Amphotericin B-Loaded Poly(Lactide)-Poly(Ethylene Glycol)-Blend Nanoparticles: Characterization and In Vitro Efficacy and Toxicity
Caroline Danziato Rodrigues,
Diani Meza Casa,
Luciana Facco Dalmolin,
Luciana Erzinger Alves de Camargo,
Najeh Maissar Khalil,
Rubiana Mara Mainardes.
In this study, we developed poly(lactide)-poly(ethylene glycol) (PLA-PEG) blend nanoparticles with variable molecular PEG
weights (2, 10, or 20 kDa) to encapsulate antifungal amphotericin B (AmB) and to evaluate its in vitro efficacy in strains of Candida sp.
and in vitro cytotoxicity in human erythrocytes. The nanoparticles were prepared using an emulsification/solvent evaporation technique
and were characterized with respect to size, size distribution, AmB entrapment efficiency, AmB state of aggregation, and AmB in vitro
release profile. The mean particle size was 241 nm, and AmB encapsulation efficiency was above 68.9%. The AmB in vitro release profile
demonstrated a burst effect within the first 24 h, which released approximately 20% of AmB, followed by a sustained release of approximately
29.5% of AmB over 26 days. The nanoparticles protected the erythrocytes from lysis caused by AmB within the first 12 h,
and AmB was efficacious against strains of Candida sp. in its sustained release profile. The PEG molecular weight did not demonstrate an effect
on the physicochemical and biological parameters. Thus, PLA-PEG blend nanoparticles may function as potential carriers for AmB.
Keywords: Amphotericin B, drug delivery, hemolysis, in vitro antifungal, polymeric nanoparticles.
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