scholarly journals 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

Pharmaceutics ◽  
2021 ◽  
Vol 13 (8) ◽  
pp. 1290
Author(s):  
Rathapon Asasutjarit ◽  
Nawarat Sooksai ◽  
Adryan Fristiohady ◽  
Kriyapa Lairungruang ◽  
Shiow-Fern Ng ◽  
...  

Andrographolide (AG) is an active compound isolated from Andrographis paniculata (Family Acanthaceae). Although it possesses beneficial bioactivities to the skin, there is insufficient information of its applications for treatment of skin disorders due to low water solubility leading to complications in product development. To overcome the problem, an AG-loaded nanoemulsion (AG-NE) was formulated and prepared using a microfluidization technique. This study aimed to investigate the effect of pressure and the number of homogenization cycles (factors) on droplet size, polydispersity index and zeta potential of AG-NE (responses) and to determine the effect of AG-NE on skin cancer cells and UVB irradiation-induced skin disorders in rats. Relationships between factors versus responses obtained from the face-centered central composite design were described by quadratic models. The optimum value of parameters for the production of optimized AG-NE (Op-AG-NE) were 20,000 psi of pressure and 5 homogenization cycles. Op-AG-NE showed promising cytotoxicity effects on the human malignant melanoma- (A375 cells) and non-melanoma cells (A-431 cells) via apoptosis induction with a high selectivity index and also inhibited intracellular tyrosinase activity in the A375 cells. Op-AG-NE could reduce melanin index and healed UVB irradiation exposed skin. Op-AG-NE thus had potential for treatment of skin cancers and skin disorders from exposure to UVB radiation.

Molecules ◽  
2021 ◽  
Vol 26 (4) ◽  
pp. 816
Author(s):  
Tomasz Tuzimski ◽  
Anna Petruczynik ◽  
Barbara Kaproń ◽  
Anna Makuch-Kocka ◽  
Małgorzata Szultka-Młyńska ◽  
...  

Melanoma is a serious form of skin cancer that begins in cells known as melanocytes. While it is less common than the other forms of skin cancer, melanoma is more dangerous because of its ability to spread to other organs more rapidly if it is not treated at an early stage. The number of people diagnosed with melanoma has increased over the last few decades. The most widely used treatments include surgery, chemotherapy, and radiation therapy. The search for new drugs to treat various cancers is one of the most important challenges of modern scientific research. Some isoquinoline alkaloids found in different plant species have strong cytotoxic effects on various cancer cells. We tested the effect of isoquinoline alkaloids and extracts obtained from various parts of Mahonia aquifolium collected in various vegetation seasons on human melanoma cancer cells and our data indicated that investigated extract induced significant reduction in cell viability of Human malignant melanoma cells (A375), human Caucasian malignant melanoma cell line (G361), and human malignant melanoma cell line (SKMEL3 cancer cell lines in a dose- and time-dependent manner. Differences in cytotoxic activity were observed for extracts obtained from various parts of Mahonia aquifolium. Significant differences were also obtained in the alkaloids content and cytotoxic activity of the extracts depending on the season of collection of plant material. Our investigations exhibit that these plant extracts can be recommended for further in vivo experiments in order to confirm the possibility of their use in the treatment of human melanomas.


2019 ◽  
Vol 819 ◽  
pp. 139-144
Author(s):  
Nawarat Sooksai ◽  
Worapapar Treesuppharat ◽  
Sewan Theeramunkong ◽  
Rathapon Asasutjarit

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.


2018 ◽  
Vol 2 (1) ◽  
pp. 1-8 ◽  
Author(s):  
Yogi Udjaja

Skin cancer is an abnormal growth of human skin that can damage skin cells. By knowing the symptoms of skin cancer as early as posssible, it is helpful in preventing the spread of cancer cells and treatment. There are many factors that cause skin cancer, but in general the cause is exposure to ultraviolet rays from the sun.  Therefore, an expert system application is required to detect skin cancer.  By using backward chining and probalility methode; which data is in form of someone’s risk factor and clinical sympthoms, then the application will provide temporary diagnosis.  This application is built in an android platfrom because in its development android is more used than other platforms. The accuracy obtained from this application is 96.67%.


2009 ◽  
Vol 2 (1) ◽  
pp. 30-36 ◽  
Author(s):  
Motoki Terada ◽  
Chikara Ohnishi ◽  
Nobuhiro Ueno ◽  
Akio Shimizu ◽  
Michiyuki Kanai ◽  
...  

Molecules ◽  
2021 ◽  
Vol 26 (10) ◽  
pp. 2924
Author(s):  
Cláudia Camacho ◽  
Helena Tomás ◽  
João Rodrigues

The DACHPtCl2 compound (trans-(R,R)-1,2-diaminocyclohexanedichloroplatinum(II)) is a potent anticancer drug with a broad spectrum of activity and is less toxic than oxaliplatin (trans-l-diaminocyclohexane oxalate platinum II), with which it shares the active metal fragment DACHPt. Nevertheless, due to poor water solubility, its use as a chemotherapeutic drug is limited. Here, DACHPtCl2 was conjugated, in a bidentate form, with half-generation PAMAM dendrimers (G0.5–G3.5) with carboxylate end-groups, and the resulting conjugates were evaluated against various types of cancer cell lines. In this way, we aimed at increasing the solubility and availability at the target site of DACHPt while potentially reducing the adverse side effects. DNA binding assays showed a hyperchromic effect compatible with DNA helix’s disruption upon the interaction of the metallodendrimers and/or the released active metallic fragments with DNA. Furthermore, the prepared DACHPt metallodendrimers presented cytotoxicity in a wide set of cancer cell lines used (the relative potency regarding oxaliplatin was in general high) and were not hemotoxic. Importantly, their selectivity for A2780 and CACO-2 cancer cells with respect to non-cancer cells was particularly high. Subsequently, the anticancer drug 5-FU was loaded in a selected metallodendrimer (the G2.5COO(DACHPt)16) to investigate a possible synergistic effect between the two drugs carried by the same dendrimer scaffold and tested for cytotoxicity in A2780cisR and CACO-2 cancer cell lines. This combination resulted in IC50 values much lower than the IC50 for 5-FU but higher than those found for the metallodendrimers without 5-FU. It seems, thus, that the metallic fragment-induced cytotoxicity dominates over the cytotoxicity of 5-FU in the set of considered cell lines.


2017 ◽  
Vol 8 (3) ◽  
pp. e2638-e2638 ◽  
Author(s):  
Tong-Hong Wang ◽  
Chieh-Wen Chan ◽  
Jia-You Fang ◽  
Ya-Min Shih ◽  
Yi-Wen Liu ◽  
...  

RSC Advances ◽  
2015 ◽  
Vol 5 (1) ◽  
pp. 20-26 ◽  
Author(s):  
Hao Cheng ◽  
Chuanxi Wang ◽  
Zhenzhu Xu ◽  
Huihui Lin ◽  
Chi Zhang

Folic acid-conjugated nanocomposites with NIR fluorescence, water-solubility, and low toxicity are prepared and used as target-imaging agents for cancer cells.


2009 ◽  
Vol 19 (16) ◽  
pp. 4814-4817 ◽  
Author(s):  
Malgorzata Drag-Zalesinska ◽  
Julita Kulbacka ◽  
Jolanta Saczko ◽  
Teresa Wysocka ◽  
Maciej Zabel ◽  
...  

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