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

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 formu-lations 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 mu g/ml was observed in PC-3 cells and 25.43 mu g/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.