Title:Preparation and In vitro Evaluation of Efficacy and Toxicity of Polysorbate 80-coated Bovine Serum Albumin Nanoparticles containing Amphotericin B
Volume: 15
Issue: 7
Author(s): Ligia Santos Pedroso, Najeh Maissar Khalil and Rubiana Mara Mainardes*
Affiliation:
- Pharmacy Department, Laboratory of Pharmaceutical Nanotechnology, Universidade Estadual do Centro-Oeste/ UNICENTRO, Simeão Camargo Varela de Sa Street 03, 85040-080 Guarapuava, PR,Brazil
Keywords:
Amphotericin B, nanoparticles, bovine serum albumin, polysorbate-80, Cryptococcus neoformans, nanoencapsulation
process.
Abstract: Objective: In this study, bovine serum albumin (BSA) nanoparticles coated with polysorbate-
80 (PS-80) and containing amphotericin B (AmB) were developed using a coacervation method.
Methods: The nanoparticles were spherical, had a uniform size distribution (polydispersity < 0.25), a
small mean size (185 ± 5 nm), a high zeta potential (-38.0 ± 0.7 mV), and a high AmB encapsulation
efficiency (93 ± 1%). The AmB release profile was prolonged and diffusion-controlled, resulting in a
low degree of AmB aggregation in solution. The physicochemical characteristics of these AmB containing
nanoparticles were evaluated by X-ray diffraction, Fourier transform infrared spectroscopy, differential
scanning calorimetry, and derivative thermogravimetry and showed that the nanoencapsulation
process lead to AmB amorphization while maintaining its chemical integrity.
Results: In a hemolysis assay, AmB-loaded PS-80-coated BSA nanoparticles demonstrated an absence
of cytotoxicity toward erythrocytes, whereas pure and commercial AmB were highly hemolytic.
Conclusion: In an assay to assess antifungal activity against Cryptococcus neoformans, AmB-charged
PS-80-coated BSA nanoparticles were effective, however, due to the prolonged AmB release from the
nanoparticles, the MIC was higher than for pure or commercial AmB. PS-80-coated BSA nanoparticles
are potential carriers for the delivery of AmB for the treatment of Cryptococcus sp infections.
