Research Article

Naltrexone Hydrochloride Loaded W/O Microemulsions: Preparation, Characterization and Exploring the Anti-leishmanial Activity

Volume: 55 Number: 2 September 23, 2025

Naltrexone Hydrochloride Loaded W/O Microemulsions: Preparation, Characterization and Exploring the Anti-leishmanial Activity

Abstract

Background and Aims: This study investigated the potential of naltrexone hydrochloride (NH) loaded water-in-oil (W/O) microemulsions (ME) as an alternative treatment strategy for cutaneous leishmaniasis caused by Leishmania tropica. This study aims to provide a topical alternative to the treatment of leishmaniasis, while also identifying a new therapeutic use of naltrexone other than its use in opioid addiction. Methods: Stable water-in-oil microemulsion formulations were developed using linseed oil, Span 60®, and polyethylene glycol 400. Microemulsions were prepared using triangle phase diagrams and optimization was performed by determining the droplet size, viscosity, pH, conductivity, and zeta potential values. The antileishmanial activity of the optimized microemulsion formulation was tested under in vitro conditions. Results: The optimized formulation (ME-2) demonstrated favorable physicochemical properties, including a droplet size of 99.86 nm, low polydispersity index (0.242), and high zeta potential (-42.9 mV), ensuring stability and homogeneity. In vitro release studies indicated first-order kinetics, suggesting the controlled release of NH. The antileishmanial activity of ME-2 was evaluated against L. tropica promastigote, revealing a 50% inhibition at an IC50 concentration of 5.17 µM. While amphotericin B, the gold standard, exhibited superior efficacy (IC50 = 0.063 µM), NH demonstrated a dose-dependent reduction in promastigote viability. This suggests its potential as a supplementary treatment, particularly in cases where amphotericin B's toxicity is a concern. Conclusion: Future studies focusing on structural optimization, mechanism elucidation, and in vivo validation could enhance NH’s efficacy, offering a promising alternative for leishmaniasis management. This work establishes a foundational basis for leveraging NH microemulsions in parasitic disease therapy.

Keywords

References

  1. Abd Sisak, M.A., Daik, R., & Ramli, S. (2017). Study on the effect of oil phase and co-surfactant on microemulsion systems. Malaysian Journal of Analytical Sciences, 21:1409-1416. google scholar
  2. Al-Mohaimeed, A.M., Mostafa, G.A., & El-Tohamy, M.F. (2021). New construction of functionalized CuO/Al2O3 nanocomposite-based polymeric sensor for potentiometric estimation of naltrexone hydrochloride in commercial formulations. Polymers, 13(24), 4459. google scholar
  3. Arya, R., Dhembla, C., Makde, R.D., Sundd, M., & Kundu, S. (2021). An overview of the fatty acid biosynthesis in the protozoan parasite leishmania and its relevance as a drug target against leishmaniasis. Molecular and Biochemical Parasitol- ogy. 246, 111416. Available from: http://www.eurosurveillance.org/ViewArticle. aspx?ArticleId=20533 google scholar
  4. Chang, L., Pope, G.A., Jang, S.H., & Tagavifar, M. (2019). Prediction of microemulsion phase behavior from surfactant and co-solvent structures. Fuel., 237, 494-514. google scholar
  5. Choubey, A., Dehury, B., Kumar, S., Medhi, B., & Mondal, P. (2022). Naltrexone a potential therapeutic candidate for COVID-19. Journal of Biomolecular Structure and Dynamics, 40(3), 963-970. google scholar
  6. da Silva, S.S.S., de Andrade, A.F., de Paiva-Cavalcanti, M., de Carvalho, J.C.M., de Araújo Viana-Marques, D., Porto, A.L.F., & Bezerra, R.P. (2023). Potential of bioactive molecules from photosynthetic microorganisms on Leishmania spp.: A review. Algal Research, 103241. google scholar
  7. de Vries, H.J., & Schallig, H.D. (2022). Cutaneous leishmaniasis: a 2022 updated narrative review into diagnosis and management developments. American Journal of Clinical Dermatology, 23(6), 823-840. google scholar
  8. Eser, M., & Çavuş, İ. (2023). In vitro and in silico evaluations of the antileishmanial activities of new benzimidazole-triazole derivatives. Veterinary Sciences and Practices, 10: 648. google scholar

