Innovative Microemulsion Loaded with Unusual Dimeric Flavonoids from Fridericia platyphylla (Cham.) L.G. Lohmann Roots.

Autor: do Nascimento JR; Institut of Biosciences, Coastal Campus of São Vicente, Paulista State University-UNESP, São Vicente, São Paulo, Brazil., de Matos Monteiro Lira BS; Department of Pharmacy, Federal University of Piauí, Teresina, Brazil., do Nascimento MO; Department of Pharmacy, Federal University of Piauí, Teresina, Brazil., Lopes GLN; Department of Pharmacy, Federal University of Piauí, Teresina, Brazil., Ferreira GM; Department of Clinical and Toxicological Analyses, School of Pharmaceutical Sciences, University of São Paulo, São Paulo, Brazil., de Souza Nunes GC; Research Nucleus in Pharmaceutical Sciences Program, State University of Maringá, Paraná, Brazil., Gonçalves RS; Department of Chemistry, Federal University of Maranhão, São Luís, 11330-900, Brazil., Carvalho ALM; Department of Pharmacy, Federal University of Piauí, Teresina, Brazil., Vilegas W; Institut of Biosciences, Coastal Campus of São Vicente, Paulista State University-UNESP, São Vicente, São Paulo, Brazil., da Rocha CQ; Department of Chemistry, Federal University of Maranhão, São Luís, 11330-900, Brazil. rocha.claudia@ufma.br.
Jazyk: angličtina
Zdroj: AAPS PharmSciTech [AAPS PharmSciTech] 2023 Oct 17; Vol. 24 (8), pp. 212. Date of Electronic Publication: 2023 Oct 17.
DOI: 10.1208/s12249-023-02655-z
Abstrakt: Fridericia platyphylla (Cham.) L.G. Lohmann is a species native to the Brazilian cerrado, with promising bioactivity. The organic fraction of the roots is rich in unusual dimeric flavonoids, reported as potential candidates for cancer treatment. The exploration of these flavonoids is very important, considering their diverse biological activities and the need for innovative therapeutic options. This work aimed to develop and characterize a microemulsion loaded with a non-polar fraction (DCM). The constituents were chosen, and the pseudo-ternary diagram was constructed to determine the region of microemulsion formation. The microemulsions blank (ME), with 3% (ME3) and 5% (ME5) of fraction DCM, were characterized in terms of droplet size, zeta potential, and polydispersity index. Both MEs showed particle sizes <100 nm; only ME3 exhibited better values for polydispersity index and zeta potential and was therefore selected for further study. The organoleptic and physicochemical characteristics were evaluated, revealing limpidity and transparency typical of these microstructures, physiologically acceptable pH, refractive index of 1.42±0.01, and density of 1.017 g/cm 3 ±0.01. The stability tests showed good stability profiles even after exposure to extreme thermal conditions, with minimal changes in pH and the content of the incorporated fraction. The in vitro release study demonstrated that ME3 enabled the controlled release of the fraction, with a cumulative amount released over 60% within 6 h. Furthermore, fraction DCM and ME3 exhibited no toxicity in Tenebrio molitor larvae. The developed microemulsion exhibited excellent properties, so this study represents the first successful attempt to develop a formulation that incorporates the dimeric flavonoid fraction.
(© 2023. The Author(s), under exclusive licence to American Association of Pharmaceutical Scientists.)
Databáze: MEDLINE