Engineered Porous Beta-Cyclodextrin-Loaded Raloxifene Framework with Potential Anticancer Activity: Physicochemical...

Area of Science:

• Pharmaceutical Sciences
• Materials Science
• Oncology

Background:

• Breast cancer is a leading cause of mortality, particularly in women.
• Raloxifene, a selective estrogen receptor modulator, is used for breast cancer treatment but suffers from poor aqueous solubility.
• Beta-cyclodextrin-based nanosponges offer a novel approach to enhance the solubility and dissolution of poorly soluble drugs.

Purpose of the Study:

• To investigate the enhancement of solubility and dissolution rate of raloxifene using nanosponges.
• To evaluate the cytotoxic activity of raloxifene-loaded nanosponges against breast cancer cell lines.

Main Methods:

• Fabrication and optimization of cyclodextrin nanosponges crosslinked with diphenyl carbonate.
• Characterization of nanosponges using FTIR, PXRD, TEM, and SEM.
• In-vitro assessment of solubility, dissolution, and cytotoxicity on MCF-7 cells.

Main Results:

• Raloxifene-loaded nanosponges showed a particle size of 440±8.5 nm and a negative zeta potential.
• Significantly enhanced in-vitro dissolution behavior of raloxifene.
• Statistically significant in-vitro cytotoxicity of loaded nanosponges against MCF-7 cells compared to free raloxifene.

Conclusions:

• The developed nanosponges effectively improved raloxifene's solubility and dissolution.
• The incorporation of raloxifene into nanosponges enhanced its anticancer activity.
• Raloxifene-loaded nanosponges represent a promising nanocarrier for anticancer drug delivery.