Solubilization and dissolution of tamoxifen-hydroxybutenyl cyclodextrin complexes

Area of Science:

• Pharmaceutical Sciences
• Drug Delivery Systems
• Physical Chemistry

Background:

• Tamoxifen is a widely used medication with limited aqueous solubility.
• Improving tamoxifen's solubility and dissolution is crucial for effective drug delivery and bioavailability.
• Cyclodextrins are known excipients for enhancing drug solubility.

Purpose of the Study:

• To investigate the effect of hydroxybutenyl-beta-cyclodextrin (HBenBCD) on tamoxifen base and tamoxifen citrate solubility and dissolution.
• To explore the influence of formulation and environmental factors on tamoxifen-HBenBCD complexation.
• To compare the dissolution profiles of tamoxifen base and tamoxifen citrate when complexed with HBenBCD.

Main Methods:

• Solubility studies in aqueous and organic media with and without HBenBCD.
• Investigation of pH and buffer effects on tamoxifen solubility.
• Preparation of tamoxifen:HBenBCD formulations, including liquid fill capsules.
• Dissolution testing of prepared formulations.

Main Results:

• HBenBCD significantly enhanced the solubility of both tamoxifen base and tamoxifen citrate.
• Solubility was influenced by medium pH and buffer composition.
• Dissolution studies confirmed effective solubilization across diverse tamoxifen:HBenBCD formulations.
• Complexation with HBenBCD enabled tamoxifen base to exhibit solubility and dissolution profiles comparable to tamoxifen citrate.

Conclusions:

• HBenBCD is a promising excipient for improving tamoxifen solubility and dissolution.
• The developed tamoxifen-HBenBCD formulations show potential for enhanced drug delivery.
• HBenBCD complexation offers a strategy to achieve consistent tamoxifen performance regardless of salt form.