Pre-formulation Study of Tamoxifen and Excipients in Formulation of Nanoparticle Drug Delivery System

Abstract

The inactive ingredients (excipients) are integral to the pharmaceutical drug delivery system. If not selected intelligently and added without a proper scientific approach can lead to the instability of the active pharmaceutical ingredient (API), low therapeutic outcome, or untoward effects. In this investigation, pre-formulation studies were carried out to confirm that the excipients used in the preparation of the nanoparticles were compatible with tamoxifen. The high-performance liquid chromatography-ultra-violet assay, Fourier-transform infrared spectroscopy (FTIR), X-ray diffraction (XRD), and thermogravimetric analysis (TGA) of the stored preparation showed that the nanoparticles were stable, indicating that the ingredients were not reactive and compatible with each other. The tamoxifen drug content was above 98%. Also, the FTIR spectrum of the optimized and physical mixture showed that the API retained its major (1357.89 cm-1, 1589.34 cm-1, 1739.79 cm-, 12870.08 cm-1, and 3402.43 cm-1) characteristic peaks. The XRD confirmed that the drug is very well dispersed in amorphous form with no extraneous peaks. The TGA isotherm indicated that the melting point of the optimized formulation was 400 oC which is significantly higher than the pure tamoxifen, which is 150 oC. the TGA results indicated that the formulation is heat stable.