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Raloxifene-Loaded Lipid Nanovesicles: A Journey to Select the Optimal Nanocarrier Formulation Through
Jana K ALwattar1, Mohammad Ahmad Assi1, Sahar Nasser1
1Department of Pharmaceutical Sciences, School of Pharmacy, Lebanese International University, Beirut P.O. Box 11-5020, Lebanon.
Biomedicines
|September 27, 2025
Summary
Raloxifene-loaded hexosomes demonstrate superior anticancer activity against breast cancer cells compared to other nanocarriers. Further studies are needed to confirm their therapeutic potential.
Area of Science:
- Nanotechnology in drug delivery
- Oncology
- Pharmacology
Background:
- Cancer is a leading global cause of death, with breast cancer being the most common in women.
- Raloxifene (RLX), a selective estrogen receptor modulator, is used for breast cancer treatment in postmenopausal women.
Purpose of the Study:
- To evaluate the anticancer efficacy of raloxifene-loaded hexosomes, nanoliposomes, and nanoniosomes.
- To identify the most effective nanocarrier formulation for raloxifene delivery.
Main Methods:
- Characterization of nanovesicles (particle size, zeta potential, entrapment efficiency).
- Assessment of cytotoxicity on MCF-7 breast cancer cells and MCF10 non-tumorigenic cells.
Main Results:
- All nanocarriers showed nanometric size, negative surface charge, and good encapsulation efficiency.
- Raloxifene-loaded hexosomes exhibited the most potent cytotoxic activity against MCF-7 cells (IC50 = 45.3 ± 1.10 µM).
Conclusions:
- Hexosomal formulation of raloxifene demonstrated superior cytotoxic effects compared to other nanovesicles.
- Further in vitro studies are required to elucidate the mechanisms and confirm the therapeutic potential of RLX-loaded hexosomes.

