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Abstract

In recent years, ethosomes have been employed extensively as a transdermal drug delivery system due to their improved bioavailability, modified release characteristics, and compatibility as compared to topical formulations that are currently accessible. Because of their enhanced bioavailability, altered release properties, and compatibility with currently available topical formulations, ethosomes have been widely used as a transdermal drug delivery system in recent years.In this study, the cold technique was used to prepare fluconazole-entrapped ethosomes for topical administration.Size, percentage entrapment, pH, viscosity, in vitro drug release study, and interaction study were assessed for the prepared ethosome formulation.The optimal formulation was selected based on its size, entrapment effectiveness, and release profile. The findings of measuring the viscosity and pH of the fluconazole ethosomes trapped in gel were satisfactory, confirming that ethosomes could be an effective carrier for fluconazole topical delivery.

Keywords

Fluconazole, Ethosomes, Fungal infection, Phospholipid

Introduction

Inhibiting ergosterol synthesis, a crucial component of fungal cell membranes, results in membrane disruption and fungal cell death. Fluconazole is a broad-spectrum antifungal medication that belongs to the triazole class and is commonly used to treat superficial fungal infections, including dermatophytosis, tinea infections, and candidiasis. The fungal cytochrome P450-dependent enzyme lanosterol 14-α-demethylase, which is necessary for the synthesis of ergosterol, a key structural element of the fungal cell membrane, is selectively inhibited by fluconazole. Blocking this enzyme prevents lanosterol from being converted to ergosterol, which results in an excess of ergosterol and the buildup of toxic, aberrant sterols inside the fungal cell. The cell membrane thus becomes weak and porous, making it difficult to sustain regular processes like growth and permeability control. In the end, this disruption results in the organism's death and prevention of fungal cell reproduction. Crucially, fluconazole is a safe and efficient antifungal drug due to its excellent selectivity for fungal enzymes and negligible impact on human sterol production. Worldwide, the prevalence of fungal infections of the skin, hair, and nails has increased. A fungal infection can spread quickly and seriously. Numerous fungal species, particularly Candida albicans, are the primary cause of fungal infections. These species thrive and spread on the skin's surface, causing symptoms such skin thickening, reddening, and itching. Transdermal medication delivery systems can treat important problems like vaginal infections and skin infections like onchocytosis. Most often, topical semisolid dose forms are used to treat fungal infections on the skin in order to prevent the GIT irritations, either systemic or otherwise. Targeting the infection site, reducing systemic side effects, and achieving high patient compliance are just a few advantages of topical treatment for fungal infections. Various topical antifungal compounds have been used to treat a variety of skin infections, but they are unable to deeply penetrate the stratum corneum layer and instead remain there, making this system a complete failure. The skin serves as both a major target and a barrier for the delivery of topical drugs. An inventive method for the topical administration of fluconazole is the use of ethosomal solutions filled with the drug. Phospholipids, ethanol, and water make up ethersomes, which are vesicular transporters. These formulations are intended to improve the drug's ability to pass through the skin, delivering a precise and regulated release of the active ingredient right at the infection site.

Skin:

The primary components of skin are skin layers, which are made up of small wrinkles, hairs, and lipids on the skin's outermost surface. Additional components of skin include skin layers. The optical behaviors of these components vary greatly depending on their structural makeup.

Skin layers:

The most versatile and broad route for topical and systemic drug administration is the skin. When applied topically, the stratum corneum, the skin's outermost layer, limits the bioavailability of medications by acting as the skin's strongest barrier to drug penetration.

