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Preparation and In vitro Evaluation of Efficacy and Toxicity of Polysorbate 80-coated Bovine Serum Albumin Nanoparticles containing Amphotericin B

[ Vol. 15 , Issue. 7 ]

Author(s):

Ligia Santos Pedroso, Najeh Maissar Khalil and Rubiana Mara Mainardes*   Pages 1055 - 1063 ( 9 )

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.

Keywords:

Amphotericin B, nanoparticles, bovine serum albumin, polysorbate-80, Cryptococcus neoformans, nanoencapsulation process.

Affiliation:

Pharmacy Department, Laboratory of Pharmaceutical Nanotechnology, Universidade Estadual do Centro-Oeste/ UNICENTRO, Simeão Camargo Varela de Sa Street 03, 85040-080 Guarapuava, PR, Pharmacy Department, Laboratory of Pharmaceutical Nanotechnology, Universidade Estadual do Centro-Oeste/ UNICENTRO, Simeão Camargo Varela de Sa Street 03, 85040-080 Guarapuava, PR, Pharmacy Department, Laboratory of Pharmaceutical Nanotechnology, Universidade Estadual do Centro-Oeste/ UNICENTRO, Simeão Camargo Varela de Sa Street 03, 85040-080 Guarapuava, PR

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