Preparation of Terpenoid-Invasomes with Selective Activity against S. aureus and Characterization by Cryo Transmission Electron Microscopy
Open Access
- 1 May 2020
- journal article
- research article
- Published by MDPI AG in Biomedicines
- Vol. 8 (5), 105
- https://doi.org/10.3390/biomedicines8050105
Abstract
Terpenoids are natural plant-derived products that are applied to treat a broad range of human diseases, such as airway infections and inflammation. However, pharmaceutical applications of terpenoids against bacterial infection remain challenging due to their poor water solubility. Here, we produce invasomes encapsulating thymol, menthol, camphor and 1,8-cineol, characterize them via cryo transmission electron microscopy and assess their bactericidal properties. While control- and cineol-invasomes are similarly distributed between unilamellar and bilamellar vesicles, a shift towards unilamellar invasomes is observable after encapsulation of thymol, menthol or camphor. Thymol- and camphor-invasomes show a size reduction, whereas menthol-invasomes are enlarged and cineol-invasomes remain unchanged compared to control. While thymol-invasomes lead to the strongest growth inhibition of S. aureus, camphor- or cineol-invasomes mediate cell death and S. aureus growth is not affected by menthol-invasomes. Flow cytometric analysis validate that invasomes comprising thymol are highly bactericidal to S. aureus. Notably, treatment with thymol-invasomes does not affect survival of Gram-negative E. coli. In summary, we successfully produce terpenoid-invasomes and demonstrate that particularly thymol-invasomes show a strong selective activity against Gram-positive bacteria. Our findings provide a promising approach to increase the bioavailability of terpenoid-based drugs and may be directly applicable for treating severe bacterial infections such as methicillin-resistant S. aureus.Keywords
This publication has 39 references indexed in Scilit:
- 1,8-Cineol inhibits nuclear translocation of NF-κB p65 and NF-κB-dependent transcriptional activityBiochimica et Biophysica Acta (BBA) - Molecular Cell Research, 2013
- Thymol nanospheres as an effective anti-bacterial agentInternational Journal of Pharmaceutics, 2012
- Fiji: an open-source platform for biological-image analysisNature Methods, 2012
- Nanosuspension: An approach to enhance solubility of drugsJournal of Advanced Pharmaceutical Technology & Research, 2011
- Synergistic properties of the terpenoids aromadendrene and 1,8-cineole from the essential oil of Eucalyptus globulus against antibiotic-susceptible and antibiotic-resistant pathogensPhytomedicine, 2010
- Fluticasone and budesonide nanosuspensions for pulmonary delivery: Preparation, characterization, and pharmacokinetic studiesJournal of Pharmaceutical Sciences, 2008
- Terpenoids: natural inhibitors of NF-κB signaling with anti-inflammatory and anticancer potentialCellular and Molecular Life Sciences, 2008
- The function of terpene natural products in the natural worldNature Chemical Biology, 2007
- Effects of oregano, carvacrol and thymol on Staphylococcus aureus and Staphylococcus epidermidis biofilmsJournal of Medical Microbiology, 2007
- Difference in surface properties between Escherichia coli and Staphylococcus aureus as revealed by electrophoretic mobility measurementsBiophysical Chemistry, 1995