Self Nanoemulsifying drug delivery system for antimalarial artesunate: Formulation development, characterisation and biodistribution studies

 Dr. Raman Sureshkumar, Y. AnilRaju Sairatan

JSS College of Pharmacy,Ootacamund

(A constituent college of JSS University, Mysore)

Artesunate, a lipophilic antimalarial drug, has poor oral bioavailability due to hepatic first-pass metabolism. Artesunate nanoemulsion were developed using lipid, surfactant and Co Surfactant respectively (Capryol 90, Cremophor EL and Ethanol) by Spontaneous emulsification method. The aim of this investigation was to develop self nanoemulsifying drug delivery system(SNEDDS) for Artesunate and to assess the pharmacokinetic parameters and biodistribution. 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 15.95nm, 0.152, -1.19mV, 19.54cPs, 1.287, 100, 367.2μS/cm respectively with formulation 5. The in  vitro drug release from SNEDDS formulation for artesunate was extremely significant in comparison to the marketed formulation and pure drug suspension. A maximum release of 98.78%, 62.78% and 20.88% for artesunate, was observed with the SNEDDS, marketed formulation and pure drug suspension respectively. The pharmacokinetic parameters of Cmax, AUC (0–2h), AUC (0–∞), Kel, Tmax and MRT were found to be 2467 ± 11.98 ng mL-1,1278 ± 0.18 h ng mL-1, 3278 ± 0.78 h ng mL-1, 1.04 ± 0.07 h-1, 1.0 h and 1.87 ± 0.01 h, respectively. From biodistribution studies the concentration of Artesunate was found to be maximum in the order of liver > lung > kidney > spleen > brain > heart. The maximum concentration (1951.8 ng g-1) was found in the liver.

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