Microemulsions strongly promoted the activity of α-bisabolol against different Leishmania species and its skin permeation.

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  • Additional Information
    • Source:
      Publisher: Academic Press Country of Publication: United States NLM ID: 0370713 Publication Model: Print-Electronic Cited Medium: Internet ISSN: 1090-2449 (Electronic) Linking ISSN: 00144894 NLM ISO Abbreviation: Exp Parasitol Subsets: MEDLINE
    • Publication Information:
      Publication: Orlando, FL : Academic Press
      Original Publication: New York.
    • Subject Terms:
      Monocyclic Sesquiterpenes*/pharmacology ; Monocyclic Sesquiterpenes*/chemistry ; Emulsions*/chemistry ; Sesquiterpenes*/pharmacology ; Sesquiterpenes*/chemistry ; Skin*/parasitology ; Macrophages, Peritoneal*/drug effects ; Macrophages, Peritoneal*/parasitology; Animals ; Mice ; Leishmaniasis, Cutaneous/drug therapy ; Leishmaniasis, Cutaneous/parasitology ; Spectroscopy, Fourier Transform Infrared ; Skin Absorption/drug effects ; Mice, Inbred BALB C ; Female ; Leishmania/drug effects ; Surface-Active Agents/pharmacology ; Surface-Active Agents/chemistry ; Antiprotozoal Agents/pharmacology ; Antiprotozoal Agents/chemistry
    • Abstract:
      This study aimed to develop microemulsions (MEs) containing α-bisabolol for the topical treatment of cutaneous leishmaniasis (CL). Initially, pseudoternary phase diagrams were developed using α-bisabolol as the oil phase, Eumulgin® CO 40 as the surfactant, Polymol® HE as the co-surfactant, and distilled water as the aqueous phase. Two transparent liquid systems (TLS) containing 5% of α-bisabolol were selected and characterized (F5E25 and F5EP25). Next, skin permeation and retention assays were performed using Franz cells. The interaction of the formulation with the stratum corneum (SC) was evaluated using the FTIR technique. The cytotoxicity was evaluated in murine peritoneal macrophages. Finally, the antileishmanial activity of microemulsions was determined in promastigotes and amastigotes of L. amazonensis (strain MHOM/BR/77/LTB 0016). As a result, the selected formulations showed isotropy, nanometric size (below 25 nm), Newtonian behavior and pH ranging from 6.5 to 6.9. The MEs achieved a 2.5-fold increase in the flux and skin-permeated amount of α-bisabolol. ATR-FTIR results showed that microemulsions promoted fluidization and extraction of lipids and proteins of the stratum corneum, increasing the diffusion coefficient and partition coefficient of the drug in the skin. Additionally, F5E25 and F5EP25 showed higher activity against promastigotes (IC 50 13.27 and 18.29, respectively) compared to unencapsulated α-bisabolol (IC 50 53.8). Furthermore, F5E25 and F5EP25 also showed antileishmanial activity against intracellular amastigotes of L. amazonensis, with IC 50 50 times lower than free α-bisabolol and high selectivity index (up to 15). Therefore, the systems obtained are favorable to topical administration, with significant antileishmanial activity against L. amazonensis promastigotes and amastigotes, being a promising system for future in vivo trials.
      Competing Interests: Declaration of competing interest The authors declare that they have no known competing financial interests or personal relationships that could have appeared to influence the work reported in this paper.
      (Copyright © 2024 Elsevier Inc. All rights reserved.)
    • Contributed Indexing:
      Keywords: Amastigotes; Cutaneous leishmaniasis; Microemulsions and α-bisabolol; Promastigotes
    • Accession Number:
      24WE03BX2T (bisabolol)
      0 (Monocyclic Sesquiterpenes)
      0 (Emulsions)
      0 (Sesquiterpenes)
      0 (Surface-Active Agents)
      0 (Antiprotozoal Agents)
    • Publication Date:
      Date Created: 20240802 Date Completed: 20240910 Latest Revision: 20240910
    • Publication Date:
      20240911
    • Accession Number:
      10.1016/j.exppara.2024.108808
    • Accession Number:
      39094996