作者: Stacy M Stephenson , Sandy Ni , Robert J Lee
DOI:
关键词: Liposome 、 Liposomal daunorubicin 、 Drug delivery 、 Cytotoxicity 、 Daunorubicin 、 Epidermoid carcinoma 、 Folate receptor 、 Pharmacology 、 Biology 、 Doxorubicin
摘要: Background The folate receptor (FR) is amplified in a wide variety of human tumors. Thus, targeting cytotoxic therapies to FR promising strategy for chemotherapy. Materials and methods FR-targeted liposomal daunorubicin (f-L-DNR) was compared non-targeted DNR (L-DNR) cellular uptake cytotoxicity FR-expressing cells. Liposomal retention evaluated liposomes loaded with either sodium citrate or ammonium sulfate as the trapping agent. determined by flow cytometry fluorometry measurements while 3-(4,5dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay. Results superior prepared using sulfate. Cellular f-L-DNR KB oral carcinoma cells, Chinese hamster ovary (CHO-FR-beta), KG-1 acute myelogenous leukemia cells were 9.4, 40, 4,6-fold higher than L-DNR, respectively. CHO-FR-beta 18 times 49 Both could be inhibited 1 mM folic acid. Conclusion FR-mediated delivery increases cytotoxicity. Therefore, therapeutic evaluation relevant animal models warranted.