Shape mediated splenotropic delivery of buparvaquone loaded solid lipid nanoparticles

Area of Science:

• Nanotechnology
• Pharmacology
• Drug Delivery

Background:

• Theileriosis is a spleen-resident parasitic infection requiring targeted drug delivery.
• Current treatments may lack efficacy due to poor drug distribution.
• Developing effective splenotropic drug delivery systems is crucial.

Purpose of the Study:

• To develop and evaluate asymmetric Buparvaquone (BPQ)-loaded solid lipid nanoparticles (SLN) for splenotropic drug delivery.
• To assess the physicochemical properties, stability, and in vivo biodistribution of BPQ SLN.
• To investigate the potential of these nanoparticles for treating spleen-resident infections.

Main Methods:

• Asymmetric BPQ SLN were prepared using a modified nanoprecipitation method.
• Particle size, polydispersity index, entrapment efficiency, and drug loading were determined.
• Scanning electron microscopy (SEM) was used to analyze particle morphology.
• Hemolytic potential, serum stability, and 99mTc-radiolabeling efficiency were assessed.
• Biodistribution studies were conducted in mice following intravenous administration.

Main Results:

• BPQ SLN exhibited optimal particle size (650.28 nm), high entrapment efficiency (96.57%), and drug loading (24.63%).
• SEM revealed elongated asymmetric particles with an aspect ratio of 2.727.
• The nanoparticles demonstrated good serum stability, low hemolytic potential, and high radiolabeling efficiency (>95%).
• In vivo studies showed >75% accumulation in reticuloendothelial system organs, with a high spleen-to-liver ratio (up to 11.94).
• High splenic uptake was attributed to Kupffer cell bypass, particle rigidity, and low lipid molecular weight.

Conclusions:

• Asymmetric BPQ SLN are a viable splenotropic drug delivery system.
• The nanoparticles facilitate enhanced drug accumulation in the spleen.
• This system holds promise for improving the efficacy of theileriosis treatment.