In Vitro Evaluation of a Foamable Microemulsion Towards an Improved Topical Delivery of Diclofenac Sodium

透皮 Zeta电位 微乳液 双氯芬酸钠 角质层 粒径 色谱法 溶解度 化学 活性成分 材料科学 化学工程 生物医学工程 纳米技术 药理学 肺表面活性物质 有机化学 纳米颗粒 医学 生物化学 物理化学 病理 工程类
作者
Baraa Hajjar,Jieyu Zuo,Chulhun Park,Shirzad Azarmi,Daniela Amaral Silva,Nádia Araci Bou‐Chacra,Raimar Löbenberg
出处
期刊:Aaps Pharmscitech [Springer Science+Business Media]
卷期号:23 (4) 被引量:6
标识
DOI:10.1208/s12249-022-02258-0
摘要

Topical microemulsion (ME) might provide a novel and advanced transdermal delivery system due to the enhances of drug solubility and permeability across the stratum corneum. Foams are topical delivery systems that have excellent patient compliance, acceptability, and preference. Therefore, this study aimed to investigate a foamable microemulsion as an alternative topical and transdermal dosage form for diclofenac sodium (DS). The physicochemical properties (optical clarity, percentage transmittance, homogeneity, consistency of formulation, particle size, zeta potential, conductivity, viscosity, and morphology, etc.) of the DS-loaded ME were investigated. The foam stability of both drug-free ME and DS-loaded ME was measured. The foam quality was evaluated, and the chemical stability over 90 days was determined. Franz diffusion cells were employed to assess the in vitro drug release of a foamed DS-loaded ME and compared with a commercial topical product. A foamable and stable DS-loaded ME that maintained small particle sizes and constant zeta potential and was transparent and translucent in appearance after 90 days was successfully produced. The foam of the DS-loaded ME was physically more stable compared to the drug-free foam. The foam had an increased drug release rate compared to the commercial product. The foamable DS-loaded ME has a great potential to enhance the transdermal delivery of DS after topical administration. Foamed DS-loaded ME is a promising alternative to the current topical formulation of DS.
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