Primaquine Loaded Chitosan Nanoparticles For Liver Targeting

Primaquine (PQ) loaded chitosan (CS) nanoparticles were prepared by ionic gelation technique using different concentrations of chitosan and sodium tripolyphosphate (TPP) and the potential of using these nanoparticles for liver targeting was investigated. Various factors such as concentration of chitosan and the amount of the cross-linking agent (TPP) were investigated to reveal their influences on the zeta potential, particle size, entrapment efficiency and in vitro release of the resulted nanoparticles. The formulation conditions were optimized to obtain a positive charged spherical nanoparticles with zeta potential of 29.0mV, polydispersity index of 0.213 and particle size in the range of 100-200nm. The entrapment efficiency of best batch of cross-linked chitosan nanoparticles encapsulated with primaquine (PQ-CS-NP) (i.e. 0.6mg/ml TPP into 0.1% chitosan solution) was found to be 93.21±0.17. It was observed that the in vitro release of primaquine from CS NPs was 96.52±0.54 within 24 h demonstrating sustained drug release effect. TEM showed that the prepared nanoparticles were smooth and spherical in shape. DSC and FTIR revealed no significant interactions between primaquine and CS after encapsulation and cross-linking. XRD data indicated that primaquine creates a non crystalline dispersion into the chitosan nanoparticles. The optimized batch of nanoparticles was tested in vivo to study the liver targeting effect. Primaquine loaded chitosan nanoparticles showed a much higher distribution of drug into liver as compared to that in blood. In comparison, primaquine solution showed lesser concentration in both liver and blood after IV administration into mice. The results concluded that chitosan nanoparticles were efficient carriers for the targeting of drug into liver.