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. 2022 Jul 11;27(14):4430.
doi: 10.3390/molecules27144430.

Formulation, Optimization, and Evaluation of Moringa oleifera Leaf Polyphenol-Loaded Phytosome Delivery System against Breast Cancer Cell Lines

Jecinta Wanjiru  1   2 , Jeremiah Gathirwa  2 , Elingarami Sauli  1 , Hulda Shaid Swai  1
Affiliations

Formulation, Optimization, and Evaluation of Moringa oleifera Leaf Polyphenol-Loaded Phytosome Delivery System against Breast Cancer Cell Lines

Jecinta Wanjiru et al. Molecules. .

Abstract

Moringa oleifera leaf polyphenols (Mopp) were encapsulated with phytosomes to enhance their efficacy on 4T1 cancer cell lines. The Mopp were extracted via microwave-assisted extraction. Moringa oleifera polyphenol-loaded phytosomes (MoP) were prepared with the nanoprecipitation method and characterized using the dynamic light scattering and dialysis membrane techniques. The in vitro cytotoxic and antiproliferative activity were investigated with the (3-[4,5-dimethylthiazol-2-yl]-2,5-diphenyltetrazole) MTT assay. Acute toxicity was assessed using Swiss albino mice. An MoP particle size of 296 ± 0.29 nm, −40.1 ± 1.19 mV zeta potential, and polydispersity index of 0.106 ± 0.002 were obtained. The total phenolic content was 50.81 ± 0.02 mg GAE/g, while encapsulation efficiency was 90.32 ± 0.11%. The drug release profiles demonstrated biphasic and prolonged subsequent sustained release. In vitro assays indicated MoP had a low cytotoxicity effect of 98.84 ± 0.53 μg/mL, doxorubicin was 68.35 ± 3.508, and Mopp was 212.9 ± 1.30 μg/mL. Moreover, MoP exhibited the highest antiproliferative effect on 4T1 cancer cells with an inhibitory concentration of 7.73 ± 2.87 μg/mL and selectivity index > 3. The results indicated a significant difference (p ≤ 0.001) in MoP when compared to Mopp and doxorubicin. The in vivo investigation showed the safety of MoP at a dose below 2000 mg/kg. The present findings suggest that MoP may serve as an effective and promising formulation for breast cancer drug delivery and therapy.

Keywords: Moringa oleifera; antiproliferation; breast cancer; natural nanoparticles; polyphenols.

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Conflict of interest statement

The authors declare no conflict of interests.

Figures

Figure 1
Figure 1
Total phenolic content of standard gallic acid (R2 values are a representation of the mean data set of n = 3.
Figure 2
Figure 2
The total phenolic content of Mopp before and after MoP complex formulation.
Figure 3
Figure 3
The average particle size and PDI of optimized MoP formulation.
Figure 4
Figure 4
Zeta potential of optimized MoP formulation.
Figure 5
Figure 5
FITR spectra of MoP (a), Mopp FTIR spectra (b), and phospholipids (c).
Figure 6
Figure 6
In vitro release profile of optimized MoP compared to free Mopp in phosphate-buffered saline pH 7.4 at 37 ± 0.5 °C (mean ± SD, n = 3).
Figure 7
Figure 7
Bioaccessibility comparison of Mopp and MoP after exposure to simulated gastrointestinal conditions.
Figure 8
Figure 8
CC50 (concentration of the drug that reduces cell viability by 50%) and IC50 (concentration that inhibits 50% of breast cancer cells) of doxorubicin (standard drug) and extract (Mopp and MoP) comparisons toward Vero cell lines and 4T1 cell lines.
Figure 9
Figure 9
Percentage cell inhibition comparison for MoP and doxorubicin at different dosages. Bars with different letters per concentration are significantly different (p < 0.05) according to Student’s t-test analysis.
See this image and copyright information in PMC

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