Development and Characterization of Clioquinol Nanocrystals

Francielli Lima dos Santos; Julia Capp Zilles; Simone Jacobus Berlitz; Irene Clemes Kulkamp Guerreiro; Alexandre Meneghello Fuentefria; Renata Vidor Contri

doi:10.22456/dar.v10i1.152513

Authors

Francielli Lima dos Santos Programa de Pós-Graduação em Ciências Farmacêuticas (PPGCF) - Universidade Federal do Rio Grande do Sul https://orcid.org/0000-0002-2289-0046
Julia Capp Zilles Programa de Pós-Graduação em Ciências Farmacêuticas (PPGCF) - Universidade Federal do Rio Grande do Sul https://orcid.org/0000-0003-0620-0452
Simone Jacobus Berlitz Graduação em Nanotecnologia Farmacêutica (PPGNANO) - Universidade Federal do Rio Grande do Sul https://orcid.org/0000-0002-9904-792X
Irene Clemes Kulkamp Guerreiro Programa de Pós-Graduação em Ciências Farmacêuticas (PPGCF); Graduação em Nanotecnologia Farmacêutica (PPGNANO) - Universidade Federal do Rio Grande do Sul https://orcid.org/0000-0001-8607-7612
Alexandre Meneghello Fuentefria Programa de Pós-Graduação em Ciências Farmacêuticas (PPGCF) - Universidade Federal do Rio Grande do Sul https://orcid.org/0000-0003-2979-4417
Renata Vidor Contri Programa de Pós-Graduação em Ciências Farmacêuticas (PPGCF) - Universidade Federal do Rio Grande do Sul https://orcid.org/0000-0002-0141-0808

DOI:

https://doi.org/10.22456/dar.v10i1.152513

Keywords:

Antifungal, Clioquinol, Nanosuspension, Polysorbate 80, Skin, Wet bead milling

Abstract

Drug nanocrystals, composed solely of active substance and stabilizer, have recently been proposed for cutaneous applications, including the management of skin fungal infections (dermatomycoses), which are often difficult to treat. Clioquinol nanocrystals were obtained using different preparation methods, drug concentrations, surfactants, and bead sizes. The selected nanocrystal suspension (bead milling, 1% drug, 1% polysorbate 80) exhibited an average particle size of approximately 300 nm (polydispersity index of 0.254), a zeta potential of −7.6 mV, a pH value of 5.4, a drug content of about 97% (relative to 10 mg/mL), and a nanocrystallization efficiency of approximately 96%. The presence of the surfactant was essential to ensure nanocrystal stability for 90 days at room temperature. Overall, the results indicate that clioquinol nanocrystals are possible to be obtained by small-scale wet bead milling and present suitable nanometric features, being considered a promising alternative as cutaneous antifungal therapy.

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