Development of novel methotrexate-loaded nanocochleates for breast cancer targeting.

Abstract The objective of this research was to develop stable methotrexate(MTX) loaded nanocochleates (MTX-NC) drug delivery system to achieve controlled drug release,targeted delivery and enhanced anticancer potency with reduced dose and its effect on Breast cancer cell line. The development involved the loading of MTX to nanocochleates (MTX-NC) through conversion of phosphatidyl choline and cholesterol bearing liposome on addition of calcium ions and compared with MTX and MTX-NC. Optimized NC under optimized conditions showed particle size and zeta potential of 298.7nm and -12.9mv respectively, high entrapment efficiency 75%, drug loading of 37.5% and drug content 99%. Investigation on the drug lipid interaction using FTIR confirmed the compatibility of drug with the lipid carrier. SEM and TEM images of NC indicated that the particles were in a rod cylindrical shape with a smooth surface.Formulated MTX-NC demonstrated higher in-vitro anticancer activity in human breast cancer MCF-7 cells. The concentration of the drug needed for growth inhibition of was 47% for free MTX(80µg/ml) while it was -35.6% for the MTX-NC (80µg/ml) . Furthermore, the LC50 value of free MTX and MTX-NC was NE and 75.3µg/ml respectivelty.GI50 value of free MTX and MTX-NC was <10µg/ml. The results indicate that the MTX- NC has the potential to be applied for targeting anticancer drug delivery.