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

Abstract

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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Acknowledgements

The authors acknowledge the support of the Drug Development and Innovation Centre at the University of Alberta and Applied Pharmaceutical Innovation.

Funding

Funding support was provided by Taibah University (Madinah, Saudi Arabia), Mitacs Accelerate (IT24899, Mitacs, Canada), and the Alberta Innovates Graduate Student Scholarship (Canada).

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Authors and Affiliations

Authors

Contributions

Braa Hajjar performed the experiments and collected the data. Braa Hajjar and Jieyu Zuo analyzed the data and wrote original manuscript; Chulhun Park, Shirzad Azarmi, Daniela Amaral Silva, and Nadia Araci Bou-Chacra contributed to discussion and writing—review and editing; Raimar Lobenberg contributed to conceptualization, writing—review and editing, supervision, project administration, and funding acquisition. All the authors reviewed and approved the final version of the manuscript.

Corresponding author

Correspondence to Raimar Löbenberg.

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The authors declare that this article does not contain any studies with human and animal subjects performed by any of the authors. Dr. Azarmi and Dr. Löbenberg are co-founders of RS Therapeutics Inc.

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Hajjar, B., Zuo, J., Park, C. et al. In Vitro Evaluation of a Foamable Microemulsion Towards an Improved Topical Delivery of Diclofenac Sodium. AAPS PharmSciTech 23, 102 (2022). https://doi.org/10.1208/s12249-022-02258-0

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KEY WORDS

  • topical delivery system
  • microemulsion
  • foam
  • diclofenac sodium