Production of polycaprolactone nanoparticles with hydrodynamic diameters below 100nm.

Abstract

Cancer is a worldwide increasing burden and its therapy is often challenging and causes severe side effects in healthy tissue. If drugs are loaded into nanoparticles, side effects can be reduced, and efficiency can be increased via the enhanced permeability and retention effect. This effect is based on the fact that nanoparticles with sizes from 10 to 200nm can accumulate in tumor tissue due to their leaky vasculature. In this work, we produced polycaprolactone (PCL) in the sizes 1.8, 5.4, and 13.6kDa and were able to produce spherical shaped nanoparticles with mean diameters of 64 ± 19nm out of the PCL5.4 and 45 ± 8nm out of the PCL13.6 reproducibly. By encapsulation of paclitaxel the diameter of that nanoparticles did not increase, and we were able to encapsulate 73±7fmol paclitaxel per 1000particles in the PCL5.4-nanoparticles and 35±8fmol PTX per 1000 PCL13.6-nanoparticles. Furthermore, we coupled the aptamer S15 to preformed PCL5.4-nanoparticles resulting in particles with a hydrodynamic diameter of 153nm. This offers the opportunity to use these nanoparticles for targeted drug delivery.