Bortezomib-loaded solid lipid nanoparticles: preparation, characterization, and intestinal permeability investigation

Area of Science:

• Pharmaceutical Sciences
• Drug Delivery Systems
• Nanotechnology

Background:

• Bortezomib (BTZ) is a proteasome inhibitor used for multiple myeloma and mantle cell lymphoma.
• BTZ exhibits limited intestinal permeability, hindering oral administration.
• Solid lipid nanoparticles (SLNs) are investigated as a carrier system to enhance drug absorption.

Purpose of the Study:

• To develop and characterize bortezomib-loaded solid lipid nanoparticles (BTZ-SLNs).
• To evaluate the effect of SLNs on the intestinal permeability of BTZ.
• To assess the potential of BTZ-SLNs for improved oral drug delivery.

Main Methods:

• BTZ-SLNs were prepared using the hot oil-in-water emulsification method.
• Nanoparticles were characterized for physicochemical properties including particle size, surface charge, entrapment efficiency, and drug loading.
• In situ single-pass intestinal perfusion technique was employed to study intestinal permeability.

Main Results:

• BTZ-SLNs exhibited a mean particle size of 94.6 nm and a negative surface charge (-18 mV).
• Entrapment efficiency was 68.3% with a drug loading of 0.8%.
• BTZ-SLNs demonstrated a threefold higher effective permeability (Peff) compared to plain BTZ solution.

Conclusions:

• Solid lipid nanoparticles effectively encapsulate bortezomib.
• BTZ-SLNs significantly improve the intestinal permeability of bortezomib.
• This SLN formulation holds potential for enhancing oral bioavailability of bortezomib.