Formulation, optimization and characterization of raloxifene hydrochloride loaded PLGA nanoparticles by using Taguchi design for breast cancer application

Multidrug resistance in breast cancer and the associated side-effects of anticancer therapies are significant hurdles in chemotherapy-based treatment. Biodegradable polymeric nano-based targeted drug delivery technologies showed tremendous advantages in targeted local delivery with limited off-targeted side effects. Therefore, there is a persistent need to develop targeted nanomedicine systems for treatment of breast cancer. The current research attempted to develop poly (lactic-co-glycolic acid) nanoparticles loaded with raloxifene by modified emulsification solvent diffusion evaporation method to improve oral bioavailability by using Taguchi design. It was observed that the optimized formulation (1:4 drug to polymer ratio) poly (lactic-co-glycolic acid) showed a mean particle size and Polydispersity index of 218 +/- 23.7 nm and 0.231 +/- 0.04, respectively. The entrapment efficiency was found to be 82.30% +/- 1.02%. In vitro drug delivery was found to be 92.5% +/- 1.48% in 40 h. The nanoparticles were to remain stable at 2 degrees C-8 degrees C even after 30 days. Differential scanning calorimetry and Fourier transform infrared spectroscopy characterization techniques showed that there was no interaction between the drug and excipient. Stability studies indicate that polymeric nanoparticles were stable at 2 degrees C-8 degrees C after 6 months. Raloxifene nanoparticles may be the most potent targeting moieties to treat highly invasive and metastatic MCF-7 breast cancer cells.

Automated summary

Multidrug resistance in breast cancer and associated side effects of anticancer therapies are major obstacles in chemotherapy-based treatment. Biodegradable polymeric nano-based targeted drug delivery technologies have shown significant advantages in targeted local delivery with minimal off-target side effects. Therefore, there is a continuous need for the development of targeted nanomedicine systems for breast cancer treatment. This study aimed to develop poly (lactic-co-glycolic acid) nanoparticles loaded with raloxifene to improve oral bioavailability. The optimized formulation showed desirable particle size, polydispersity index, and drug entrapment efficiency, and demonstrated stability during storage.