使用肉豆蔻酸异丙酯作为油相,在三个 S 比(2:1、1:1 和 1:2;吐温 80:异丙醇)下构建伪三元相图。S 比为 2:1 时显示出较大的微乳液区域。透射电子显微镜图像显示,油滴呈球形且无聚集,粒径<50nm。选择微乳液(Cy-2-ME12O55SM)掺入卡波姆 940 凝胶中用于局部应用。离体扩散研究表明,与环孢素混悬液相比,微乳凝胶具有更好的渗透效果(>24h)。微乳凝胶对兔皮无刺激性。在药物保留研究中,微乳凝胶显示出高药物保留(滞留,38.92%)在皮肤组织中,这是由于微乳液在渗透到皮肤层后失稳导致环孢素沉淀。由于环孢素沉淀而产生的储库效应可能有助于环孢素的持续作用,从而有效治疗银屑病。