Highly efficient release of lovastatin from poly(lactic-co-glycolic acid) nanoparticles enhances bone repair in rats.

Lovastatin exhibits higher thermal stability and lower degradation rate than simvastatin. However, the amount of research studying a lovastatin delivery device has been far less than similar research on simvastatin. As a consequence, a high lovastatin release rate system has not been developed. We hypothesized that highly efficient release of lovastatin from poly(lactic-co-glycolic acid) (PLGA) nanoparticles in a short-term release (7 days) could provide an effective delivery system for bone repair. This study optimized the emulsion (o/w) technique in the fabrication process for PLGA nanoparticles, thereby producing the first recorded case of a high release rate (97%) of lovastatin. We also calculated the calibration curve of lovastatin using a UV spectrometer. The results demonstrated that the ALPase activity in human osteoblasts could be significantly stimulated by lovastatin carried in PLGA nanoparticles, but was prominently decreased by free lovastatin with the concentration higher than 4 µg/ml. Animal studies showed that the amount of lovastatin contained in 1 mg PLGA was the optimum dosage. These results suggest the new lovastatin-releasing PLGA delivery device exhibits potential for clinical treatment of bony defects.