Details

Primary Language

English

Subjects

Clinical Pharmacology and Therapeutics

Journal Section

Research Article

Early Pub Date

September 23, 2025

Publication Date

September 23, 2025

Submission Date

February 7, 2025

Acceptance Date

May 8, 2025

Published in Issue

Year 2025 Volume: 55 Number: 2

APA
Özyılmaz, E. D., Güler, E., Süer, K., Özbilgin, A., Çavuş, İ., & Çomoğlu, T. (2025). Naltrexone Hydrochloride Loaded W/O Microemulsions: Preparation, Characterization and Exploring the Anti-leishmanial Activity. İstanbul Journal of Pharmacy, 55(2), 149-159. https://doi.org/10.26650/IstanbulJPharm.2025.1634744
AMA
1.Özyılmaz ED, Güler E, Süer K, Özbilgin A, Çavuş İ, Çomoğlu T. Naltrexone Hydrochloride Loaded W/O Microemulsions: Preparation, Characterization and Exploring the Anti-leishmanial Activity. iujp. 2025;55(2):149-159. doi:10.26650/IstanbulJPharm.2025.1634744
Chicago
Özyılmaz, Emine Dilek, Emrah Güler, Kaya Süer, Ahmet Özbilgin, İbrahim Çavuş, and Tansel Çomoğlu. 2025. “Naltrexone Hydrochloride Loaded W O Microemulsions: Preparation, Characterization and Exploring the Anti-Leishmanial Activity”. İstanbul Journal of Pharmacy 55 (2): 149-59. https://doi.org/10.26650/IstanbulJPharm.2025.1634744.
EndNote
Özyılmaz ED, Güler E, Süer K, Özbilgin A, Çavuş İ, Çomoğlu T (September 1, 2025) Naltrexone Hydrochloride Loaded W/O Microemulsions: Preparation, Characterization and Exploring the Anti-leishmanial Activity. İstanbul Journal of Pharmacy 55 2 149–159.
IEEE
[1]E. D. Özyılmaz, E. Güler, K. Süer, A. Özbilgin, İ. Çavuş, and T. Çomoğlu, “Naltrexone Hydrochloride Loaded W/O Microemulsions: Preparation, Characterization and Exploring the Anti-leishmanial Activity”, iujp, vol. 55, no. 2, pp. 149–159, Sept. 2025, doi: 10.26650/IstanbulJPharm.2025.1634744.
ISNAD
Özyılmaz, Emine Dilek - Güler, Emrah - Süer, Kaya - Özbilgin, Ahmet - Çavuş, İbrahim - Çomoğlu, Tansel. “Naltrexone Hydrochloride Loaded W O Microemulsions: Preparation, Characterization and Exploring the Anti-Leishmanial Activity”. İstanbul Journal of Pharmacy 55/2 (September 1, 2025): 149-159. https://doi.org/10.26650/IstanbulJPharm.2025.1634744.
JAMA
1.Özyılmaz ED, Güler E, Süer K, Özbilgin A, Çavuş İ, Çomoğlu T. Naltrexone Hydrochloride Loaded W/O Microemulsions: Preparation, Characterization and Exploring the Anti-leishmanial Activity. iujp. 2025;55:149–159.
MLA
Özyılmaz, Emine Dilek, et al. “Naltrexone Hydrochloride Loaded W O Microemulsions: Preparation, Characterization and Exploring the Anti-Leishmanial Activity”. İstanbul Journal of Pharmacy, vol. 55, no. 2, Sept. 2025, pp. 149-5, doi:10.26650/IstanbulJPharm.2025.1634744.
Vancouver
1.Emine Dilek Özyılmaz, Emrah Güler, Kaya Süer, Ahmet Özbilgin, İbrahim Çavuş, Tansel Çomoğlu. Naltrexone Hydrochloride Loaded W/O Microemulsions: Preparation, Characterization and Exploring the Anti-leishmanial Activity. iujp. 2025 Sep. 1;55(2):149-5. doi:10.26650/IstanbulJPharm.2025.1634744