Formulation Optimization and Characterization of Solid Lipid Nanoparticles of Apixaban

Area of Science:

• Pharmaceutical Sciences
• Nanotechnology
• Drug Delivery

Background:

• Apixaban, an oral anticoagulant, has poor solubility and limited bioavailability (approx. 50%).
• Blood clotting disorders like deep vein thrombosis and pulmonary embolism are leading causes of mortality.
• These conditions often arise post-surgery or with oral anticoagulant therapy.

Purpose of the Study:

• To improve the solubility, bioavailability, and therapeutic efficacy of Apixaban.
• To develop Apixaban-loaded solid lipid nanoparticles (SLN) for enhanced drug delivery.

Main Methods:

• Solid lipid nanoparticles (SLN) were prepared using the hot-homogenization method.
• Glyceryl monostearate was selected as the lipid excipient due to high Apixaban solubility.
• Design of Experiments (DOE) software was used for optimization, with Box-Behnken design and ANOVA for analysis.

Main Results:

• The optimized formulation (F10) exhibited a particle size of 167.1 nm and an entrapment efficiency of 87.32%.
• Lyophilized F10 nanoparticles showed a particle size of 130 nm via SEM.
• The optimized SLN formulation was encapsulated in capsules for oral administration.

Conclusions:

• Solid lipid nanoparticles significantly improved Apixaban's solubility and bioavailability.
• The developed SLN formulation offers a sustained release profile, potentially reducing clotting-related complications.