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Nada Khudair

Qatar University, Qatar

Title: Non-ionic surfactant vesicles as delivery system for Letrozole

Biography

Biography: Nada Khudair

Abstract

Background: Aromatase is an enzyme that leads the bioconversion of androgen into estrogen, which is a main source for cell proliferation and growth in hormone dependent breast cancer. Letrozole (LTZ) is a third generation potent aromatase inhibitor that is approved by the Food and Drug Administration (FDA) for the management of hormone positive breast cancer. The current formulation (Femara®) lacks an effective bioavailability due to LTZ poor-water solubility and rapid systemic metabolism. Aim: To design and characterize LTZ powdered formulations using two formulation approaches; proniosomes and promicelles. Methods: Rotary evaporator apparatus was utilized to produce promicelles. A total of four formulations were prepared, each with a different drug to surfactant ratio. The formulations were prepared by slurry technique and loaded with LTZ. LTZ promicelles and the generated micelles were characterized using zetasizer, scanning electron microscopy (SEM), transmission electron microscopy (TEM) and ultra-performance liquid chromatography (UPLC). Results: Formulation (3) and (4) loaded with 20% LTZ (w/w) were found to be promising with a particle size of 7466±1145 nm and 8543±915 nm, respectively. The drug content was analyzed through UPLC and was found to be 93.45% and 74%, respectively. LTZ entrapment efficiency was reported highest in formulation (4) with a value of 97.5%. Finally, the images obtained from TEM revealed spherical micelles that were in the micro size, confirming the data from the zetasizer. Conclusion: The promicelles were successfully designed and characterized. Particles were spherical and in the micro size with a high entrapment efficiency, indicating improved physicochemical properties of LTZ.