Abstract: Lycopene has extensively been shown to inhibit tumor growth in nude mice bearing Breast. However, high tumor-suppressive Lycopene dosages encumber the development of oral controlled-release formulations because of a short biological half-life (< 2 h), poor absorption, low aqueous solubility, and extensive first-pass metabolism. Here, we present the design, fabrication, optimization, characterization, and biologicalevaluation of estrone-conjugated lycopene -loaded gelatin nanoparticles for targeting estrogen receptor- positive breast cancer MCF-7 cells. Gelatin nanoparticles (GN) were uniformly compact sized, stable at physiological pH, and showed good drug entrapment efficiency.