一种用于痤疮治疗的新型水凝胶增稠氨苯砜微乳:开发、表征、理化稳定性和体外渗透研究

Lida Beheshti-Mall, H. Shafaroodi, Zahra Jafariazar, M. Afshar
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引用次数: 5

摘要

寻常痤疮是一种常见的炎症性皮肤状况,已被重新归类为慢性疾病。近年来,局部痤疮治疗的范围大大扩大,各种局部药物包括局部氨苯砜都是可用的。氨苯砜具有特殊的物理化学性质,使其局部配方具有挑战性。本研究的目的是制备一种水凝胶增稠微乳剂作为氨苯砜的局部给药系统。制备了以氨苯砜(5%)、肉豆酸异丙酯、吐温80、二甘醇单乙醚、乙醇和水为主要原料的微乳。用卡波姆940对最佳微乳液进行改性。考察了优化制剂的滴度、pH、折射率、电导率、流变性以及对大鼠皮肤的透皮性。与对照凝胶相比,优化后的配方显著提高了氨苯砜的透皮性。虽然薄荷醇的加入增加了粒径,但薄荷醇(5%)微乳的通量是对照的2.51倍。然而,该药物的皮肤吸收率低于3%。六个月的加速研究证明了微凝胶的物理化学稳定性。本研究结果表明,基于薄荷醇的水凝胶增稠微乳液体系可能是一种很有前途的局部给药载体。
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A novel hydrogel-thickened microemulsion of dapsone for acne treatment: Development, characterization, physicochemical stability and ex vivo permeation studies
Acne vulgaris is a common inflammatory skin condition, which has been reclassified as a chronic disease. The spectrum of topical acne treatments has expanded substantially in recent years and various topical medications including topical dapsone are available. Dapsone has special physicochemical properties that make its topical formulation challenging. The aim of this study was preparing a hydrogelthickened microemulsion as a topical delivery system for dapsone. The microemulsions composed of dapsone (5%), isopropyl myristate, tween 80, diethylene glycol monoethyl ether, ethanol and water were prepared. The optimum microemulsion was modified with carbomer 940. Droplet size, pH, refractive index, conductivity, rheology of the optimized formulation, and skin permeation of dapsone through rat skin were evaluated. The optimized formulation significantly increased the skin permeation of dapsone in comparison to that of control gel. Although incorporation of menthol increased the particle size, the flux of microemulgel consisting of menthol (5%) was 2.51 times higher than that of the control. However, the skin absorption of the drug was less than 3%. Six month accelerated studies proved the physicochemical stability of microemulgels. The results of this research indicate that menthol based hydrogelthickened microemulsion system could be a promising vehicle for topical delivery of dapsone.
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