Abstract
Purpose: To enhance raloxifene (RLX) delivery and cytotoxicity against breast cancer (MCF-7) cell lines.
 Methods: This was a solubility study of RLX in different oils, surfactants, and co-surfactants. Twelve formulae were tested to reach the smallest globular size, and hydroxypropyl methylcellulose, (HPMC), and Carbopol 947 polymers were tested for formation of transdermal films. The formula with the lowest size was compared with raw RLX in diffusion studies using a Franz diffusion cell. Finally, a cytotoxicity study against MCF-7 breast cancer cell lines was conducted.
 Results: The maximum solubility of RLX was in Tween 80, peppermint oil, and PEG 200; therefore, these were the main components of the 12 formulations. The release of RLX loaded on the selfnanoemulsion drug delivery system (SNEDDS) was increased 3-fold compared with raw RLX.Cytotoxicity results revealed that RLX SNEDDs decreased MCF-7 cell survival by approximately 40 %, compared with raw RLX (control), which augmented the RLX suppression of breast cancer cell lines.
 Conclusion: Improvement in RLX cytotoxicity is a novel strategy to suppress breast cancer.
 Keywords: Raloxifene, Osteoporosis, Bioavailability, Nanoemulsion, Nanoparticles
Highlights
Raloxifene (RLX) is used to treat osteoporotic postmenopausal women and may lower the chances of acquiring certain types of breast cancers [1]
The purpose of this study was to improve RLX bioavailability through the use of self-nanoemulsion drug delivery systems (SNEDDS) stacked in a transdermal location to maintain a strategic distance from digestive processes [9]
We experimented with the oils to see which one has the highest solubility of RLX and found that the peppermint oil has the highest RLX solubility with a concentration of 1.69 mg/mL
Summary
Raloxifene (RLX) is used to treat osteoporotic postmenopausal women and may lower the chances of acquiring certain types of breast cancers (i.e., invasive breast cancer) [1]. RLX is not an oestrogen hormone, but it acts like oestrogen in some parts of the body. Oestrogen levels in the blood decrease, affecting bone cells and tissues. RLX acts like an oestrogen blocker [2]. RLX does not relieve menopausal symptoms such as hot flashes, as it belongs to a class of drugs known as selective oestrogen receptor modulators (SERMs). The main problem is to improve its low bioavailability (2%) resulting from excessive hepatic metabolism [3]
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