An Approach to Enhance Dissolution Rate of Tamoxifen Citrate

Abstract EN

We tested the solubility and dissolution of tamoxifen citrate to ascertain the optimal conditions for faster dissolution.

Using the solvent evaporation method and hydrophilic carriers, we formulated tamoxifen citrate (TC) that contained solid dispersions (SDs).

We increased the solubility and dissolution rate of TC with a solid dispersion system that consisted of polyethylene glycol (PEG-6000), beta-cyclodextrin (β-CD), and a combination of carriers.

Physicochemical characteristics of solubility (mg/ml) were found to be 0.987±0.04 (water), 1.324±0.05 (6.8pH PBS), and 1.156±0.03 (7.4 pH PBS) for F5 formulation, percentage yield was between 98.74 ± 1.11% and 99.06 ± 0.58%, drug content was between 98.06±0.58 and 99.06±1.10, and dissolution studies binary complex showed a faster release of TC as compared to a single polymer and pure drug.

Furthermore, thermal properties, physicochemical drug and polymer interaction, crystal properties, and morphology were determined using differential scanning calorimetry (DSC), infrared spectroscopy (FT-IR), X-ray differential studies, and scanning electron microscopy.

We used the same proportion of carrier concentrations of the formulations to calculate the solubility of TC.

Our results demonstrated that increased concentrations of β-C yielded an improved solubility of TC, which was two times higher than pure TC.

The uniformity in drug content was 97.99 %.

A quicker drug release occurred from the binary complex formulation as seen in the dissolution profile.

FTIR demonstrated an absence in the physicochemical interaction between the drug and carriers.

The drug was also found to be dispersed in the amorphous state as revealed by DSC and XRD.

The drug concentration did not vary during various storage conditions.

Our in vivo studies demonstrated that SD displayed significantly higher values of Cmax (p < 0.05) and AUC0-24 (p < 0.05) as compared to free TC.

Furthermore, Tmax in SD was significantly lower (p < 0.05), as compared to free TC.