Title:Primaquine Loaded Chitosan Nanoparticles For Liver Targeting
VOLUME: 1 ISSUE: 1
Author(s):Nidhi Gupta, Rampal Rajera, Manju Nagpal and Sandeep Arora
Affiliation:Chitkara College of Pharmacy, Chitkara University, Rajpura, Chandigarh-Patiala Highway, Punjab, India 140401.
Keywords:Chitosan, ionic gelation, liver targeting, malaria, nanoparticles, primaquine.
Abstract: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.
