Development and in vitro evaluation of Letrozole loaded biodegradable nanoparticles for breast cancer therapy

Sanjoy Kumar Dey,Bivash Mandal,Manas Bhowmik,Lakshmi Kanta Ghosh

doi:10.1590/s1984-82502009000300025

Abstract

The objectives of our study were to prepare and evaluate a biodegradable nanoparticulate system of Letrozole (LTZ) intended for breast cancer therapy. LTZ loaded poly(lactide-co-glycolide) nanoparticles (LTZ-PLGA-NPs) were prepared by emulsion-solvent evaporation method using methylene chloride and polyvinyl alcohol. Percentage of drug (with respect to polymer) was selected as formulation variable. LTZ-PLGA-NPs were characterized by particle size, zeta potential, infrared spectra, drug entrapment efficiency and in vitro release. Sonication was done with an ultrasound pulse sonicator at 70 W, 30 kHz for 90 sec to produce stable NPs of mean size range from 64 nm to 255 nm with high entrapment efficiency (68% to 82%). Percentage of drug significantly influenced particle size, entrapment efficiency and release (p <0.05). The system sustained release of LTZ significantly and further investigation could exhibit its potential usefulness in breast cancer therapy.

Highlights

IntroductionBreast cancer is the second most common type of cancer after lung cancer. It is the primary cause of cancer death among women globally, responsible for about 40000 US women deaths in 2001 (James et al, 2002)
Worldwide, breast cancer is the second most common type of cancer after lung cancer
Since nanoparticles are formed from the emulsion droplets after organic solvent diffusion, their size is dependent on the stability of the emulsion droplets which is affected by miscibility of organic phase with water

Summary

Introduction

Breast cancer is the second most common type of cancer after lung cancer. It is the primary cause of cancer death among women globally, responsible for about 40000 US women deaths in 2001 (James et al, 2002). There was one published literature on Letrozole NPs prepared by direct precipitation technique (Mondal et al, 2008). These workers reported 146-267 nm particle size with very low entrapment efficiency (12-27%). Emulsification-solvent evaporation method is interesting for many reasons: the use of pharmaceutically acceptable organic solvents, high yields, good reproducibility, and easy scaling up (Nguyen et al, 2006) It is a very popular method because it mainly allows efficient encapsulation of numerous compounds of lipophilic nature (Song et al, 1997)

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