Nanoemulsion and Solid Nanoemulsion for Improving Oral Delivery of a Breast Cancer Drug: Formulation, Evaluation, and a Comparison Study

Abstract

Letrozole (LZ) is an aromatase inhibitor, which inhibits the formation of estrogens from androgens. Nanoemulsion is a liquid emulsion formulation utilized to increase solubility, bioavailability, and drug delivery to cancer cells. This study aims to improve LZ oral delivery through formulating solid nanoemulsion (SNE). Peppermint oil, tween 80, and transcutol P were used as an oil, surfactant, and co-surfactant, respectively. The optimized nanoemulsion (NE-3) was then incorporated into solid polyethylene glycol (PEG) to formulate (SNE). The optimized (NE-3), SNE-2, and the available marketed tablet have been compared. The optimized (NE-3) was selected according to specific parameters of optimum small nano-size 80 nm, PDI of 0.181, the zeta potential of-98.2, high transmittance (99.78%), optimum pH (5.6), a high percent of LZ content (99.03 ± 1.90), the relatively low viscosity of 60.2 mPa.s, and a rapid release of LZ within 30 min. NE-3 was selected to be formulated as SNE. LZ's best release rate was 80% in 5 min with a content homogeneity of 99.85 ± 0.04 for SNE-2. Zero-order kinetics is determined to have the greatest R 2 values. Field emission scanning electron microscopy (FE-SEM) detected that SNE-2 was (36.75–96.64 nm) with a spherical form and no adhesion or aggregation. FT-IR showed no significant variations in position and shape of the absorption peaks between the pure drug and optimal formulation diagrams. This novel nanoemulsion technology aids in improving the solubility of poorly water-soluble drugs, particularly the SNE delivery method, which has a higher in-vitro release rate and expiration date of LZ than others.

Formulation of Piperine-Loaded Nanoemulsion: In Vitro Characterization, Ex Vivo Evaluation, and Cell Viability Assessment

“…The transparent nanoemulsion is thermodynamically stable if the globule diameter is between 100 and 200 nm. Therefore, the thermodynamic stability was assessed by analyzing the samples under various stress conditions (heating and cooling, centrifugation, and freeze-thaw cycles) . The prepared piperine nanoemulsions were evaluated for a heating and cooling cycle by keeping the sample at a high temperature (45 °C) and then transferring it to a cold temperature (4 °C).…”

Development of a Novel Methotrexate-Loaded Nanoemulsion for Rheumatoid Arthritis Treatment with Site-Specific Targeting Subcutaneous Delivery

“…For SEM analysis, samples were fixed in the sample holder with double-sided adhesive tape, and pictures were taken at a voltage of 5 kV. For TEM, samples were stained with a 2% phosphotungsticacid solution and then dried for 2 min before being viewed under an electron microscope at 100 kV [37,38].…”

Thermosensitive Hydrogels Loaded with Resveratrol Nanoemulsion: Formulation Optimization by Central Composite Design and Evaluation in MCF-7 Human Breast Cancer Cell Lines

“…Among the different nanotechnology approaches, nanoemulsions have proved to be very effective, due to their advantages, such as extensive surface area and stability, over other nanotechnology systems [ 23 , 24 ]. Recently, the potential of nanoemulsion in breast cancer therapy has also been demonstrated by various researchers [ 25 , 26 , 27 , 28 , 29 ]. Hence, in the current study, we aimed to utilize the advantages of nanoemulsion along with temperature-sensitive hydrogel delivery systems for the management of breast cancer.…”