Development, characterization, and in vitro evaluation of tamoxifen microemulsions

Area of Science:

• Pharmaceutical Sciences
• Nanotechnology
• Oncology

Background:

• Tamoxifen citrate (TMX) is a key therapeutic agent for estrogen receptor (ER) positive breast cancer.
• Developing effective drug delivery systems for TMX is crucial for improving treatment efficacy and patient outcomes.
• Challenges in TMX delivery include bioavailability and targeted action.

Purpose of the Study:

• To design, characterize, and evaluate novel microemulsions (MEs) for enhanced Tamoxifen citrate (TMX) drug delivery.
• To assess the in vitro efficacy of TMX-loaded MEs against breast cancer cells.
• To explore the potential of these MEs for both ER-positive and ER-negative breast cancer treatment.

Main Methods:

• Rational development and characterization of microemulsions (MEs) using well-defined excipients.
• Loading of Tamoxifen citrate (TMX) into MEs at concentrations up to 20 mM.
• In vitro assessment of MEs' effect on estradiol-induced proliferation of MCF-7 breast cancer cells.

Main Results:

• Microemulsions exhibited nanometric mean size and long shelf-life stability.
• MEs loaded with 20 mM TMX achieved over 90% reduction in viable MCF-7 cells.
• Compositions with 10 mM TMX demonstrated a cytotoxic effect exceeding 70%.

Conclusions:

• The developed microemulsions are promising drug delivery systems for Tamoxifen citrate.
• These MEs significantly inhibit breast cancer cell growth in vitro, offering a potent therapeutic strategy.
• The findings support further investigation of these MEs as an alternative administration route for various breast cancer subtypes.