Improved chemotherapeutic efficacy of injectable chrysin encapsulated by copolymer nanoparticles.
Chrysin is a flavone that is found in several plants and in honeycomb and possesses various biological activities. However, its low solubility means it has poor bioavailability, which must be resolved to enable its pharmaceutical applications. In the present study, chrysin was incorporated into methoxy poly(ethylene glycol)-β-polycaprolactone nanoparticles (chrysin-NPs) using the oil-in-water technique in order to overcome problems associated with chrysin. The properties of chrysin-NPs were analyzed, and their anticancer effects were investigated in vitro and in vivo. Chrysin-NPs were 77 nm sized (as determined by dynamic laser light scattering) and showed a monodisperse distribution. The zeta potential of chrysin-NPs was -2.22 mV, and they were spherically shaped by cryo-transmission electron microscopy (cryo-TEM). The loading efficiency of chrysin-NPs was 46.96%. Chrysin-NPs retained the cytotoxicity of chrysin in A549 cells. The therapeutic efficacies of chrysin-NPs were compared with those of chrysin in an A549-derived xenograft mouse model. Chrysin-NPs were intravenously injected at a 10 times lower dosage than chrysin 3 times per week (q2d×3/week). However, free chrysin was orally administrated 5 times per week (q1d×5/week). Chrysin-NP-treated group showed significant tumor growth delay, which was similar to that of chrysin-treated group, despite the considerably lower total dosage. These results suggest that the injectable chrysin-NPs enhance therapeutic efficacy in vivo and offer a beneficial formulation for chemotherapy.
College of Pharmacy; Innovative Drug Center, Duksung Women's University, Seoul, Republic of Korea.
Kyoung Mee
KM
Kim
College of Pharmacy; Innovative Drug Center, Duksung Women's University, Seoul, Republic of Korea.
Hyun Kyung
HK
Lim
College of Pharmacy; Innovative Drug Center, Duksung Women's University, Seoul, Republic of Korea.
Sang Hee
SH
Shim
College of Pharmacy; Innovative Drug Center, Duksung Women's University, Seoul, Republic of Korea.
Joohee
J
Jung
D000072283:A549 Cells; D000818:Animals; D000970:Antineoplastic Agents / Q000737:chemistry / Q000494:pharmacology / Q000627:therapeutic use*; D017209:Apoptosis / Q000187:drug effects; D016923:Cell Death / Q000187:drug effects; D049109:Cell Proliferation / Q000187:drug effects; D002626:Chemistry, Pharmaceutical; D004337:Drug Carriers / Q000737:chemistry; D065546:Drug Liberation / Q000187:drug effects; D005419:Flavonoids / Q000737:chemistry / Q000494:pharmacology / Q000627:therapeutic use*; D006801:Humans; D051379:Mice; D053758:Nanoparticles / Q000737:chemistry*; D011091:Polyesters / Q000737:chemistry*; D011092:Polyethylene Glycols / Q000737:chemistry; D012995:Solubility; D013696:Temperature
D000970:Antineoplastic Agents; D004337:Drug Carriers; D005419:Flavonoids; D011091:Polyesters; C016240:polycaprolactone; C043561:chrysin; D011092:Polyethylene Glycols
chemotherapeutic efficacy; chrysin; in vivo model; nanoparticle; non-small-cell lung cancer