4.2 Article

Evaluation of Oral Bioavailability and Anticancer Potential of Raloxifene Solid Lipid Nanoparticles

Journal

JOURNAL OF NANOSCIENCE AND NANOTECHNOLOGY
Volume 14, Issue 8, Pages 5638-5645

Publisher

AMER SCIENTIFIC PUBLISHERS
DOI: 10.1166/jnn.2014.8872

Keywords

Solid Lipid Nanoparticles; Raloxifene; Bioavailability; Efficacy; Breast Cancer Model

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The objective of the present investigation was formulation of raloxifene loaded solid lipid nanoparticles (R-SLN) for oral administration and evaluation of its anticancer potential in 7,12-dimethylbenzanthracene (DMBA)-induced breast cancer in Sprague-Dawley rats. Optimized R-SLN formulation prepared by modified micro-emulsion method resulted in R-SLN of 288.0 +/- 28.5 nm size and 95.56% entrapment efficiency. R-SLN exhibited in vitro prolonged release of raloxifene for 72 h in phosphate buffered saline. R-SLN was stable in simulated gastro-intestinal (GIT) fluids consisting of pH 1.2, pH 7.4, simulated gastric fluid and simulated intestinal fluid. A two-fold increase was observed in raloxifene oral bioavailability from R-SLN. R-SLN exhibited enhanced efficacy and chemopreventive activity over pure raloxifene as indicated by evaluation of tumor burden (P < 0.001) and tumor incidence (P < 0.001). The results indicate the potential of raloxifene solid lipid nanoparticles in optimizing chemoprevention of breast cancer by R-SLN.

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