FORMULATION AND CHARACTERIZATION OF GDL-BASED ARTESUNATE SOLID LIPID NANOPARTICLE

ANAMIKA JAIN; S. P. VYAS

doi:10.22159/ijap.2023v15i5.48913

Authors

ANAMIKA JAIN Drug Delivery and Research Laboratory, Department of Pharmaceutical Sciences, Dr. Harisingh Gour University, Sagar-470003, M. P., India https://orcid.org/0000-0002-0125-3400
S. P. VYAS Drug Delivery and Research Laboratory, Department of Pharmaceutical Sciences, Dr. Harisingh Gour University, Sagar-470003, M. P., India

DOI:

https://doi.org/10.22159/ijap.2023v15i5.48913

Keywords:

Malaria, RBCs, Glyceryldilaurate

Abstract

Objective: The present research aimed to prepare and characterize glyceryl dilaurate (GDL) containing solid lipid nanoparticles (SLN) with tween 80 and lecithin as an emulsifier in which the artesunate drug was loaded.

Methods: SLNs were synthesized by solvent emulsification–diffusion technique. The formulation was characterized for size, size distribution, zeta potential, shape and morphology, and DSC. In vitro drug release studies were performed at pH 5.0 and pH 7.4 to mimic in vivo conditions. Hemolytic studies and In vitro, antiplasmodial activities were carried out. Plasmodium berghei (NK65 resistant strain) infected mice were used to test the in vivo antimalarial efficacy of SLN.

Results: SLN exhibited 327 nm average sizes with 0.164 PDI and-23.4 mV zeta potential. TEM images revealed a spherical structure. The entrapment efficiency of the ART was calculated as 85.68%. In vitro, drug release studies showed that entrapped drug was released in a weakly acidic environment (83.45% for ART). Hemolytic studies revealed that ART-GDL conjugate was stable and safe for parenteral delivery. IC50 value of the GDL-based ART-SLNs was calculated to be 0.32 µM. Furthermore, the GDL-based ART-SLNs resulted in enhanced parasite killing in P. berghei-infected mice and improved survivability as compared to free ART administration.

Conclusion: The present research allows safe and effective intravenous administration of artesunate. Thus GDL-Based ART-SLNs could be a potential drug delivery system for antimalarial therapy.

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