Olanzapine liquisolid tablets using Kolliphor EL with improved flowability and bioavailability: in vitro and in vivo characterization

INTRODUCTION: Liquisolid method is an innovative and most emerging industrially useful approach to augment the rate of dissolution rate and thereby, bioavailability of therapeutic agents with poor aqueous solubility.
METHODS: The current research was intended to compare the bioavailability of formulated olanzapine liquisolid tablets with its marketed tablets (MT) by conducting pharmacokinetic and pharmacology methods. The present study also aimed at improving the flow properties of liquisolid tablets using Kolliphor EL as non-volatile solvent.
RESULTS: Pre-compression powders of all the formulations showed good to excellent flow property and compressibility. The drug release profiles of liquisolid tablets were contrasted with those of marketed tablets and directly compressible tablets (DCT). Formulation K250 was considered as optimized. The AUC0-∞ value of K250 was found to be 357.2±35.5 ng.h/mL which is higher than MT (258.4±29.9 ng.h/mL). The reduction in locomotor activity was enhanced remarkably in K250 compared with MT at p<0.05. The times taken to fall in rotarod test were approximately equal in all the groups which indicate the absence of extrapyramidal side effects. There was a remarkable decrease in the number of boxes covered in open field test.
DISCUSSION AND CONCLUSION: Kolliphor EL is a potential non-volatile solvent that can be used to produce liquisolid tablets of olanzapine with improved flow, compressibility, dissolution and bioavailability properties.