Amphotericin B-loaded polymeric nanoparticles: formulation optimization by factorial design

Abstract

In this study, PLGA or PLGA-PEG blend nanoparticles were developed loading amphotericin B (AmB), an antifungal agent broadly used in therapy. A 2² × 3¹ factorial experimental design was conducted to indicate an optimal formulation of nanoparticles containing AmB and demonstrate the influence of the interactions of components on the mean particle size and drug encapsulation efficiency. The independent variables analyzed were polymer amount (two levels) and organic phase (three factors in one level). The parameters methanol as cosolvent and higher polymer amount originated from the higher AmB encapsulation, but with the larger particle size. The selected optimized parameters were set as the lower polymer amount and ethyl acetate as cosolvent in organic phase, for both PLGA and PLGA-PEG nanoparticles. These parameters originated from nanoparticles with the size of 189.5 ± 90 nm and 169 ± 6.9 nm and AmB encapsulation efficiency of 94.0 ± 1.3% and 92.8 ± 2.9% for PLGA and PLGA-PEG nanoparticles, respectively. Additionally, these formulations showed a narrow size distribution indicating homogeneity in the particle size. PLGA and PLGA-PEG nanoparticles are potential carrier for AmB delivery and the factorial design presented an important tool in optimizing nanoparticles formulations.

• Antifungal
• encapsulation efficiency
• nanoencapsulation
• particle size
• polydispersity index

Declaration of interest

The authors state no conflict of interest in this study.

The authors thank to CNPq (process 476071/2009-7 and 478020/2012-0) and Fundação Araucária (conv. 176/2012) for financial support.