Polymeric Nanocapsules Containing Ozonated Oil and Terbinafine Hydrochloride as a Potential Treatment Against Dermatophytes.

Autor: Dos Santos FL; Faculdade de Farmácia, Universidade Federal do Rio Grande do Sul, Av. Ipiranga, 2752, Azenha, Porto Alegre, RS, 90610-000, Brazil., Zilles JC; Programa de Pós-Graduação em Ciências Farmacêuticas - PPGCF, Universidade Federal do Rio Grande do Sul, Porto Alegre, RS, 90610-000, Brazil., Machado AU; Faculdade de Farmácia, Universidade Federal do Rio Grande do Sul, Av. Ipiranga, 2752, Azenha, Porto Alegre, RS, 90610-000, Brazil., Marques MS; Programa de Pós-Graduação em Ciências Farmacêuticas - PPGCF, Universidade Federal do Rio Grande do Sul, Porto Alegre, RS, 90610-000, Brazil., da Costa BS; Programa de Pós-Graduação em Ciências Farmacêuticas - PPGCF, Universidade Federal do Rio Grande do Sul, Porto Alegre, RS, 90610-000, Brazil., Kulkamp Guerreiro IC; Faculdade de Farmácia, Universidade Federal do Rio Grande do Sul, Av. Ipiranga, 2752, Azenha, Porto Alegre, RS, 90610-000, Brazil.; Programa de Pós-Graduação em Ciências Farmacêuticas - PPGCF, Universidade Federal do Rio Grande do Sul, Porto Alegre, RS, 90610-000, Brazil.; Programa de Pós-Graduação em Farmacologia e Terapêutica - PPGFT, Universidade Federal do Rio Grande do Sul, Porto Alegre, RS, 90050-170, Brazil., Fuentefria AM; Faculdade de Farmácia, Universidade Federal do Rio Grande do Sul, Av. Ipiranga, 2752, Azenha, Porto Alegre, RS, 90610-000, Brazil.; Programa de Pós-Graduação em Ciências Farmacêuticas - PPGCF, Universidade Federal do Rio Grande do Sul, Porto Alegre, RS, 90610-000, Brazil.; Programa de Pós-Graduação em Farmacologia e Terapêutica - PPGFT, Universidade Federal do Rio Grande do Sul, Porto Alegre, RS, 90050-170, Brazil., Contri RV; Faculdade de Farmácia, Universidade Federal do Rio Grande do Sul, Av. Ipiranga, 2752, Azenha, Porto Alegre, RS, 90610-000, Brazil. renata.contri@ufrgs.br.; Programa de Pós-Graduação em Ciências Farmacêuticas - PPGCF, Universidade Federal do Rio Grande do Sul, Porto Alegre, RS, 90610-000, Brazil. renata.contri@ufrgs.br.
Jazyk: angličtina
Zdroj: AAPS PharmSciTech [AAPS PharmSciTech] 2023 Oct 02; Vol. 24 (7), pp. 198. Date of Electronic Publication: 2023 Oct 02.
DOI: 10.1208/s12249-023-02657-x
Abstrakt: Terbinafine hydrochloride is a synthetic allylamine whose mechanism of action consists of inhibiting the enzyme squalene epoxidase that participates in the first stage of ergosterol synthesis, interfering with fungal membrane function. Ozonated oils are used for topical application of ozone, producing reactive oxygen species that cause cellular damage in microorganisms, therefore being an alternative treatment for acute and chronic skin infections. This study aimed to develop and characterize Eudragit ® RS100 nanocapsules, obtained by interfacial deposition of preformed polymer method, containing 0.5% terbinafine hydrochloride and 5% ozonated sunflower seed oil as a potential treatment against dermatophytes. The polymeric nanocapsules were characterized regarding particle size, zeta potential, pH, drug content, encapsulation efficiency, and stability. The in vitro drug release, in vitro skin permeation, and in vitro antifungal activity were also evaluated. The particle size was around 150 nm with a narrow size distribution, the zeta potential was around + 6 mV, and the pH was 2.2. The drug content was close to 95% with an encapsulation efficiency of 53%. The nanocapsules were capable to control the drug release and the skin permeation. The in vitro susceptibility test showed greater antifungal activity for the developed nanocapsules, against all dermatophyte strains tested, compared to the drug solution. Therefore, the polymeric nanocapsules suspension containing terbinafine hydrochloride and ozonated oil can be considered a potential high-efficacy candidate for the treatment of dermatophytosis, with a possible reduction in the drug dose and frequency of applications. Studies to evaluate safety and efficacy in vivo still need to be performed.
(© 2023. The Author(s), under exclusive licence to American Association of Pharmaceutical Scientists.)
Databáze: MEDLINE
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