SOLUBILITY ENHANCEMENT OF ANTICANCER (METHOTREXATE) BY USING PAMAM DENDRIMER AS A SOLUBILIZING AGENT

Abstract

Methotrexate (MTX) is an immunosuppressive medication used as an anticancer agent. Preformulation studies were carried out by identification test including Appearance (A bright yellow orange crystalline powder), Chemical test (Positive), Melting point (188-193C), Solubility profile (Insoluble in water, ethanol and chloroform, Soluble in methanol but freely soluble in dilute solution of Hydrochloric acid and Sodium hydroxide), Scanning of the drug (λmax was 304nm) I.R. Spectroscopy and prepared calibration curve by U.V Spectroscopy and HPLC method. Calibration curve of MTX in water was prepared by U.V.Spectroscopy and HPLC while in Biological sample and PBS was prepared by HPLC. PAMAM dendrimers (G4-NH2) 0.2% was used as a Solubilizing agent to solubilize MTX for the delivery of the drug. The effect of solvent, pH as well as temperature was calculated by HPLC method. In the Spectroscopical analysis of drug the λmax was shifted from 304 to 372.9.The transmittance of MTX shifted from 59.4 to 75.3 nm after the addition of G4-NH2 Dendrimer. The average particle size of MTX G4-NH2 dendrimer solubilized was 216.5 nm. 24.57% drug was in-vitro released in 24 hours. In the Pharmacokinetic study C_max was significantly higher than the pure drug.