Journal de bioéquivalence et de biodisponibilité

Abstrait

Artesunate Loaded Self Nanoemulsified Drug Delivery System: A Preliminary Study for Improved Efficacy in the Treatment of Malaria: Formulation, Characterization and Bio-Distribution Study

Suresh Kumar R

The current study focused on formulation and evaluation of Artesunate loaded Self Nanoemulsified Drug Delivery System (SNEDDS). The research oriented towards the establishment of the pharmacokinetic parameters and biodistribution of Artesunate for SNEDDS. Artesunate nanoemulsion were developed using lipid, surfactant and Co Surfactant respectively (Capryol 90, Cremophor EL and Ethanol) by Spontaneous emulsification method. The investigation includes various characterization studies viz., particle size distribution, poly dispersibility index, zeta potential, viscosity, refractive index, % transmission and conductivity. The results were found to be 110.4 nm, 0.386, -36.6 mV, 19.54 cps, 1.287, 100, 367.2 μS/cm respectively with the optimized formulation 5. The in vitro drug release of Artesunate from SNEDDS formulation for was extremely significant when compared to pure drug suspension and the marketed formulation. The maximum release of drug from SNEDDS, marketed formulation and pure drug suspension was 98.78%, 62.78% and 20.88% respectively. The pharmacokinetic parameters of Cmax, AUC(0- 2 h), AUC(0-∞), Kel, Tmax and MRT were found to be 2467 ± 11.98 ng/ml, 1278 ± 0.18 h.ng/ml, 3278 ± 0.78 h.ng/ml, 1.04 ± 0.07 h-1, 1.0 h and 1.87 ± 0.01 h, respectively. From biodistribution studies the concentration of dihydroartemisinin (metabolite of Artesunate) was found to be maximum in the order of liver>lung>kidney>spleen>brain>heart. The highest concentration of 1951.8 ng/g was found to be in the liver.