On the Preparation of Folate-modified Lipid Nanocapsules and Their Targeting Ability towards Breast Cancer Cells

• Main Authors: Yung-Lun Hsieh, 謝詠倫
• Other Authors: 何國川
• Format: Others
• Language: zh-TW
• Online Access: http://ndltd.ncl.edu.tw/handle/01593795705374234234

碩士 === 臺灣大學 === 高分子科學與工程學研究所 === 98 === In this study, lipid nanocapsules (LNCs) modified with folic acid (FA), denoted as folate-LNCs, were synthesized and their interactions with the folate receptors over-expressed on the surface of the breast cancer cells are discussed. The folate-LNCs were synthesized with the expectation of improving the targeting ability of LNCs towards the breast cancer cells. The LNCs were synthesized by the phase transition temperature method. During heating process, emulsion system changed from o/w and passed through the phase transitional zone to w/o/w. LNCs were produced by adding large amount of cooling water at the phase transitional zone. To synthesize folate-LNCs, the surface of the LNCs was first modified with a layer of 3-aminopropyltriethoxysilane (APTES) to generate amino groups on the surface of LNCs by condensation reaction. Thereafter, folic acid was conjugated to APTES-LNCs through the formation of the peptide bond by the N-hydroxysuccinimide ester of folic acid (NHS/DCC method) and amino group. The Si-O-C and C=O peaks in the FTIR spectrum were observed, indicating the folate-LNCs were successfully synthesized. Besides, the particle size increased from 10 to 40 nm after FA was conjugated to LNCs, evidenced by zeta-sizer and TEM. No aggregation was observed for the LNCs and folate-LNCs. In order to examine the biocompatibility of the folate-LNCs, the 3T3, fibroblast cells were cultured with various concentrations of folate-LNCs. It was found that the maximum tolerance concentration of the folate-LNCs to fibroblast cells was 55 μL/mL. On the other hand, the targeting ability of the folate-LNCs to the human breast cancer cells, BT-20, was examined by the flow cytometry and confocal microscopy techniques. The results showed that the targeting ability of the LNCs to breast cancer cells was improved by conjugating folic acid.