Controlled release of Capreomycin sulfate from pH-responsive nanocapsules

Abstract

The synthesis of polymeric nanocapsules loaded with the antituberculosis drug Capreomycin sulphate is presented in this work. The pHresponsive polymeric nanocapsules were successfully synthesized using the RAFT-based vesicle templating approach in the presence of Capreomycin sulphate. Anionic small polyelectrolytes comprising randomly distributed butyl acrylate and acrylic acid units were adsorbed on cationic vesicles of dimethyldioctadecyl ammonium bromide (DODAB). N,N-(dimethylamino)ethyl methacrylate (DMAEMA) and methyl methacrylate (MMA) or tertiary butyl methacrylate (tBMA) and MMA were used for the formation of the polymeric shells. Subsequently the tBMA was hydrolyzed to obtain negatively charged nanocapsules. The nanocapsule morphology for both approaches was characterized by DLS and TEM. The most stable hollow latex particles were obtained with the monomer composition of DMAEMA:MMA = 1:1. These nanocapsules were found to be colloidally stable and pH-responsive. The entrapment efficiency of drug determined by UV-Vis-spectroscopy was 70 %. The drug release rate from nanocapsules at pH 6.5 was found to be relatively fast (substantial release within one hour already), however we believe slower release can be achieved by using a thicker polymer shell.