One platform comparison of solubilization potential of dendrimer with some solubilizing agents.

ABSTRACT

OBJECTIVE: To compare various solubilizing agents for their solubilizing propensity as well as effect of pH, concentration and time on solubility of a highly hydrophobic drug. MATERIALS AND METHODS: Dendrimers were synthesized by divergent method. Solubilization studies were carried out at different pH, concentration and time using Paclitaxel (PTX) as model drug. Hemolytic toxicity study was also performed. RESULTS: The solubility of PTX was increased with increasing concentration of solubilizing agents and the order of solubility enhancement effect of different solubilizing agents was found to be in the following order fifth generation (5.0 G) poly(propylene imine) (PPI) dendrimers > ß-CD > Tween 80 > polyethylene glycol 6000. The solubility of PTX was found to be highest at pH 5.0 followed by pH 7.4 than pH 9.2. The result of hemolytic toxicity studies displayed that when these solubilizing agents are given in combination with PTX, the toxicity was found to be reduced as compare to plain drug. CONCLUSIONS: The solubility of PTX was found to be significantly higher in the presence of 5.0 G PPI dendrimers as compared to the other solubilizing agents. It is also concluded that 5.0 G PPI dendrimers not only enhanced the solubility of PTX many folds but also reduced the toxicity of PTX.