Itraconazole-loaded poly(lactic-co-glycolic) acid nanoparticles for improved antifungal activity.
OBJECTIVE
Poly(lactic-co-glycolic) acid (PLGA) nanoparticles containing the hydrophobic antifungal itraconazole (ITZ) were developed to address the need for more effective means of treating fungal infections.


METHODS
PLGA-ITZ nanoparticles were synthesized using an oil-in-water emulsion evaporation method. Nanoparticle morphology (studied by transmission electron microscopy), size zeta potential (dynamic light scattering), encapsulation efficiency (UV-visible spectroscopy), release profile and antifungal activity were characterized.


RESULTS
PLGA-ITZ nanoparticles (of 220 nm in diameter) completely inhibited Aspergillus flavus growth over 11 days at 0.03 mg/ml ITZ; a similar effect was achieved at ×100 ITZ concentrations (3 mg/ml) in emulsified form. The ITZ in water formulation had the least antifungal effect, inhibiting growth for only 2 days at 3 mg/ml ITZ.


CONCLUSIONS
This system is envisioned to increase bioavailability of ITZ by improving aqueous dispersibility and increasing antifungal penetration, thereby increasing antifungal activity of the entrapped drug.
Patel
Nipur R
NR
Biological & Agricultural Engineering Department, Louisiana State University Agricultural Center, Baton Rouge, LA 70803, USA.
Damann
Kenneth
K
Leonardi
Claudia
C
Sabliov
Cristina M
CM
D000935:Antifungal Agents / Q000008:administration & dosage* / Q000494:pharmacology; D001231:Aspergillus flavus / Q000187:drug effects / Q000235:genetics / Q000254:growth & development; D049452:Green Fluorescent Proteins / Q000235:genetics; D017964:Itraconazole / Q000008:administration & dosage* / Q000494:pharmacology; D019344:Lactic Acid / Q000008:administration & dosage*; D008826:Microbial Sensitivity Tests; D046529:Microscopy, Electron, Transmission; D053758:Nanoparticles; D011100:Polyglycolic Acid / Q000008:administration & dosage*; D000077182:Polylactic Acid-Polyglycolic Acid Copolymer; D013056:Spectrophotometry, Ultraviolet
D000935:Antifungal Agents; D049452:Green Fluorescent Proteins; D000077182:Polylactic Acid-Polyglycolic Acid Copolymer; D011100:Polyglycolic Acid; D017964:Itraconazole; D019344:Lactic Acid