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Research Article

Preparation, Physicochemical Characterization and Anti-Fungal Evaluation of Amphotericin B-Loaded PLGA-PEG-Galactosamine Nanoparticles

Ghobad Mohammadi 1*, Mostafa Fathian-Kolahkaj 2, Pardis Mohammadi 1, Khosro Adibkia 3, Ali Fattahi 1

1 Pharmaceutical Sciences Research Center Health Institute, Kermanshah University of Medical Sciences, Kermanshah, Iran.
2 Student Research Committee, Kermanshah University of Medical Sciences, Kermanshah, Iran.
3 Faculty of Pharmacy, Tabriz University of Medical Sciences, Tabriz, Iran.

Abstract

Purpose: the present study aimed to formulate PLGA and PLGA-PEG-Galactosamine NPs loaded with amphotericin B with appropriate physicochemical properties and antifungal activity. PLGA was functionalized with GalN to increase the adhesion and antifungal activity of NPs against Candida albicans.
Methods: the physicochemical properties of NPs were characterized by particle size determination, zeta potential, drug crystallinity, loading efficiency, dissolution studies, DSC, XRPD, and FT-IR. Antifungal activity of the NPs at different drug/polymer ratios was examined by determining MICs.
Results: the FT-IR and 1HNMR analysis successfully confirmed the formation of PLGA- PEG-GalN NPs. The PLGA NPs were in the size range of 174.1 ± 3.49 to 238.2±7.59 nm while PLGA-GalN NPs were 255.6 ±4.08 nm in size, respectively. Loading efficiency was in the range of 67%±2.4 to 77%±1.6, and entrapment efficiency in the range of 68.185%±1.9 to 73.05%±0.6. Zeta potential and loading efficiency for PLGA-GalN NPs were –0.456, 71%. The NPs indicated an amorphous status according to XRPD patterns and DSC thermograms. The PLGA-PEG-GalN NPs showed higher fungistatic activity than PLGA NPs.
Conclusion: the results demonstrated that the antifungal activity of PLGA-PEG-GalN NPs was higher than pure amphotericin B and PLGA NPs.
Keywords: Amphotericin B, Candida Albicans, Galactosamine, PLGA, PEG, Nanoparticles
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Submitted: 14 May 2019
Revision: 11 Jul 2020
Accepted: 15 Jul 2020
ePublished: 15 Jul 2020
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