title: MPEG-DSPE polymeric micelle for translymphatic chemotherapy of lymph node metastasis.
abstract: Lymph node metastasis is one of the major pathways for tumor formation and it is difficult to deliver chemotherapeutics at therapeutic concentrations to lymph node metastasis. This study prepared methyl poly(ethylene glycol)-distearoylphosphatidylethanolamine/doxorubicin (MPEG-DSPE/DOX) micelle for the treatment of lymph node metastasis. The MPEG-DSPE/DOX micelle prepared were of spherical morphology with a particle size of 20 ± 5 nm. The uptake rates of DOX and MPEG-DSPE/DOX micelle by A375 cells were 51.2% and 88.7%, respectively. The phagocytosis rate of MPEG-DSPE/Rhodamine B micelle by RAW264.7 cells was 17.2-fold lower than for Rhodamine B alone. After subcutaneous injection, MPEG-DSPE micelle underwent lymphatic absorption and accumulated in popliteal lymph nodes. MPEG-DSPE/DOX micelle significantly alleviated damage to the subcutaneous tissue of the injection sites compared with DOX alone. We established a model of nude mice bearing lymph node metastasis of A375 cells. After subcutaneous injection, the weights of both the popliteal and iliac lymph nodes of the MPEG-DSPE/DOX micelle group were significantly lower than in the saline and DOX groups. MPEG-DSPE/DOX micelle effectively killed the tumor cells in popliteal and iliac lymph nodes. In conclusion, MPEG-DSPE micelle is a promising drug delivery system for the treatment of lymph node metastasis.
authors.affiliation: Key Laboratory of Smart Drug Delivery, Department of Pharmaceutics, School of Pharmacy, Fudan University, 826 Zhangheng Road, Shanghai 201203, China.
authors.forename: Xue
authors.initials: X
authors.lastname: Li
authors.affiliation: Key Laboratory of Smart Drug Delivery, Department of Pharmaceutics, School of Pharmacy, Fudan University, 826 Zhangheng Road, Shanghai 201203, China.
authors.forename: Qing
authors.initials: Q
authors.lastname: Dong
authors.affiliation: Institute of Biomedical Engineering and Technology, Shanghai Engineering Research Center of Molecular Therapeutics and New Drug Development, Institutes for Advanced Interdisciplinary Research, East China Normal University, Shanghai 200062, China.
authors.forename: Zhiqiang
authors.initials: Z
authors.lastname: Yan
authors.affiliation: Key Laboratory of Smart Drug Delivery, Department of Pharmaceutics, School of Pharmacy, Fudan University, 826 Zhangheng Road, Shanghai 201203, China.
authors.forename: Weiyue
authors.initials: W
authors.lastname: Lu
authors.affiliation: National Population and Family Planning Key Laboratory of Contraceptive Drugs and Devices, Shanghai Institute of Planned Parenthood Research, Shanghai 200032, China.
authors.forename: Lingling
authors.initials: L
authors.lastname: Feng
authors.affiliation: Key Laboratory of Smart Drug Delivery, Department of Pharmaceutics, School of Pharmacy, Fudan University, 826 Zhangheng Road, Shanghai 201203, China.
authors.forename: Cao
authors.initials: C
authors.lastname: Xie
authors.affiliation: Key Laboratory of Smart Drug Delivery, Department of Pharmaceutics, School of Pharmacy, Fudan University, 826 Zhangheng Road, Shanghai 201203, China.
authors.forename: Zuoxu
authors.initials: Z
authors.lastname: Xie
authors.affiliation: Key Laboratory of Smart Drug Delivery, Department of Pharmaceutics, School of Pharmacy, Fudan University, 826 Zhangheng Road, Shanghai 201203, China.
authors.forename: Bingxia
authors.initials: B
authors.lastname: Su
authors.affiliation: Key Laboratory of Smart Drug Delivery, Department of Pharmaceutics, School of Pharmacy, Fudan University, 826 Zhangheng Road, Shanghai 201203, China. Electronic address: liumin@shmu.edu.cn.
authors.forename: Min
authors.initials: M
authors.lastname: Liu
mesh_terms: D000818:Animals; D000903:Antibiotics, Antineoplastic / Q000008:administration & dosage* / Q000493:pharmacokinetics / Q000627:therapeutic use*; D045744:Cell Line, Tumor; D004317:Doxorubicin / Q000008:administration & dosage* / Q000493:pharmacokinetics / Q000627:therapeutic use*; D016503:Drug Delivery Systems; D006801:Humans; D008198:Lymph Nodes / Q000378:metabolism*; D008207:Lymphatic Metastasis; D008264:Macrophages / Q000187:drug effects; D008297:Male; D051379:Mice; D008819:Mice, Nude; D008823:Micelles; D008863:Microspheres; D010316:Particle Size; D010587:Phagocytosis / Q000187:drug effects; D010714:Phosphatidylethanolamines; D011092:Polyethylene Glycols; D051381:Rats; D017208:Rats, Wistar
chemical_list: D000903:Antibiotics, Antineoplastic; D008823:Micelles; D010714:Phosphatidylethanolamines; C107570:polyethylene glycol-distearoylphosphatidylethanolamine; D011092:Polyethylene Glycols; D004317:Doxorubicin
keywords: Lymph node; MPEG-DSPE; Metastasis; Polymeric micelle