An Approach to Enhance Dissolution Rate of Tamoxifen Citrate

Area of Science:

• Pharmaceutical Sciences
• Drug Delivery Systems
• Materials Science

Background:

• Tamoxifen citrate (TC) is a crucial pharmaceutical agent with limited solubility and dissolution rates, hindering its therapeutic efficacy.
• Developing advanced drug delivery systems is essential to overcome bioavailability challenges associated with poorly soluble drugs like TC.

Purpose of the Study:

• To formulate enhanced solid dispersions (SDs) of tamoxifen citrate (TC) using hydrophilic carriers to improve its solubility and dissolution characteristics.
• To investigate the physicochemical properties and in vivo performance of the developed TC-loaded SDs.

Main Methods:

• Tamoxifen citrate solid dispersions were prepared using the solvent evaporation method with hydrophilic carriers, including polyethylene glycol (PEG-6000) and beta-cyclodextrin (β-CD).
• Solubility, dissolution rate, drug content uniformity, and yield were evaluated.
• Physicochemical characterization involved differential scanning calorimetry (DSC), infrared spectroscopy (FT-IR), X-ray diffraction (XRD), and scanning electron microscopy (SEM). In vivo studies assessed pharmacokinetic parameters.

Main Results:

• Formulations with β-CD significantly increased TC solubility (up to two-fold higher than pure TC) and dissolution rate compared to single carriers or the pure drug.
• Characterization confirmed the amorphous state of the drug within the SDs and revealed no significant physicochemical interactions between TC and the carriers.
• In vivo studies showed significantly higher Cmax and AUC0-24, and a lower Tmax for the SD formulation compared to free TC, indicating improved bioavailability.

Conclusions:

• The developed solid dispersion system, particularly formulations incorporating beta-cyclodextrin, effectively enhances tamoxifen citrate solubility, dissolution, and in vivo absorption.
• This approach offers a promising strategy for improving the therapeutic potential of tamoxifen citrate and other poorly soluble drugs.