Development and Pharmacokinetics Study of Antifungal Peptide Nanoliposomes by Liquid Chromatography-tandem Mass Spectrometry

Author(s): Shuoye Yang*

Journal Name: Current Pharmaceutical Analysis

Volume 15 , Issue 4 , 2019

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Graphical Abstract:


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.

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.

Keywords: Antifungal peptide, liposomes, pharmacokinetics, in vivo, LC-MS/MS, protein drugs.

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Article Details

Year: 2019
Published on: 19 March, 2019
Page: [312 - 318]
Pages: 7
DOI: 10.2174/1573412914666180307155328
Price: $65

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