Microstructure and biopharmaceutical performances of curcumin-loaded low-energy nanoemulsions containing eucalyptol and pinene: Terpenes’ role overcome penetration enhancement effect?
| Autor: | Snezana Savic, Evgenia Mitsou, Dominique Jasmin Lunter, Vassiliki Papadimitriou, Ana Zugic, Aristotelis Xenakis, Bojan Marković, Danijela Randjelovic, Ines Nikolić, Ivana Pantelić |
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| Rok vydání: | 2020 |
| Předmět: |
Adult
Curcumin Skin Absorption Monoterpene Polysorbates Pharmaceutical Science 02 engineering and technology Administration Cutaneous Penetration 030226 pharmacology & pharmacy Polyvinyl alcohol Terpene Surface-Active Agents Young Adult 03 medical and health sciences chemistry.chemical_compound 0302 clinical medicine Lecithins Low-energy nanoemulsion Humans Solubility Skin Pinene Eucalyptol Chromatography Terpenes Penetration (firestop) 021001 nanoscience & nanotechnology Nanostructures chemistry Monoterpenes Interfacial dynamics Nanoparticles Emulsions Female 0210 nano-technology Oils Electron paramagnetic resonance spectroscopy |
| Zdroj: | European Journal of Pharmaceutical Sciences |
| Popis: | The objective of this work was to develop low-energy nanoemulsions for enhanced dermal delivery of curcumin, using monoterpene compounds eucalyptol (EUC) and pinene (PIN) as chemical penetration enhancers. Spontaneous emulsification was the preparation method. All formulations contained 10% of the oil phase (medium-chain triglycerides (MCT), or their mixture with EUC or PIN). Formulations were stabilized by the combination of polysorbate 80 and soybean lecithin (surfactant-to-oil-ratio=1). Concentration of curcumin was set to 3 mg/ml. Average droplet diameter of all tested formulations ranged from 102 nm to 132 nm, but the ones containing monoterpenes had significantly smaller size compared to the MCT formulation. Such finding was profoundly studied through electron paramagnetic resonance spectroscopy, which proved that the presence of monoterpenes modified the nanoemulsions’ interfacial environment, resulting in droplet size reduction. The release study of curcumin (using Franz cells) demonstrated that the cumulative amount released after 6 h of the experiment was 10.1 ± 0.2% for the MCT nanoemulsions, 13.9 ± 0.1% and 14.0 ± 0.2% for PIN and EUC formulations, respectively. In vivo tape stripping revealed their performances in delivering curcumin into the skin, indicating the following order: EUC>MCT>PIN. The formulation with EUC was clearly the most successful, giving the highest cumulative amount of curcumin that penetrated per surface unit: 34.24±5.68 µg/cm2. The MCT formulation followed (30.62±2.61 µg/cm2) and, finally, the one with PIN (21.61±0.11 µg/cm2). These results corelated with curcumin's solubility in the chosen oils: 4.18±0.02 mg/ml for EUC, 1.67±0.04 mg/ml for MCT and 0.21±0.01 mg/ml for PIN. Probably, higher solubility in the oil phase of the nanoemulsion promoted curcumin's solubility in the superficial skin layers, providing enhanced penetration. This is the peer-reviewed version of the article: European Journal of Pharmaceutical Sciences, 2020, 142, 105135, [https://doi.org/10.1016/j.ejps.2019.105135] The published version: [http://cer.ihtm.bg.ac.rs/handle/123456789/3309] |
| Databáze: | OpenAIRE |
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