Volume 1 Issue 2
Antimalarial Activity of 2 -Aryl- 3H-indol-3-one Formulated in Albumin-based Nanosuspensions
Nambinina Rakotoarivelo, Nehal Ibrahim, Hany Ibrahim, Cendrine Cabou, Livia Vivas, Eloise Thompson,Jean-Pierre Nallet, Françoise Nepveu*, Alexis Valentin
Bioreducible indolone-N-oxides have demonstrated their potent antimalarial activities with, however, a short half-life. The deoxygenated analogues, 2-aryl-3H-indol-3-ones, a reduced chemical form obtained by synthesis, have similar antiplasmodial properties against the blood stages of Plasmodium falciparum in vitro, with, however, a low aqueous solubility in vivo. Albumin-based nanosuspensions were used to solubilize these new compounds to conduct experiments in vivo using the P. berghei ANKA murine model to determine the antimalarial activity of the most active derivative of this deoxygenated series, the 5-methoxy-2-(4- methoxyphenyl)-3H-indol-3-one (IND-1).
Tablet Formulation and Enhancement of Aqueous Solubility of Valsartan by Solvent Evaporation Co-Crystal Technique
Vikas G. Rajurkar*, Sanket S. Jangale, Vinayak K.Deshmukh, Vilas B. Ghawate, Amol R. Pawar,Prasad A.Kale
The enhancement of aqueous solubility, physicochemical and micromeritics properties of poorly soluble drugs is of major concern in pharmaceutical formulation industries. It is observed in the drug industry that on average more than 1/3 of newly drugs are poorly water-soluble. Poor “drug like” properties of lead compounds lead to ineffective absorption from the site of administration, less bioavailability which has been designated as an important part of the high clinical failure.