Platensimycin (PTM)
is a promising natural product drug lead against
Gram-positive bacteria, including methicillin-resistant Staphylococcus
aureus (MRSA), while the clinical development was hampered
by problems related to its poor solubility and pharmacokinetic properties.
In this study, we used liposomes and micelles as carriers of PTM to
prepare PTM nanoformulations for the treatment of MRSA infection in
mice. PTM-loaded nanoparticles could effectively reduce residual bacteria
in the MRSA-infected macrophage cell model, comparing to free PTM.
More importantly, in vivo studies showed that encapsulation
of PTM by liposomes or micelles effectively improved the pharmacokinetic
properties of PTM in Sprague–Dawley rats and the survival rate
of MRSA-infected C57BL/6J mice. Our study has thus suggested that
the clinically used nanocarriers, such as liposome and micelle, might
also be useful to improve the efficacy of other natural product drug
leads to accelerate their in vivo evaluation and
preclinical development.