Development and characterization of lectin-functionalized vesicular constructs bearing amphotericin B for bio-film targeting

Abstract

The long-term goal of this work will be to develop a topical formulation for oropharyngeal candidosis. Liposomes were prepared by the vesicle extrusion technique from mixtures of dipalmitoylphosphatidylcholine, cholesterol, and stearylamine incorporating a reactive phospholipid, the m-maleimidobenzoyl-N-hydroxysuccinimide ester derivative of dipalmitoylphosphatidylethanolamine, which was conjugated with the N-succinimidyl-S-acetylthioacetate derivatives of succinyl concanavalin A. Morphology of liposomes was studied by transmission electron microscopy and bio-film architecture using fluorescence microscopy. Lectinized vesicles were put into contact with bovine submaxillary mucin, to determine the in vitro activity and specificity. Targeting study was performed using 3-(4,5-dimethyl-2-thiazolyl)-2,5-diphenyl-2H-tetrazolium bromide (MTT) assay. The liposomes were found to have a diameter in the range of 360–450 and 390–510 nm for uncoated and coated formulations, respectively. The MTT assay showed a strong association of lectin-bearing liposomes with candidal bio-film. The results suggest that surface-modified liposomes can effectively target candidal bio-film in vitro.

Keywords::

• Liposomes
• lectins
• bio-film
• targeting
• proteoliposomes
• Candida albicans

Acknowledgements

M. S. S. is indebted to the Head of the Department of Pharmaceutical Sciences, Dr Hari Singh Gour University, Sagar for providing all the facilities for carrying out the research work. The author is also grateful to SAIF, AIIMS, New Delhi for TEM facility.

Declaration of interest: The authors report no conflicts of interest.