title: Molecular recognition by Kluyveromyces of amphotericin B-loaded, galactose-tagged, poly (lactic acid) microspheres.
abstract: In an effort to develop a new way of drug delivery, especially for polyenic antifungal molecules, we have incorporated amphotericin B (AmB) into biodegradable galactosylated poly (L-lactic acid) (L-PLA) and poly (L-lactic-co-glycolic acid) (PLGA) microspheres. These drug carriers were prepared by solvent evaporation using an oil/water (o/w) emulsion. The ratio of galactosyl spacers with different chain lengths was 1.74-2.78%. The maximal quantity of AmB encapsulated reported to 100 mg of the galactosylated microspheres was 7.14 mg for L-PLA (encapsulation rate 45% of mole) and 6.42 mg for PLGA derivatives (encapsulation rate 81% of mole). In our yeast model, drug release depended on three factors: (i) presence of galactosylated antennae, (ii) length of galactosyl antenna and (iii) nature of the polymer. More of the AmB trapped in PLGA microspheres was released than from PLA microspheres. These novel functionalised microspheres could be required for the delivering of therapeutic agents according to their recognition to specific cells.
authors.affiliation: UMR 5078 CNRS, Université Claude Bernard, Bât. 305, 43 bd du 11 Novembre 1918, 69622, Villeurbanne Cedex, France.
authors.forename: Rima
authors.initials: R
authors.lastname: Kassab
authors.forename: Hélène
authors.initials: H
authors.lastname: Parrot-Lopez
authors.forename: Hatem
authors.initials: H
authors.lastname: Fessi
authors.forename: Jean
authors.initials: J
authors.lastname: Menaucourt
authors.forename: Roger
authors.initials: R
authors.lastname: Bonaly
authors.forename: Joël
authors.initials: J
authors.lastname: Coulon
mesh_terms: D000666:Amphotericin B / Q000008:administration & dosage* / Q000494:pharmacology; D000935:Antifungal Agents / Q000008:administration & dosage* / Q000494:pharmacology; D004337:Drug Carriers / Q000138:chemical synthesis* / Q000737:chemistry*; D005690:Galactose / Q000737:chemistry*; D006016:Glycolates / Q000737:chemistry*; D007716:Kluyveromyces / Q000187:drug effects / Q000254:growth & development / Q000502:physiology*; D019344:Lactic Acid; D016015:Logistic Models; D018625:Microscopy, Atomic Force; D008863:Microspheres; D015394:Molecular Structure; D008970:Molecular Weight; D011100:Polyglycolic Acid; D000077182:Polylactic Acid-Polyglycolic Acid Copolymer; D011108:Polymers / Q000737:chemistry; D013379:Substrate Specificity
chemical_list: D000935:Antifungal Agents; D004337:Drug Carriers; D006016:Glycolates; D011108:Polymers; D000077182:Polylactic Acid-Polyglycolic Acid Copolymer; D011100:Polyglycolic Acid; D019344:Lactic Acid; D000666:Amphotericin B; D005690:Galactose