title: Anti-tumor activity and safety evaluation of fisetin-loaded methoxy poly(ethylene glycol)-poly(epsilon-caprolactone) nanoparticles.
abstract: Fisetin (3,3',4',7-tetrahydroxyflavone) is a potential anti-tumor agent but poor water solubility hinders its application and complicates direct parenteral administration. Nanoparticle encapsulation is an efficient way to enhance the solubility of some hydrophobic drugs. In this study, methoxy poly(ethylene glycol)-polycaprolactone (MPEG-PCL) nanoparticles were successfully prepared for fisetin delivery in vitro and in vivo. Narrow distribution fisetin-loaded MPEG-PCL NPs (aproximately100 nm) were obtained via emulsification (O/W) and displayed a sustained release behavior in vitro. Moreover, hemolysis and cell cytotoxicity testing showed that MPEG-PCL is biocompatible and safe for intravenous injection. Most importantly, NPs encapsulation enhanced the anti-cancer activity of fisetin as shown in a subcutaneous LL/2 tumor model, and reduced the hepatotoxicity of fisetin. Therefore, our data demonstrate that fisetin-loaded MPEG-PCL NPs have potential application in cancer chemotherapy.
authors.forename: Qian
authors.initials: Q
authors.lastname: Yang
authors.forename: Jinfeng
authors.initials: J
authors.lastname: Liao
authors.forename: Xin
authors.initials: X
authors.lastname: Deng
authors.forename: Jian
authors.initials: J
authors.lastname: Liang
authors.forename: Chaofeng
authors.initials: C
authors.lastname: Long
authors.forename: Chengshi
authors.initials: C
authors.lastname: Xie
authors.forename: Xiaoxin
authors.initials: X
authors.lastname: Chen
authors.forename: Lan
authors.initials: L
authors.lastname: Zhang
authors.forename: Jinxin
authors.initials: J
authors.lastname: Sun
authors.forename: Jinrong
authors.initials: J
authors.lastname: Peng
authors.forename: Bingyang
authors.initials: B
authors.lastname: Chu
authors.forename: Gang
authors.initials: G
authors.lastname: Guo
authors.forename: Feng
authors.initials: F
authors.lastname: Luo
authors.forename: Zhiyong
authors.initials: Z
authors.lastname: Qian
mesh_terms: D000042:Absorption; D000818:Animals; D000970:Antineoplastic Agents / Q000008:administration & dosage / Q000009:adverse effects / Q000737:chemistry; D045744:Cell Line, Tumor; D004058:Diffusion; D005419:Flavonoids / Q000008:administration & dosage* / Q000009:adverse effects / Q000737:chemistry*; D044948:Flavonols; D007275:Injections, Intravenous; D008297:Male; D051379:Mice; D008810:Mice, Inbred C57BL; D053769:Nanocapsules / Q000008:administration & dosage* / Q000737:chemistry* / Q000648:ultrastructure; D009374:Neoplasms, Experimental / Q000188:drug therapy* / Q000473:pathology*; D010316:Particle Size; D011091:Polyesters / Q000737:chemistry*; D011092:Polyethylene Glycols / Q000737:chemistry*; D051381:Rats; D017207:Rats, Sprague-Dawley; D016896:Treatment Outcome
chemical_list: D000970:Antineoplastic Agents; D005419:Flavonoids; D044948:Flavonols; D053769:Nanocapsules; D011091:Polyesters; C439611:methoxy poly(ethylene glycol-co-epsilon-caprolactone); D011092:Polyethylene Glycols; C017875:fisetin