Fingolimod Hydrochloride Gel for Dermatological Applications: Optimization of Formulation Strength and Effect of Colloidal Oatmeal (Aveeno®) as Penetration Enhancer

作者: M. Tamakuwala , G. Stagni

DOI: 10.1208/S12249-015-0415-9

关键词: Fingolimod HydrochlorideHydroxypropyl cellulosePermeability (electromagnetism)PermeationChromatographyStratum corneumAtopic dermatitisPsoriasisChemistryDermis

摘要: Fingolimod (FNGL) is an immune-modulatory agent prescribed for relapsing forms of multiple sclerosis. Because its mechanism action, FNGL potentially a treatment chronic, non-curable T-lymphocyte-driven inflammatory skin diseases (TLDISD) such as psoriasis and atopic dermatitis. Since severe side effects limit the systemic administration FNGL, objective this study to develop hydroxypropyl cellulose (2%) gel dermatological applications. First, effect strength (0.05%, 0.10%, 0.50%, 1.00%) on permeability retention was investigated. We carried out several permeation studies with vertical Franz diffusion cells (i) or (ii) excised dorsal porcine ear (EDPES) membrane. also quantified in stratum corneum dermis tape-stripping method. Permeability parameters well amount retained increased significantly (p < 0.01) strength; however, there no statistically significant difference between 0.50% 1.00% gels both EDPES. Therefore, we selected investigate colloidal oatmeal (0%, 1%, 3%, 6%, 10%) vitro retention. Colloidal has beneficial properties TLDISD may complement activity. (p < 0.001) at 6% 10% enhancement ratio 3.5 2.4, respectively, whereas decreased compared base gel. In conclusion, FNGL.HCL Aveeno® very promising characteristics delivery skin.

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