Ligand Decorated Primaquine loaded Nanocarriers for Liver Targeting for Triggered Antimalarial Activity.

OBJECTIVE The aim of the current research to formulate a nano delivery system for effective delivery of primaquine for liver targeting to achieve the potential antimalarial activity. An objective of current development is to formulate a lactobionic acid conjugated polyphosphazene based nanodelivery of primaquine for liver targeting to distinguish antimalarial activity. METHOD The particle size, entrapment efficiency, in-vitro drug release pattern, hepatotoxicity, MTT assay, erythrocyte toxicity assay, histopathology study, HepG2 cell uptake study, antimalarial study, and organ-distribution was also carried out to estimate the activity and potential features of nanoparticle system. RESULTS The results obtained from the above analysis justify the efficiency and effectiveness of the system. The NMR studies confirm the conjugation pattern and the TEM represent the spherical morphological features of nanoparticles. The controlled release pattern from the in-vitro release study was observed and found to be 73.25% of drug release in 20 hrs and also found in nano-size range (61.6± 1.56 nm) by particle size analysis. SGOT level, SGPT, ALP, Parasitemia level of optimized drug-loaded PEGylated lactobionic acid conjugated polyphosphazene derivatized nanoparticles (FF) was found to lie in safe range showing that the formulation is non-toxic to the liver. Higher cell uptake on HepG2 cell lines of Primaquine drug-loaded PEGylated lactobionic acid conjugated polyphosphazene polymeric nanoparticles showed higher cell uptake on HepG2 cell lines as compared to the drug-loaded in PEGylated polyphosphazene polymeric nanoparticles and plain drug. Percentage cell viability of drug-loaded PEGylated lactobionic acid conjugated polyphosphazene derivatized nanoparticles was decreased with enhancing the concentration of prepared nanoparticle system accessed by MTT assay. CONCLUSION From the studies, it can be concluded that the optimized formulation of drug-loaded PEGylated lactobionic acid conjugated polyphosphazene derivatized nanoparticles showed high liver targeting, least toxicity to the liver, controlled release of the drug as well as higher antimalarial activity against hepatocytes in low dose and more effectively and can be treated as a potential candidate for antimalarial therapy.