PROCESS OPTIMIZATION FOR PREPARATION OF LEFLUNOMIDE LOADED NANOSTRUCTURED LIPID CARRIERS FOR TOPICAL DELIVERY

Dr. Akanksha Patel*, Vibha Savaliya and Dr. Jaya Patel

ABSTRACT

Rheumatoid arthritis is a progressive and disabling autoimmune disease. It causes inflammation, swelling, and pain
in and around the joints and other body organs. Leflunomide is one of the diseases modifying anti-rheumatic drugs
that is considered effective in preventing irreversible damage associated with Rheumatoid arthritis. It is highly
lipophilic drug falling in class-II of Biopharmaceutical Classification System. Leflunomide containing
Nanostructured lipid carriers were proposed with a view to increase solubility and permeability leading to
increased bioavailability. There are different methods listed in literature to prepare NLC. This study was conducted
to develop simple single step method for development of Leflunomide containing NLC. Various approaches of hot
melt emulsification were tested. The hot melt emulsification technique employing high-speed homogeniser proved
to be the most capable one. It was further optimised for stirring speed, stirring time, order of addition and cooling
temperature. The dispersion was assessed for particle size, particle size distribution, %entrapment efficiency,
morphology using transmission electron microscope, and stability. The optimised batch presented spherical
particles with particle size of 155±11.393 nm with tight particle size distribution (PDI: 0.110±0.014) and stability
of 6 months. The %Entrapment efficiency was found to be 83.95±3.13%.

Keywords: Nanostructured lipid carriers, NLC, lipidic Nanoparticles, ophthalmic drug delivery, hot melt emulsification, Leflunomide, process optimization.