Formulation and in vitro evaluation of ufasomes for dermal administration of methotrexate.

Arvind Sharma, Sandeep Arora
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引用次数: 42

Abstract

Dermal drug delivery system that is required to localizes methotrexate (MTX) in the synovial joint is needed to treat inflammation in rheumatoid arthritis (RA). The present investigation aims at exploring the potential of fatty acid vesicles for the topical delivery of methotrexate. Vesicles were prepared by film hydration method using oleic acid as a fatty acid principal component. Developed vesicles were characterized for size, size distribution, shape, in vitro release, pH dependent, and storage stability. Interaction between MTX and oleic acid was investigated using differential scanning calorimetry. The MTX amount permeated through rat skin was three- to fourfold higher using oleic acid compared to those from plain drug solution or carbopol gel. At the end of the skin permeation assay using ufasomes, up to 50% of the administered dose was found in the skin. These results suggest that methotrexate encapsulated in oleic acid vesicles may be of value for the topical administration of MTX in the treatment of psoriasis.

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甲氨蝶呤皮肤给药用异速体的配方及体外评价。
类风湿性关节炎(RA)的炎症治疗需要皮肤给药系统来定位滑膜关节中的甲氨蝶呤(MTX)。本研究旨在探索脂肪酸囊泡局部递送甲氨蝶呤的潜力。以油酸为主要脂肪酸组分,采用膜水化法制备了囊泡。发育囊泡的大小,大小分布,形状,体外释放,pH依赖性和储存稳定性表征。用差示扫描量热法研究了MTX与油酸的相互作用。通过大鼠皮肤渗透的MTX量使用油酸比使用普通药物溶液或卡波醇凝胶高三到四倍。在使用ufasomes进行皮肤渗透试验结束时,在皮肤中发现了高达50%的给药剂量。这些结果表明,油酸囊泡中包裹的甲氨蝶呤可能对局部给药MTX治疗牛皮癣有价值。
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