Formulation and evaluation of a tipical preparation containing Roflumilast

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Psoriasis is a chronic, proliferative, inflammatory dermatologic disease that accelerates the skin cell proliferation rate from 26-28 days to 3-4 days, resulting in increased skin thickness and cutaneous plaques. Its symptoms are red lesions with white scales and silver colored flakes, accompanied by a burning sensation and pruritus. The most common type of psoriasis is Plaque Psoriasis; topical agents are also the best therapeutic approach in the case of Mild-to-Moderate Plaque Psoriasis. Roflumilast is a selective phosphodiesterase-4 (PDE-4) inhibitor that was approved as a topical agent in the case of mild-to-moderate plaque psoriasis by the U.S. Food and Drug Administration (FDA). Its mechanism of action in this skin disease is not yet fully understood, but it likely provides anti-inflammatory effects. This paper aimed to formulate and evaluate a nanogel containing Roflumilast. Two gel compositions were prepared with and without hydroxypropyl-beta-cyclodextrin (HPBCD). Physicochemical characterization included pH measurement, rheological analysis, particle size analysis, and in vitro drug-release studies. Both nanogels showed acceptable values in the case of pH measurements. Rheology analysis confirmed shear-thinning behavior, which is favorable for topical preparations. Particle size analysis demonstrated smaller values for the nanogel containing Roflumilast and HPBCD compared to the nanogel containing Roflumilast. An in-vitro drug release study indicated higher drug release in the case of the nanogel containing Roflumilast and HPBCD. In conclusion, Roflumilast nanogels were successfully formulated and showed suitable physicochemical properties for topical use. The incorporation of HPBCD increased the solubility of Roflumilast in Tween 80, reduced particle size, and enhanced drug release.

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Kulcsszavak
Roflumilast, Nanogel, Nanogel preparation, Plaque psoriasis, Hydroxypropyl-beta-cyclodextrin (HPBCD), Topical drug delivery, Particel size analysis, Rheology analysis, In vitro drug release
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