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Thyme Oil–Containing Fluconazole-Loaded Transferosomal Bigel for Transdermal Delivery

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Abstract

The objective of the present research was to develop fluconazole-loaded transferosomal bigels for transdermal delivery by employing statistical optimization (23 factorial design–based). Thin-film hydration was employed to prepare fluconazole-loaded transferomal suspensions, which were then incorporated into bigel system. A 23 factorial design was employed where ratios of lipids to edge activators, lipids (soya lecithin to cholesterol), and edge activators (sodium deoxycholate to Tween 80) were factors. Ex vivo permeation flux (Jss) of transferosomal bigels across porcine skin was analyzed as response. The optimal setting for optimized formulation (FO) was A= 4.96, B= 3.82, and C= 2.16. The optimized transferosomes showed 52.38 ± 1.76% DEE, 76.37 nm vesicle size, 0.233 PDI, − 20.3 mV zeta potential, and desirable deformability. TEM of optimized transferosomes exhibited a multilamelar structure. FO bigel’s FE-SEM revealed a globule-shaped vesicular structure. Further, the optimized transferosomal suspension was incorporated into thyme oil (0.1% w/w)–containing bigel (TO-FO). Ex vivo transdermal fluconazole permeation from different transferosomal bigels was sustained over 24 h. The highest permeation flux (4.101 μg/cm2/h) was estimated for TO-FO bigel. TO-FO bigel presented 1.67-fold more increments of antifungal activity against Candida albicans than FO bigel. The prepared thyme oil (0.1% w/w)–containing transfersomal bigel formulations can be used as topical delivery system to treat candida related fungal infections.

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Acknowledgements

The authors are thankful to the President, Siksha ‘O' Anusandhan (Deemed to be University), Bhubaneswar 751030, Odisha, India.

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Authors and Affiliations

  1. Department of Pharmaceutics, Seemanta Institute of Pharmaceutical Sciences, Mayurbhanj, Jharpokharia, Odisha, 757086, India

    Biswarup Das

  2. Department of Pharmaceutics, School of Pharmaceutical Sciences, Siksha ‘O’ Anusandhan (Deemed to be University), Bhubaneswar, Odisha, 751003, India

    Biswarup Das, Amit Kumar Nayak & Subrata Mallick

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  1. Biswarup Das
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B. D.: conceptualization, investigation, methodology, data curation, writing—original draft; A. K. N.: supervision, methodology, formal analysis, validation, discussion, review; S. M.: supervision, review, and editing.

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Correspondence to Amit Kumar Nayak or Subrata Mallick.

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Das, B., Nayak, A.K. & Mallick, S. Thyme Oil–Containing Fluconazole-Loaded Transferosomal Bigel for Transdermal Delivery. AAPS PharmSciTech 24, 240 (2023). https://doi.org/10.1208/s12249-023-02698-2

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