Characterization, antibiofilm, and mechanism of action of novel PEG-stabilized lipid nanoparticles loaded with terpinen-4-ol.
Terpinen-4-ol, an active component of tea tree oil, exhibits broad-spectrum antimicrobial activity. However, the high volatilization of terpinen-4-ol and its nonwettability property have limited its application. Our objective was to synthesize novel nanocarriers to deliver and protect terpinen-4-ol. The polyethylene glycol (PEG)-stabilized lipid nanoparticles were prepared and characterized by scanning electron microscope, Zetasizer, and differential scanning calorimetry. These nanoparticles had an average diameter of 397 nm and a Ζ-potential of 10 mV after being modified by glycine. Results showed that homogeneous particle size, high drug loading, stability, and targeting were obtained by the nanoparticles. Liquid chromatography/mass spectrometry showed a sustained release trend from nanoparticles for terpinen-4-ol. Minimum inhibitory concentration and minimum biofilm eradication concentration were tested against Candida albicans ATCC 11231. Studies on isolated mitochondria showed the blockage of biofilm respiration and inhibition of enzyme activity. The effects can be ascribed to localization of terpinen-4-ol on the membrane of mitochondria.
School of Life Sciences and Technology, Tongji University, Shanghai, China.
Li-ming
LM
Sun
Chen-lu
CL
Zhang
Ping
P
Li
D000890:Anti-Infective Agents / Q000008:administration & dosage*; D018441:Biofilms / Q000187:drug effects*; D002176:Candida albicans / Q000187:drug effects / Q000502:physiology; D003692:Delayed-Action Preparations; D004355:Drug Stability; D008055:Lipids / Q000737:chemistry; D053758:Nanoparticles / Q000737:chemistry*; D010316:Particle Size; D011092:Polyethylene Glycols / Q000737:chemistry*; D020947:Tea Tree Oil / Q000737:chemistry; D013729:Terpenes / Q000008:administration & dosage*; D014835:Volatilization
D000890:Anti-Infective Agents; D003692:Delayed-Action Preparations; D008055:Lipids; D013729:Terpenes; D011092:Polyethylene Glycols; C034019:terpinenol-4; D020947:Tea Tree Oil