Novel Tamoxifen Citrate-Loaded Polymeric Nanoformulations for Improving Treatment and uses in medical applications: An In Vitro and In Vivo Study

Abstract

Tamoxifen citrate (TAM) is one of the most regularly used therapy in hormone receptor-positive breast cancer. Although it is a successful treatment, there is a problem with its bioavailability, accordingly this study was designed to improve TAM solubility and reduce its associated toxicity. TAM-Loaded poly (D, L-lactide –co- glycolide) nanostructure (TAM-loaded PLGA) has been synthesized and employed both in vitro and in vivo experiments. The blood hemolysis induced by TAM- loaded PLGA was 4.6 % at 200 µg mL^-1, indicating that this nano-construct led to increased red blood cell protection. DNA molecule integrity was assessed and results indicated that DNA strands were protected from destruction at 200 µg mL^-1. The antioxidant activity of TAM-loaded PLGA exceeded the pure TAM, it showed concentration-dependent scavenging action in the 100-200 µg mL^-1 range, with a maximum activity of 79.2% at 200 µg mL-1. Whereas pure TAM had a decrement of 60.57%. While the activity of positive control (Vit. C) was 92.12%. Finally, the safety of TAM-loaded PLGA was examined in vivo. The functions of the heart, liver, and kidney in male mice injected with TAM-loaded PLGA were detected. A histopathological investigation was also included. TAM-loaded PLGA offered better properties as a drug delivery system, nutritional supplements, and pharmaceutical products.