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

Chem Biol Drug Des. 2023 Sep;102(3):457-470. doi: 10.1111/cbdd.14222. Epub 2023 Mar 14.

Abstract

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°C-8°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°C-8°C after 6 months. Raloxifene nanoparticles may be the most potent targeting moieties to treat highly invasive and metastatic MCF-7 breast cancer cells.

Keywords: Pluronic-F127; Taguchi design; controlled release; nanoparticles.

MeSH terms

  • Breast Neoplasms* / drug therapy
  • Drug Carriers / chemistry
  • Female
  • Humans
  • Lactic Acid / chemistry
  • Nanoparticles* / chemistry
  • Particle Size
  • Polyglycolic Acid / chemistry
  • Polylactic Acid-Polyglycolic Acid Copolymer
  • Raloxifene Hydrochloride

Substances

  • Polylactic Acid-Polyglycolic Acid Copolymer
  • Raloxifene Hydrochloride
  • Drug Carriers
  • Polyglycolic Acid
  • Lactic Acid
  • glycolic acid