Andrographolide-Loaded Nanoemulsion and its Activity against Non-Melanoma Skin Cancer Cells

Abstract

Andrographolide (AG) is a diterpenoid lactone found in Andrographis paniculata leaves and stems. It has excellent activity against various cancer cells, for example, skin cancer cells. However, application of AG for skin cancer treatment in clinical trials is limited due to its poor water solubility. To overcome this problem, oil in water AG-loaded nanoemulsion (AG-NE) would be prepared. The objectives of this study were to investigate physicochemical properties of AG-NE and to determine its activity against non-melanoma skin cancer cells. Nanoemulsion (NE) without AG (NE base) and NE containing AG (0.1%w/w) were prepared by high-pressure homogenization technique. They contained a mixture of Tween 80 and Span 80 (5:1) (10% w/w) as an emulsifier. Their droplet size, zeta potential and physical stability were evaluated. Cytotoxicity of AG and AG-NE to non-melanoma skin cancer cells (A-431 cells) and normal skin fibroblast cells (HFF-1 cells) were investigated. The results showed that NE base and AG-NE had droplet size in a nanometer range. They had low viscosity with the flow behavior consistent with Newtonian liquids. Although their zeta potential values were slightly low, they showed good physical stability against centrifugal force. AG and AG-NE were not toxic to HFF-1 cells, but they could induce apoptosis of A-431 cells with IC50 of 25.83 μg/ml and 58.32 mg/ml, respectively. Therefore, AG-NE has become possible to use for investigation of its efficacy and safety in animal models and clinical trials.

Andrographolide/Phospholipid/Cyclodextrin Complex-Loaded Nanoemulsion: Preparation, Optimization, <i>in Vitro</i> and <i>in Vivo</i> Evaluation

“…The process of AHPC-NE was optimized using CCD-RSM and AHPC-NE with excellent physicochemical properties were successfully prepared and characterized. Compared with the AG-loaded NE prepared by Sooksai et al, 39) AHPC-NE exhibited smaller droplet size and higher LC. Notably, the droplet size is critical to the efficacy of the NE.…”

Statistical modeling, optimization and characterization of andrographolide loaded emulgel for its therapeutic application on skin cancer through enhancing its skin permeability

“…At specific time intervals At specific time intervals (0, 1,2,3, 4, 5, 10, 15, 20, 24hrs), the samples (1 ml) were collected, and replaced simultaneously with fresh medium to maintain sink conditions. The samples were collected, appropriately diluted, and examined by a UV–visible spectrophotometer at 225 nm ( Sooksai et al, 2019 ). The optimized formulation ANG12 was further studied for release kinetics, particle size analysis, ex-vivo permeation, biocompatibility, cytotoxicity, cell cycle analysis, skin irritability, and in-vivo cellular uptake.…”

Optimization of Production Parameters for Andrographolide-Loaded Nanoemulsion Preparation by Microfluidization and Evaluations of Its Bioactivities in Skin Cancer Cells and UVB Radiation-Exposed Skin

“…The formulation of AG-NEs used in this study was based on the formulation of AG-NEs, which was previously reported with some modifications [ 4 ]. All AG-NEs contained the same compositions and were prepared by microfluidization technique.…”

“…To investigate the cytotoxic selectivity, a selectivity index (SI) of the test samples was determined by the following Equation (4): SI = IC50 of normal cells IC50 of cancer cells × 100 (4) where IC50 was a half-maximal inhibitory concentration of the test samples that induce fifty percentage of CV of the tested cells.…”

“…To date, the pharmacological activities of AG have been extensively investigated. This terpene-based compound exhibited strong bioactivities for treatment of various diseases, for example, diseases related to inflammation [ 2 ], viral and bacterial infection [ 1 ], central nervous system disorders [ 3 ], including cancers, e.g., leukemia, breast cancer and non-melanoma [ 1 , 4 , 5 ]. Recently, it has been found to be beneficial to the skin.…”