Effects of simvastatin-loaded polymeric micelles on human osteoblast-like MG-63 cells

Abstract

<p id="spar0015">To develop an optimized simvastatin (SV) delivery device for bone regeneration, SV-loaded poly(ethylene glycol)-poly(ɛ-caprolactone) (PECL) micelles were constructed. The micelles had an average size of 80&nbsp;nm. The <em>in vitro</em> release behavior of SV from the micelles showed prolonged release compared to the free SV. The following four groups were tested in a cytologic experiment: a free SV group, a SV-loaded micelle group with SV concentrations ranging from 2.5&nbsp;&times;&nbsp;10^&minus;6 to 2.5&nbsp;&times;&nbsp;10^&minus;10&nbsp;M, a drug-free micelle group and a blank control group. The effect of SV-loaded micelles on osteoblast-like MG-63 cells was determined <em>via</em> analysis of cell proliferation, alkaline phosphatase activity, and cell calcification. In addition, the mRNA and protein expression of the BMP-2 gene were determined with real-time fluorescence quantitative polymerase chain reaction and western blot techniques, respectively. The results show that SV-loaded PECL micelles cause effective suppression of the osteoblast early proliferation inhibition, stimulation of osteoblast differentiation and mineralization, and stimulation of the BMP-2 expression. Therefore, SV-loaded PECL micelles are predicted to have great potential in bone regeneration applications.</p><!--VALIDHTML--><hr /