DESIGN, DEVELOPMENT AND OPTIMIZATION OF LETROZOLE NANOPARTICLES FOR BREAST CANCER TREATMENT

Abstract

The objective of the present research work was to design, develop and optimize Letrozole loaded polymeric nanoparticles in order to potentially 
maximize the therapeutic efficiency, to decrease toxicity as well as to minimize the drug side effects. Pectin and Tween 80 were used as polymer and 
surfactants respectively. Letrozole polymeric nanoparticles (LTZ-PNPs) were prepared by precipitation method. The drug - polymer compatibility was 
studied using Fourier Transform Infrared (FTIR) and Differential Scanning Microscopy (DSC). The formulations’ optimization was done by design 
expert. The drug content (DC) and entrapment efficiency (EE) of nanoparticles (NPs) were evaluated by UV-Vis microscopy. The particle size of NPs 
were investigated using dynamic light scattering technique. The Franz diffusion cell was used for In-Vitro drug release studies. Accelerated stability 
studies were performed as per ICH guidelines. FTIR and DSC studies revealed compatibility between Letrozole and pectin. The DC was found to be 
uniform within all formulations (95%) and 96.87 % for the optimized formulation (F9). The E.E was found to be in the range of 68.87 to 95.11%. The 
NPs particle size was between 194 nm and 333 nm; F9 showed the particle size of 218.5 nm. Drug release from all formulated NPs followed non - 
fickian transport, thus the release mechanism was diffusion. The optimized formulation did not show a large variation in DC and EE when stored at 40 
°C/75% RH as per ICH guidelines.