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Preparation and Characterization of Nanoliposomes for the Entrapment of Bioactive Hydrophilic Globular Proteins
Published on: August 31, 2019
[Preparation of warangalone-loaded liposomes and its inhibitory effect on breast cancer cells]
Lianzhi Mao1, Huiping Liu2, Huahuan Liu1
1Department of Nutrition and Food Hygiene, School of Public Health, Southern Medical University, Guangzhou 510515, China.
Objective:
To prepare warangalone-loaded thermosensitive liposomes (WLTSL) and evaluate its inhibitory effect on breast cancer cells in vitro.
Methods:
MTT assay was used to assess the changes in proliferation of 3 breast cancer cell lines (MDA-MB-231, MCF7, and SKBR3) following treatment with warangalone, soy isoflavone and genistein. Colony-forming assay and wound healing assay was used to assess colony forming activity and migration of MDA-MB-231 cells treated with warangalone. The effect of warangalone on the expression of MMP2 and MMP9 in MDA-MB-231 cells was examined with Western blotting. The thermosensitive liposomes (TSL) and WLTSL were prepared using a thin film hydration method, and the morphology, size, encapsulation efficiency and stability of the prepared liposomes were characterized using transmission electron microscopy, dynamic light scattering scanning and UV spectrophotometry. MTT assay was used to examine the inhibitory effect of WLTSL on mouse breast cancer cells (4T1) in vitro.
Results:
Warangalone showed stronger anti-proliferation effects than soy isoflavones and genistein in the 3 human breast cancer cell lines and significantly inhibited colony formation by MDA-MB-231 cells. Treatment with warangalone significantly inhibited migration of the breast cancer cells and down-regulated the cellular expressions of MMP2 and MMP9. The prepared TSL and WLTSL presented with a homogeneous, irregular spherical morphology, with a mean particle size of 56.23±0.61 nm, a polymer dispersity index of 0.241±0.014, a Zeta potential of -40.40±0.46 mV, and an encapsulation efficiency was 87.68±2.41%. WLTSL showed a good stability at 4 ℃ and 37 ℃ and a stronger inhibitory effect than warangalone in 4T1 cells.
Conclusions:
Warangalone inhibits the proliferation, migration and invasion of breast cancer cells, and the prepared WLTSL possesses good physical properties and strong anti-breast cancer activity.
Insights
Warangalone inhibits breast cancer cell proliferation and migration. Warangalone-loaded thermosensitive liposomes (WLTSL) demonstrate enhanced anti-cancer activity and good stability for potential therapeutic applications.
Area of Science:
- Pharmacology and Nanotechnology
- Cancer Biology
- Drug Delivery Systems
Background:
- Breast cancer remains a significant global health challenge, necessitating novel therapeutic strategies.
- Warangalone, a natural compound, exhibits potential anti-cancer properties.
- Developing effective drug delivery systems can enhance the therapeutic efficacy of anti-cancer agents.
Purpose of the Study:
- To synthesize and characterize warangalone-loaded thermosensitive liposomes (WLTSL).
- To evaluate the in vitro anti-cancer effects of WLTSL on various breast cancer cell lines.
- To assess the physical properties and stability of the developed liposomal formulation.
Main Methods:
- Preparation of thermosensitive liposomes (TSL) and WLTSL via thin film hydration.
- Characterization of liposomes using dynamic light scattering, transmission electron microscopy, and UV spectrophotometry.
- In vitro evaluation of anti-proliferative, anti-migratory, and invasion inhibitory effects using MTT, colony-forming, and wound healing assays; MMP2/MMP9 expression analyzed by Western blotting.
Main Results:
- Warangalone demonstrated superior anti-proliferative effects compared to soy isoflavones and genistein.
- Warangalone significantly inhibited MDA-MB-231 cell migration and downregulated MMP2/MMP9 expression.
- WLTSL exhibited favorable physicochemical properties, including optimal size, high encapsulation efficiency (87.68±2.41%), and good stability, with enhanced inhibitory effects on 4T1 cells compared to free warangalone.
Conclusions:
- Warangalone effectively inhibits breast cancer cell proliferation, migration, and invasion.
- The developed WLTSL formulation possesses desirable physical characteristics and potent anti-breast cancer activity.
- WLTSL represents a promising nanocarrier for warangalone in breast cancer therapy.
