期刊
EUROPEAN JOURNAL OF PHARMACEUTICS AND BIOPHARMACEUTICS
卷 191, 期 -, 页码 114-123出版社
ELSEVIER
DOI: 10.1016/j.ejpb.2023.08.020
关键词
Isobologram; Combination index; RAW 264.7 cells; HET-CAM assay; Safety profile
The study demonstrates that the combination of 8-caryophyllene and indomethacin delivered in nanoemulsions enhances the anti-inflammatory effect. There is a synergistic action between the two substances. The nanoemulsified combination shows lower IC50 in inhibiting nitric oxide production and exhibits no cytotoxicity or irritating effects on cell lines and embryonated eggs.
The potentiation of pharmacological effects can be achieved through several strategies, such as the association of substances and delivery in nanostructured systems. In practice, potentiation can be measured by the law of mass action and joint evaluation of the combination index (CI) and dose-response curves. In this context, this study aimed to evaluate the anti-inflammatory effect of the association of 8-caryophyllene and indomethacin in the free form and delivered in nanoemulsions using the in vitro model of LPS-stimulated murine macrophage. The results indicated potentiation of the anti-inflammatory effect of nanoemulsified substances compared to free substances, as well as synergistic action between the sesquiterpene and the selected NSAID. In comparison, the association of 8-caryophyllene and indomethacin in the free form inhibited the production of nitric oxide by 50% at 48.60 & mu;g/ mL (CI = 0.21), while the nanoemulsified association of these substances resulted in an IC50 of 1.45 & mu;g/mL (CI = 0.14). In parallel, cytotoxicity assays on HaCaT and MRC-5 cell lines demonstrated the safety of IC50-equivalent concentrations of the anti-inflammatory action, and no irritating effects on the chorioallantoic membrane of embryonated eggs were observed (HET-CAM assay). The results suggest that 8-caryophyllene may be an alternative to replace an inert oily core in nanoemulsion systems when anti-inflammatory effects are desirable.
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