Vol. 14 No. 86 (2025): Continuous Edition (February – December 2025)
Articles

Epiisopiloturin–Hydroxypropyl-β-Cyclodextrin inclusion complexes: preparation, characterization, and application in neglected diseases

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  • Karolynne Rodrigues de Melo,
  • Maria Vitória Barbosa dos Santos,
  • Débora Vitória Firmino de Lima,
  • Cybelly Marques de Melo,
  • Pedro José Rolim Neto,
  • Rosali Maria Ferreira da Silva
Karolynne Rodrigues de Melo
Federal University of Pernambuco (UFPE), Department of Pharmacy, Brazil.
Author Biography

MSc, Federal University of Pernambuco (UFPE), Department of Pharmacy, Brazil.

Maria Vitória Barbosa dos Santos
Federal University of Pernambuco (UFPE), Department of Pharmacy, Brazil.
Author Biography

Undergraduate, Federal University of Pernambuco (UFPE), Department of Pharmacy, Brazil.

Débora Vitória Firmino de Lima
Federal University of Pernambuco (UFPE), Department of Pharmacy, Brazil.
Author Biography

B.Sc, Federal University of Pernambuco (UFPE), Department of Pharmacy, Brazil.

Cybelly Marques de Melo
Federal University of Pernambuco (UFPE), Department of Pharmacy, Brazil.
Author Biography

PhD, Federal University of Pernambuco (UFPE), Department of Pharmacy, Brazil.

Pedro José Rolim Neto
Federal University of Pernambuco (UFPE), Department of Pharmacy, Brazil.
Author Biography

PhD, Federal University of Pernambuco (UFPE), Department of Pharmacy, Brazil.

Rosali Maria Ferreira da Silva
Federal University of Pernambuco (UFPE), Department of Pharmacy, Brazil.
Author Biography

PhD, Federal University of Pernambuco (UFPE), Department of Pharmacy, Brazil.

DOI: https://doi.org/10.34069/AI/2025.86.02.16

Published 2025-10-04

Keywords

  • Epiisopiloturin,
  • Cyclodextrin,
  • Inclusion complex,
  • Increased solubility

How to Cite

Rodrigues de Melo, K., Barbosa dos Santos, M. V., Firmino de Lima, D. V., Marques de Melo, C., Rolim Neto, P. J., & Ferreira da Silva, R. M. (2025). Epiisopiloturin–Hydroxypropyl-β-Cyclodextrin inclusion complexes: preparation, characterization, and application in neglected diseases. Amazonia Investiga, 14(86), 215–225. https://doi.org/10.34069/AI/2025.86.02.16

Copyright (c) 2025 Karolynne Rodrigues de Melo, Maria Vitória Barbosa dos Santos, Débora Vitória Firmino de Lima, Cybelly Marques de Melo, Pedro José Rolim Neto, Rosali Maria Ferreira da Silva

Creative Commons License

This work is licensed under a Creative Commons Attribution 4.0 International License.

Abstract

Context: Pilocarpus microphyllus (Jaborandi) is widely used for extracting pilocarpine, generating biomass rich in secondary metabolites. Among these, epiisopiloturin (EPI) exhibits potential against neglected diseases, in addition to anti-inflammatory and antinociceptive effects. However, its poor aqueous solubility limits its pharmaceutical application. Objective: To enhance the solubility of EPI by forming an inclusion complex with hydroxypropyl-β-cyclodextrin (HPβCD) using the freeze-drying technique. Methods: A phase solubility study was conducted to determine the stability constant and stoichiometry. The inclusion complex was prepared via lyophilization and characterized by Differential Scanning Calorimetry (DSC), Fourier Transform Infrared Spectroscopy (FTIR), X-ray Diffraction (XRD), and in vitro dissolution testing. Results: Characterization confirmed the formation of the EPI:HPβCD complex, indicating strong interactions between components. The DSC thermogram showed the disappearance of the EPI melting peak, supported by FTIR results, suggesting successful complexation. XRD patterns revealed an amorphous structure. In vitro dissolution demonstrated a marked increase in solubility: 100% of the complexed EPI dissolved within 5 minutes, compared to only 19% of the free compound. Conclusion: Complexation with HPβCD significantly improved the solubility of EPI, reinforcing its potential for development into an innovative pharmaceutical formulation for the treatment of neglected diseases.

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