Journal
FUTURE MEDICINAL CHEMISTRY
Volume 11, Issue 20, Pages 2647-2662Publisher
FUTURE SCI LTD
DOI: 10.4155/fmc-2018-0580
Keywords
alpha-linolenic acid; amphotericin B; antifungal activity; monomethoxy polyethylene glycol; polyethylene imine
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Funding
- Natural Science Foundation of Shandong Province [ZR2016BL15]
- Science and Technology Project of University of Jinan [XKY1732]
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Aim: To encapsulate amphotericin B (AmB) with reduced toxicity and comparable activity. Results & methodology: The a-linolenic acid (ALA)-modified monomethoxy polyethylene glycol-g-PEI-g-ALA conjugate was employed to prepare AmB-loaded micelles (AmB-M). In vitro activity and release behavior of AmB-M were investigated. AmB-M enhanced AmB's water-solubility to 1.2 mg/ml, showing good storage stability. AmB-M could achieve a sustained and slow release of AmB, low hemolysis activity and negligible kidney toxicity when compared with commercial AmB injection. Antifungal activity and biofilm inhibition experiments confirmed that the antifungal activity of AmB-M against Candida albicans was similar to that of AmB injection. Conclusion: Monomethoxy polyethylene glycol-g-PEI-g-ALA micelles could be a preferable choice to treat systemic fungal infections as an efficient drug delivery system.
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