title: 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.
authors.affiliation: Department of Pharmaceutical Sciences, Biopharmaceuticals Research Laboratory, Dr HS Gour University, Sagar, MP, India.
authors.forename: M S
authors.initials: MS
authors.lastname: Sudheesh
authors.forename: Vikas
authors.initials: V
authors.lastname: Jain
authors.forename: Gyati
authors.initials: G
authors.lastname: Shilakari
authors.forename: D V
authors.initials: DV
authors.lastname: Kohli
mesh_terms: D000666:Amphotericin B / Q000008:administration & dosage* / Q000737:chemistry / Q000494:pharmacology; D000935:Antifungal Agents / Q000008:administration & dosage* / Q000737:chemistry / Q000494:pharmacology; D018441:Biofilms; D002176:Candida albicans / Q000187:drug effects* / Q000502:physiology; D037102:Lectins / Q000737:chemistry; D008081:Liposomes / Q000737:chemistry*; D008826:Microbial Sensitivity Tests; D010316:Particle Size; D011510:Proteolipids / Q000737:chemistry*
chemical_list: D000935:Antifungal Agents; D037102:Lectins; D008081:Liposomes; D011510:Proteolipids; C020485:proteoliposomes; D000666:Amphotericin B