https://scholars.lib.ntu.edu.tw/handle/123456789/539750
標題: | Cytotoxic enhancement of hexapeptide-conjugated micelles in EGFR high-expressed cancer cells | 作者: | WEN-JEN LIN Kao L.T. |
關鍵字: | Doxorubicin; EGFR; Hexapeptide; Micelles; Paclitaxel | 公開日期: | 2014 | 卷: | 11 | 期: | 10 | 起(迄)頁: | 1537-1550 | 來源出版物: | Expert Opinion on Drug Delivery | 摘要: | Objectives: The aim of this study was to develop the hexapeptide-conjugated active targeting micelles for delivery of doxorubicin (DOX) and paclitaxel (PTX) to EGFR high-expressed cancer cells.Methods: A hexapeptide, which mimicked the EGFR, was applied as a targeting ligand. The active targeting micelles were prepared using the synthesized poly(D,L-lactide-co-glycolide)-PEG copolymer conjugated with the hexapeptide. The micelles were used for encapsulating DOX and/or PTX, and the cellular uptake, in vitro drug release and cellular viability of drug-loaded peptide-conjugated and peptide-free micelles were investigated.Results: The particle size of drug-loaded peptide-conjugated and peptide-free micelles was < 150 nm with narrow size distribution. The uptake of peptide-conjugated micelles was more efficient in EGFR high-expressed MDA-MB-468 and SKOV3 cells than in EGFR low-expressed HepG2 cells. The in vitro release of DOX and PTX was faster in pH 4.0 (500 U lipase) than in pH 7.4 release medium. The cytotoxicity in terms of IC50of DOX/PTX-loaded peptide-conjugated micelles was 4.8-folds lower than that of peptide-free micelles and 18.2-folds lower than DOX/PTX drug solution in SOKV3 cells.Conclusion: The peptide-conjugated micelles acted as a nanocarrier to increase intracellular accumulation of anticancer drugs in EGFR high-expressed SKOV3 cancer cells to enhance cell cytotoxicity. ? 2014 Informa UK, Ltd. |
URI: | https://www.scopus.com/inward/record.uri?eid=2-s2.0-84907216808&doi=10.1517%2f17425247.2014.930433&partnerID=40&md5=412a7507a189364c098090f2d1d007e5 https://scholars.lib.ntu.edu.tw/handle/123456789/539750 |
ISSN: | 17425247 | DOI: | 10.1517/17425247.2014.930433 | SDG/關鍵字: | doxorubicin; epidermal growth factor receptor; hexapeptide; paclitaxel; polyglactin; antineoplastic agent; antineoplastic antibiotic; doxorubicin; drug carrier; EGFR protein, human; epidermal growth factor receptor; lactic acid; micelle; paclitaxel; polyglycolic acid; polylactic acid-polyglycolic acid copolymer; apoptosis; Article; cancer cell; cell viability; conjugate; drug cytotoxicity; drug delivery system; drug efficacy; drug half life; drug solubility; drug solution; encapsulation; endocytosis; endosome; enzyme linked immunosorbent assay; HepG2 cell line; human; human cell; hydrolysis; IC50; in vitro study; lysosome; micelle; multidrug resistance; particle size; pH; protein expression; receptor binding; sustained drug release; transmission electron microscopy; zeta potential; chemistry; metabolism; Neoplasms; tumor cell line; Antibiotics, Antineoplastic; Antineoplastic Agents, Phytogenic; Cell Line, Tumor; Doxorubicin; Drug Carriers; Humans; Lactic Acid; Micelles; Neoplasms; Paclitaxel; Particle Size; Polyglycolic Acid; Receptor, Epidermal Growth Factor |
顯示於: | 藥學系 |
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