Amphotericin B loaded nanoemulsion: Optimization, characterization and in-vitro activity against L. donovani promastigotes

Vikram Mohanlal Prajapat; Mayur Aalhate; Anitha Sriram; Srushti Mahajan; Indrani Maji; Ujala Gupta; Diksha Kumari; Kuljit Singh; Nitin Pal Kalia; Kamal Dua; Sachin Kumar Singh; Pankaj Kumar Singh

doi:10.1016/j.parint.2023.102848

Amphotericin B loaded nanoemulsion: Optimization, characterization and in-vitro activity against L. donovani promastigotes

Parasitol Int. 2024 Jun:100:102848. doi: 10.1016/j.parint.2023.102848. Epub 2023 Dec 28.

Affiliations

¹ Department of Pharmaceutics, National Institute of Pharmaceutical Education and Research (NIPER), Hyderabad 500037, India.
² Infectious Diseases Division, CSIR- Indian Institute of Integrative Medicine, Jammu 180001, India; Academy of Scientific and Innovative Research (AcSIR), Ghaziabad 201002, India.
³ Department of Biological Science, National Institute of Pharmaceutical Education and Research (NIPER), Hyderabad 500037, India.
⁴ Discipline of Pharmacy, Graduate School of Health, University of Technology Sydney, Australia; Faculty of Health, Australian Research Centre in Complementary and Integrative Medicine, University of Technology Sydney, Ultimo, NSW 2007, Australia.
⁵ Faculty of Health, Australian Research Centre in Complementary and Integrative Medicine, University of Technology Sydney, Ultimo, NSW 2007, Australia; School of Pharmaceutical Sciences, Lovely Professional University, Phagwara 144411, Punjab, India.
⁶ Department of Pharmaceutics, National Institute of Pharmaceutical Education and Research (NIPER), Hyderabad 500037, India. Electronic address: pankajksingh3@gmail.com.

PMID: 38159836
DOI: 10.1016/j.parint.2023.102848

Abstract

The present work aimed to develop and evaluate AmB-loaded nano-emulsion (AmB-NE) which will augment the solubility of AmB and lead to enhanced anti-leishmanial activity. The composition of AmB-NE was optimized by systematic screening followed by DoE-extreme vertices mixture design. The optimized NE revealed mean droplet size and PDI of 44.19 ± 5.5 nm, 0.265 ± 0.0723, respectively. The NE could efficiently encapsulate AmB with drug content and efficiency 83.509 ± 0.369% and 81.659 ± 0.013%, respectively. The presence of cholesterol and stearyl amine retarded the release (P < 0.0001) of AmB significantly compared to AmB suspension. The AmB-NE and pure AmB suspension demonstrated the IC₅₀ of 0.06309 μg/mL and 0.3309 μg/mL against L.donovani promastigotes after 48 h incubation. The formulation was robust at all exaggerated stability conditions such as freeze-thaw and centrifugation. These findings indicate that AmB-NE is an attractive approach to treat visceral leishmaniasis with improved activity.

Keywords: 1,8-cineol oil; Amphotericin B; Antifungal activity; Antileishmanial activity; Nanoemulsion.

MeSH terms

Amphotericin B / pharmacology
Animals
Antiprotozoal Agents* / pharmacology
Emulsions / pharmacology
Leishmania donovani*
Leishmania*
Leishmaniasis, Visceral* / drug therapy

Substances

Amphotericin B
Antiprotozoal Agents
Emulsions