Background:
The therapeutic ability and application of antifungal peptide (APs) are limited
by their physico-chemical and biological properties, the nano-liposomal encapsulation would improve
the in vivo circulation and stability.
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Objective: To develop a long-circulating liposomal delivery systems encapsulated APs-CGA-N12 with
PEGylated lipids and cholesterol, and investigated through in vivo pharmacokinetics.
Methods:
The liposomes were prepared and characterized, a rapid and simple liquid chromatographytandem
mass spectrometry (LC-MS/MS) assay was developed for the determination of antifungal peptide
in vivo, the pharmacokinetic characteristics of APs liposomes were evaluated in rats.
Results:
Liposomes had a large, unilamellar structure, particle size and Zeta potential ranged from 160
to 185 nm and -0.55 to 1.1 mV, respectively. The results indicated that the plasma concentration of
peptides in reference solutions rapidly declined after intravenous administration, whereas the
liposomeencapsulated ones showed slower elimination. The AUC(0-∞) was increased by 3.0-fold in
liposomes in comparison with standard solution (20 mg·kg-1), the half-life (T1/2) was 1.6- and 1.5-fold
higher compared to the reference groups of 20 and 40 mg·kg-1, respectively.
Conclusion:
Therefore, it could be concluded that liposomal encapsulation effectively improved the
bioavailability and pharmacokinetic property of antifungal peptides.