Preparation and characterization of ascorbic acid loaded solid lipid nanoparticles and investigation of their apoptotic effects

• Published in: Colloids and surfaces, B, Biointerfaces B, Biointerfaces, 2014-09, Vol.121, p.270-280
• Main Authors: Güney, Gamze, Kutlu, H. Mehtap, Genç, Lütfi
• Format: Article
• Language: English
• Subjects: Animals; Annexin A5 - metabolism; Apoptosis - drug effects; Apoptotic effect; Ascorbic acid; Ascorbic acid (AA); Ascorbic Acid - pharmacology; Cancer; Caspase 3 - metabolism; Cell Line, Tumor; Cell Survival - drug effects; Cellular; Computing time; Confocal; Cytotoxic activity; Homogenizing; Lipids; Lipids - chemistry; Mice; Microscopy, Confocal; Nanoparticles; Nanoparticles - chemistry; Nanoparticles - ultrastructure; Nanostructure; NIH 3T3 Cells; Particle Size; Propidium - metabolism; Rats; Reproducibility of Results; Solid lipid nanoparticles (SLNs); Static Electricity
• ISSN: 0927-7765; 1873-4367
• DOI: 10.1016/j.colsurfb.2014.05.008

Schematic illustration of the produced ascorbic acid (AA) loaded SLNs (AA-SLNs) and its anti-tumor efficacy on H-Ras 5RP7 cells. •We produced AA-SLNs formulation and were characterized by Nano Zetasizer and HPLC.•The apoptotic effects of AA-SLNs were determined by Annexin V-PI, caspase-3 assay.•The structural and ultrastructural effect of AA-SLNs showed by confocal and TEM.•AA-SLNs could greatly improve anticancer effects of AA.•SLNs can be a potential nanocarrier system for AA. In this paper, ascorbic acid (Vitamin C, AA) known as an antioxidant was successfully incorporated in solid lipid nanoparticles (SLNs) by hot homogenization and efficient delivery of AA to cancer cells. The obtained SLN formulations were characterized by Nano Zetasizer ZS and HPLC with the particle size being less than 250nm. AA-SLNs exhibited sustained release and high entrapment efficiency. According to MTT test results, AA-SLNs showed high cytotoxic activity compared to the free AA against H-Ras 5RP7 cells without damaging NIH/3T3 control cells. These results were supported by the Annexin V-PI and caspase-3 assay. Furthermore, as compared to the AA, AA-SLNs exhibited more efficient cellular uptake, accumulated in the cytoplasm and induced apoptosis which was observed by confocal laser scanning microscopy (CLSM) and transmission electron microscopy (TEM). Thus, the results of this study suggest that SLNs can be a potential nanocarrier system for AA.