Reference

  1. Roshni Dhurve Ashwani Mishra Formulation and Evaluation Of Ethosomal Gel Of Fluconazole For Topical Drug Delivery International Journal on Current Trends in Drug Development & Industrial Pharmacy Vol. 3, Issue 1 – 2019
  2. Tejashree A. Ghadge, A.S. Kulkarni S.H. Majumdar, SD Chavare Ethosome: A Promising Approach for Antifungal Drug Delivery Research J. Topical and Cosmetic Sci 6(1): Jan. - June 2015
  3. Sahishta Khan, BK Dubey, GK Pandey, Amit Jain, Suresh Dhakar, Prabhat Kumar Jain, Formulation and Evaluation of Ethosomal Gel of Ciprofloxacin for Bacterial Infections, National Journal of Advanced Research Volume 5: Issue 2: April 2019: Page No. 21-25.
  4. Priyanka Parmar, Ashwani Mishra and Anupam Pathak Preparation and Evaluation of Ethosomal Gel of Clotrimazole for Fungal Infection by Mechanical Dispersion Method journal of Current Research in Pharmaceutical Sciences 2016: 06 (02) 45-49.
  5. Arjun Gaire B.Pharma, Sangit Maharjan B.Pharmb, Sumitra Shrestha M.Pharm, Sonu Pakhrin M.Pharmd, Naresh Thapa B.Pharma, Dr. Jeevan Raj Shrestha, Mrs. Bijaya Laxmi Giri M.Pharm Formulation & Evaluation of Fluconazole Gel for Topical Drug Delivery System American Scientific Research Journal for Engineering. Technology, and Sciences (ASRJETS).
  6. V. Sankar, V. Wilson, K. Siram, A. Karuppaiah, S. Hariharan, A. Justin (2019) Topical Delivery of Drugs Using Ethosomes: A review. Indian Drugs, 56(8), 7-14.
  7. Baghli, F., Khaoua, R., Guenifed, I., & Moussaoui-Khedam, N. (2024). Effect of formulation parameters on the characteristics of binary ethosomes loaded with Fluconazole. Magna Scientia Advanced Biology and Pharmacy, 13(02), 007–016.
  8. Huanbutta, K., Rattanachitthawat, N., Luangpraditkun, K., Sriamornsak, P., Puri, V., Singh, I., & Sangnim, T. (2022). Development and Evaluation of Ethosomes Loaded with Zingiber zerumbet Linn Rhizome Extract for Antifungal Skin Infection in Deep Layer Skin. Pharmaceutics, 14, 2765.
  9. Joshi, P., Tyagi, Y., Negi, A., & Ashok, P. K. (2022). Design, development and evaluation of ethosomal gel of fluconazole for topical fungal infection. Journal of Emerging Technologies and Innovative Research (JETIR), 9(9), 510–516.
  10. Agarwal, S., & Gautam, G. (2020). Formulation, development and evaluation of atorvastatin ethosomal gel. International Journal of Pharmaceutical Investigation, 10(4), 452–455.
  11. Chauhan, N., Vasava, P., Khan, S.L., et al. Ethosomes: A Novel Drug Carrier, 2021/2022.
  12. Halagali, P., Wannur, V.I., Patil, A.A., et al. Formulation and Evaluation of Quercetin Ethosomal Hydrogel for Topical Delivery System, 2023/2024.
  13. Gaire, A., Maharjan, S., Shrestha, S., Pakhrin, S., Thapa, N., Shrestha, J. R., & Giri, B. L. (n.d.). Formulation and evaluation of fluconazole gel for topical drug delivery system. American Scientific Research Journal for Engineering, Technology, and Sciences (ASRJETS).
  14. Jadhav, P.U., Gujare, S.G., Shende, M.A. Ethosomes: A Novel Tool for Vesicular Drug Delivery, Pre-2020.
  15. Indora, N., & Kaushik, D. (2015). Design, development and evaluation of ethosomal gel of fluconazole for topical fungal infection. International Journal of Engineering Science Invention Research & Development, 1(8), 280–286.
  16. Jain, N., Sharma, A., & Srivastava, A. K. (2024). Preparation and characterization of ethosomal gel drug delivery: A comprehensive review. Journal of Biomedical and Pharmaceutical Research, 13(6), 79–84.
  17. Dave, V., Kumar, D., Lewis, S., & Paliwal, S. (2010). Ethosome for enhanced transdermal drug delivery of aceclofenac. International Journal of Drug Delivery, 2, 81–92.
  18. Anju, K., Priya, S., Sandeep, D. S., Nayak, P., Kumar, P., Kumar, A., Lobo, C. L., & Krith, S. P. (2021). Formulation and optimization of zaltoprofen loaded ethosomal gel by using 2³ full factorial designs. Journal of Pharmaceutical Research International, 33(24B), 30–44 19] Supraja, R., & Sailaja, A. K. (2017). Formulation of mefenamic acid loaded ethosomal gel by hot and cold methods. Nano Biomedicine and Engineering, 9(1), 27–35.
  19. Supraja, R., & Sailaja, A. K. (2017). Formulation of mefenamic acid loaded ethosomal gel by hot and cold methods. Nano Biomedicine and Engineering, 9(1), 27–35.
  20. Jain, S., Tiwary, A. K., Sapra, B., & Jain, N. K. (2007). Formulation and evaluation of ethosomes for transdermal delivery of lamivudine. AAPS PharmSciTech, 8(4), Article 111.

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Suvarna Sangale
Corresponding author

RJS College of Pharmacy Kokamthan

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Vaishnavi Dhage
Co-author

RJS College of Pharmacy Kokamthan

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Snehal Gondkar
Co-author

RJS College of Pharmacy Kokamthan

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Tanvir Pathan
Co-author

RJS College of Pharmacy Kokamthan

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Prerana Jamdhade
Co-author

RJS College of Pharmacy Kokamthan

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Gursal Kanchan
Co-author

RJS College of Pharmacy Kokamthan

Suvarna Sangale*, Vaishnavi Dhage, Snehal Gondkar, Tanvir Pathan, Prerana Jamdhade, Gursal Kanchan, Formulation and Evaluation of Fluconazole Loaded Ethosomes for Topical Drug Delivery, Int. J. Sci. R. Tech., 2026, 3 (3), 1-10. https://doi.org/10.5281/zenodo.18851378

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