1. Activity and in vivo tracking of Amphotericin B loaded PLGA nanoparticles.
- Author
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Souza AC, Nascimento AL, de Vasconcelos NM, Jerônimo MS, Siqueira IM, R-Santos L, Cintra DO, Fuscaldi LL, Pires Júnior OR, Titze-de-Almeida R, Borin MF, Báo SN, Martins OP, Cardoso VN, Fernandes SO, Mortari MR, Tedesco AC, Amaral AC, Felipe MS, and Bocca AL
- Subjects
- Amphotericin B adverse effects, Amphotericin B therapeutic use, Animals, Antifungal Agents adverse effects, Antifungal Agents therapeutic use, Deoxycholic Acid adverse effects, Deoxycholic Acid therapeutic use, Drug Carriers pharmacokinetics, Drug Combinations, Drug Liberation, Lactic Acid pharmacokinetics, Materials Testing, Mice, Paracoccidioides drug effects, Paracoccidioides physiology, Paracoccidioidomycosis drug therapy, Polyglycolic Acid pharmacokinetics, Polylactic Acid-Polyglycolic Acid Copolymer, Safety, Succimer chemistry, Tissue Distribution, Amphotericin B chemistry, Amphotericin B pharmacology, Antifungal Agents chemistry, Antifungal Agents pharmacology, Deoxycholic Acid chemistry, Deoxycholic Acid pharmacology, Drug Carriers chemistry, Lactic Acid chemistry, Nanoparticles chemistry, Polyglycolic Acid chemistry
- Abstract
The development of biocompatible polymeric nanoparticles has become an important strategy for optimizing the therapeutic efficacy of many classical drugs, as it may expand their activities, reduce their toxicity, increase their bioactivity and improve biodistribution. In this study, nanoparticles of Amphotericin B entrapped within poly (lactic-co-glycolic) acid and incorporated with dimercaptosuccinic acid (NANO-D-AMB) as a target molecule were evaluated for their physic-chemical characteristics, pharmacokinetics, biocompatibility and antifungal activity. We found high plasma concentrations of Amphotericin B upon treatment with NANO-D-AMB and a high uptake of nanoparticles in the lungs, liver and spleen. NANO-D-AMB exhibited antifungal efficacy against Paracoccidioides brasiliensis and induced much lower cytotoxicity levels compared to D-AMB formulation in vivo and in vitro. Together, these results confirm that NANO-D-AMB improves Amphotericin B delivery and suggest this delivery system as a potential alternative to the use of Amphotericin B sodium deoxycholate., (Copyright © 2015 Elsevier Masson SAS. All rights reserved.)
- Published
- 2015
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