Lycopene loaded polymeric nanoparticles for prostate cancer treatment: Formulation, optimization using Box-behnken design and cytotoxicity studies

Abstract Purpose Currently prostate cancer treatment consists of invasive techniques and synthetic drugs which have many harmful effects like hair loss, digestive problems and increased chance of infections. Hence, a need for developing safer cancer treatments with lesser side effects has come to light. Thus, a nanotechnology based formulation loaded with carotenoid lycopene was developed for safer prostate cancer treatment. Methods Lycopene was extracted and isolated from fresh tomatoes and encapsulated in the Eudragit RL100 nanoparticles (NPs) using nano-precipitation method. After optimization using Box-Behnken design (BBD), the formulation underwent scanning electron microscopy (SEM), Fourier transform infrared spectroscopy (FTIR), differential scanning calorimetry (DSC), and in-vitro drug release studies. Later, the cytotoxicity of the formulations was tested in-vitro against androgen sensitive LNCaP cells and androgen insensitive PC-3 prostate cancer cell lines respectively. Results The formulation optimized using BBD had an excellent encapsulation efficiency (%EE) of 91.84 ± 2.3% and optimum particle size of 62.10 ± 3.7 nm. A notable increase in cumulative drug release (%CDR) of 46.67 ± 0.2% was noted compared to 26.19 ± 1.0% of pure lycopene after 24 h. From the in-vitro cytotoxicity studies, an IC50 value of 10.036 μg/ml was observed in PC-3 cells and 25.43 μg/ml in LNCaP cell lines along with an obvious change in morphology after treatment with the prepared formulation for 24 h. Conclusion Thus an optimized formulation was obtained which had a very high %EE, optimum particle size required for passive targeting to the tumor site, a significant enhancement in the in-vitro drug release of Lycopene and a good anti-prostate cancer potential based on in-vitro cytotoxicity and morphology studies. Hence, this formulation might prove to be a fruitful aid in the war against prostate cancer.