Category: Micro- and Nanotechnologies

1195-A - Optimization and characterization of the PEGylated galactosylated primaquine phosphate (PQ) loaded nanostructured lipid carriers for the enhanced antimalarial efficacy.

Monday, February 5, 2018
2:00 PM - 3:00 PM

Primaquine (PQ), an 8-aminoquinoline antimalarial drug, is the only effective drug which acts on the latent hepatic forms of the malaria parasite and it also effective against the exoerythrocytic forms of all four of the malarial species that infect humans. The limitation associated with this drug is like low plasma half-life which in turn leads to frequent administration of the drug leading to dose related toxicity. Therefore, lipid based nano drug delivery systems have been very popular in the recent times as they are very less toxic, possess drug targeting capabilities and also reduce the dosing frequency by increasing efficacy of the drug. In the present study, PEGylated galactosylated primaquine phosphate (PQ) loaded nanostructured lipid carriers (NLC) were optimized using design of experiment with the help of Box-Behnken design. The optimized NLCs were evaluated for various physical and morphological characterizations, showing a particle size of 103.4±0.61 nm, PDI of 0.17±0.011, EE of 79.8±1.4 % and zeta potential of −37.9 ± 0.97 mV. A sustained release upto 72 h was observed for PQ-NLCs. The in vitro erythrocyte toxicity showed that PQ-NLCs were less toxic than the pure drug. In vitro parasite growth inhibition assay showed an IC50 value of 71.11±6.47ng/ml for the 3D7 P. falciparum (CQ sensitive) strain and 263.86±5.68 ng/ml for RKL9 P. falciparum (CQ resistant) strain for the PQ-NLCs. Enhanced parasitemia suppression of 99.46% at 2mg/kg/day, a better suppression of parasitemia of about 28% more than pure drug and a higher survivality rate of 66.66% even after the 35th day was observed for the PQ loaded NLC. Further, from the in vivo and ex vivo fluorescent imaging, it was clearly observed that the selective ASGP receptor based targeting of the galactosyted NLCs to the liver hepatocytes was possible where the hypnozoites resides. Hence, from the above observed results it can be clearly stated that the limitations of antimalarial drugs can be overcome with the help of nano lipid carriers.

Uday KRISHNA.. Baruah

Research Scholar
JSS COLLEGE OF PHARMCY,OOTY,INDIA
Ooty, Tamil Nadu, India

Uday Krishna Baruah, born on 6th December, 1987, is a Research Scholar from India pursuing doctorate in Pharmaceutical Science at JSS college of Pharmacy, Ooty under Jagadguru Sri Shivarathreeswara University, Mysuru, India. He completed his Masters of Pharmacy from the same college. He has been associated in the field of formulation and development of lipid based drug delivery systems for the last five years. His recent field of research interest is on the development of antimalarials loaded into lipid based nano drug delivery systems for the better and improved treatment of malaria by overcoming the limitations associated with the present antimalarial drugs. His recent publication is a review article titled ”Malaria treatment using novel nano based drug delivery systems’’ in the Journal of Drug Targeting(Vol. 25, Issue 7).