title: Reversal activity of nanostructured lipid carriers loading cytotoxic drug in multi-drug resistant cancer cells.
abstract: To overcome multi-drug resistance (MDR) of cancer cells, paclitaxel (PTX) and doxorubicin (DOX)-loaded nanostructured lipid carriers (NLC) were prepared by solvent diffusion method using monostearin as solid lipid and oleic acid as liquid lipid matrix. The cytotoxicities and reversal activity of drug-loaded NLC were tested against human breast cancer (MCF-7) cells, human ovarian cancer (SKOV3) cells and their multi-drug resistant (MCF-7/ADR and SKOV3-TR30) cells. The chemical conjugant of folic acid and stearic acid (FA-SA) was further synthesized to prepare folated NLC. Comparing with taxol and doxorubicin solution, the NLC loading PTX exhibited high cytotoxicities in MCF-7 and MCF-7/ADR cells, while the NLC loading DOX only indicated high cytotoxicity in MCF-7/ADR cells. The reversal powers of the NLC loading PTX and DOX were 34.3 and 6.4 folds, respectively. The NLC loading PTX and DOX showed the same trends of enhanced cytotoxicity against SKOV3 and SKOV3-TR30 cells. The reversal powers were 31.3 and 2.2 folds for the NLC loading PTX and DOX, respectively. The modification of NLC with FA-SA could further enhance the cytotoxicities of drug in drug sensitive and drug resistant cells.
authors.affiliation: Department of Pharmacology, First Affiliated Hospital, Zhejiang University School of Medicine, Hangzhou 310003, PR China.
authors.forename: Xing-Guo
authors.initials: XG
authors.lastname: Zhang
authors.forename: Jing
authors.initials: J
authors.lastname: Miao
authors.forename: You-Qin
authors.initials: YQ
authors.lastname: Dai
authors.forename: Yong-Zhong
authors.initials: YZ
authors.lastname: Du
authors.forename: Hong
authors.initials: H
authors.lastname: Yuan
authors.forename: Fu-Qiang
authors.initials: FQ
authors.lastname: Hu
mesh_terms: D000970:Antineoplastic Agents / Q000494:pharmacology*; D045744:Cell Line, Tumor; D004058:Diffusion; D004317:Doxorubicin / Q000494:pharmacology*; D004337:Drug Carriers / Q000737:chemistry*; D018432:Drug Resistance, Multiple; D019008:Drug Resistance, Neoplasm; D005492:Folic Acid / Q000737:chemistry; D005989:Glycerides / Q000737:chemistry; D006801:Humans; D049329:Nanostructures; D019301:Oleic Acid / Q000737:chemistry; D017239:Paclitaxel / Q000494:pharmacology*; D012997:Solvents; D013229:Stearic Acids / Q000737:chemistry
chemical_list: D000970:Antineoplastic Agents; D004337:Drug Carriers; D005989:Glycerides; D012997:Solvents; D013229:Stearic Acids; C048159:glyceryl monostearate; D019301:Oleic Acid; C031183:stearic acid; D004317:Doxorubicin; D005492:Folic Acid; D017239:Paclitaxel