AUTHOR=Parvez Shabi , Yadagiri Ganesh , Karole Archana , Singh Om Prakash , Verma Anurag , Sundar Shyam , Mudavath Shyam Lal 

TITLE=Recuperating Biopharmaceutical Aspects of Amphotericin B and Paromomycin Using a Chitosan Functionalized Nanocarrier via Oral Route for Enhanced Anti-leishmanial Activity

JOURNAL=Frontiers in Cellular and Infection Microbiology

VOLUME=Volume 10 - 2020

YEAR=2020

URL=https://www.frontiersin.org/journals/cellular-and-infection-microbiology/articles/10.3389/fcimb.2020.570573

DOI=10.3389/fcimb.2020.570573

ISSN=2235-2988

ABSTRACT=The design and development of new pharmaceutical formulations for the existing anti-leishmanial is a new strategic alternate to improve efficacy and safety rather than new drug discovery. Herein hybrid solid lipid nanoparticles (SLN) have been engineered to direct the oral delivery of two anti-leishmanial drugs amphotericin B (AmB) and paromomycin (PM). The combinatorial nanocarriers consist of conventional SLN, antileishmanial drugs (AmB and PM) which have been functionalized with chitosan (Cs) grafted onto the external surface. The Cs-SLN have mean particle size of 373.9 ±1.41 nm, polydispersity index (PDI) of 0.342±0.02 and the entrapment efficiency for AmB and PM was found to be 95.20±3.19 % and 89.45± 6.86 % respectively. Characterization of SLN was performed by scanning electron microscopy and transmission electron microscopy. Complete internalization of the formulation was observed in Caco-2 cells. Cs-SLN have shown a controlled and slow drug release profile over a period of 72 hrs and was stable at gastrointestinal fluids, confirmed by in vitro simulated gastro-intestinal fluid study. Cs coating enhanced the mucoadhesive property of Cs-SLN. The in-vitro anti-leishmanial activity of Cs-SLN (1µg/ml) has shown a maximum percentage of inhibition (92.35% and 89% respectively) on intra-cellular amastigote growth of L. donovani.