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Microemulsions containing Copaifera multijuga Hayne oil-resin: Challenges to achieve an efficient system for β-caryophyllene delivery

2017; Elsevier BV; Volume: 111; Linguagem: Inglês

10.1016/j.indcrop.2017.10.025

1872-633X

Jamilly Kelly de Oliveira Neves, Alexsandra Conceição Apolinário, Karina Lidiane Alcântara Saraiva, Dayanne Tomaz Casimiro da Silva, Mysrayn Yargo de Freitas Araújo Reis, Bolívar Ponciano Goulart de Lima Damasceno, Adalberto Pessoa, Marcos Aurélio Moraes Galvão, Luiz Alberto Lira Soares, Valdir Florêncio da Veiga, José Alexsandro da Silva, Attílio Converti,

Biological Activity of Diterpenoids and Biflavonoids

β-Caryophyllene (β-CP) is a bioactive sesquiterpene abundant in copaiba oil-resin (COR), which is widely used in Brazilian folk medicine; however, its instability due to the presence of unsaturations is an obstacle to the use of COR in its natural form. Therefore, the development of a system for β-CP delivery, like the one proposed herein for the first time, may protect it and preserve its therapeutic action. Pseudo-ternary phase diagrams were constructed in this study to obtain COR-containing nanocarriers. Two microemulsions (MEs) were obtained, namely a) ME-I containing (% w/w) 47.1 water, 8.5 Plurol Oleique, 33.8 Labrasol and 10.6 COR and b) ME-II containing (% w/w) 39.0 water, 18.3 Plurol Oleique, 36.6 Labrasol and 6.1 COR. Both MEs showed physicochemical properties suitable for a delivery system such as pH 5.25-5.74, conductivity of 79.5–120.9 μS cm−1 and slightly negative Zeta potential (-3.57/-2.63 mV). Transmission electron microscopy revealed the nanometric size of MEs droplets, differential scanning calorimetry their oil/water nature, while refractive indices clarity and isotropicity. Both systems behaved as Newtonian fluids and exhibited low viscosity (64.42 ± 0.667 mPa.s for ME-I and 118.78 ± 0.503 mPa.s for ME-II). After COR incorporation in MEs, steam distillation allowed obtaining β-CP contents depending on their initial COR amount. The pharmacological effectiveness of these innovating systems for β-CP delivery was confirmed by antimicrobial and anti-inflammatory activity tests. ME-II afforded a stronger antimicrobial effect against all target microorganisms than ME-I and a much stronger one than COR. Carrageenan-induced inflammation in rat paw was visibly inhibited by MEs.