1. Fabrication of folic acid-conjugated pyrimidine-2(5H)-thione-encapsulated curdlan gum-PEGamine nanoparticles for folate receptor targeting breast cancer cells.
- Author
-
Kunjiappan, Selvaraj, Panneerselvam, Theivendren, Pavadai, Parasuraman, Balakrishnan, Vanavil, Pandian, Sureshbabu Ram Kumar, Palanisamy, Ponnusamy, Sankaranarayanan, Murugesan, Kabilan, Shanmugampillai Jeyarajaguru, Sundaram, Ganeshraja Ayyakannu, Tseng, Wei-Lung, and Kumar, Alagarsamy Santhana Krishna
- Subjects
- *
CELL membranes , *CURDLAN , *CELL receptors , *MEMBRANE potential , *FOLIC acid - Abstract
In this study 5-((2-((3-methoxy benzylidene)-amino)-phenyl)-diazenyl)-4,6-diphenyl pyrimidine-2(5H)-thione was synthesized. The pharmacological applications of pyrimidine analogs are restricted due to their poor pharmacokinetic properties. As a solution, a microbial exopolysaccharide (curdlan gum) was used to synthesize folic acid-conjugated pyrimidine-2(5H)-thione-encapsulated curdlan gum-PEGamine nanoparticles (FA-Py-CG-PEGamine NPs). The results of physicochemical properties revealed that the fabricated FA-Py-CG-PEGamine NPs were between 100 and 400 nm in size with a majorly spherical shaped, crystalline nature, and the encapsulation efficiency and loading capacity were 79.04 ± 0.79 %, and 8.12 ± 0.39 % respectively. The drug release rate was significantly higher at pH 5.4 (80.14 ± 0.79 %) compared to pH 7.2. The cytotoxic potential of FA-Py-CG-PEGamine NPs against MCF-7 cells potentially reduced the number of cells after 24 h with 42.27 μg × mL−1 as IC 50 value. The higher intracellular accumulation of pyrimidine-2(5H)-thione in MCF-7 cells leads to apoptosis, observed by AO/EBr staining and flow cytometry analysis. The highest pyrimidine-2(5H)-thione internalization in MCF-7 cells may be due to folate conjugated on the surface of curdlan gum nanoparticles. Further, internalized pyrimidine-2(5H)-thione increases the intracellular ROS level, leading to apoptosis and inducing the decalin in mitochondrial membrane potential. These outcomes demonstrated that the FA-Py-CG-PEGamine NPs were specificity-targeting folate receptors on the plasma membranes of MCF-7 Cells. [Display omitted] • Folate receptor encapsulated curdlan gum-PEGamine nanoparticles were fabricated. • Curdlan gum nanoparticles easy to modify their surface through ligands folic acid • Curdlan gum NPs potentially delivered into MCF-7 cancer cells via folate receptor. • The fabricated FA-Py-CG-PEGamine NPs showed improved anticancer activity. [ABSTRACT FROM AUTHOR]
- Published
- 2024
- Full Text
- View/download PDF