title: Effect of hydrophobicity of core on the anticancer efficiency of micelles as drug delivery carriers.
abstract: Recently, micelles, which are self-assembled by amphiphilic copolymers, have attracted tremendous attention as promising drug delivery systems for cancer treatment. Thus, the hydrophobic core of the micelles, which could efficiently encapsulate small molecular drug, will play a significant role for the anticancer efficiency. Unfortunately, the effect of hydrophobicity of micellar core on its anticancer efficiency was rarely reported. Herein, the amphiphilic diblock polymers of poly(ethylene glycol) and polyphosphoester with different side groups (butyl, hexyl, octyl) were synthesized to tune the hydrophobicity of the micellar core. We found that the in vitro cytotoxicity of the DOX-loaded micelles decreased with the increasing hydrophobicity of micellar core due to the drug release rate. However, following systemic delivery, the DOX-loaded micelles with the most hydrophobic core exhibited the most significant inhibition of tumor growth in a MDA-MB-231 tumor model, indicating the importance of hydrophobicity of core on the antitumor efficacy of drug delivery systems.
authors.affiliation: Department of Medical Materials and Rehabilitation Engineering, School of Medical Engineering, Hefei University of Technology , Hefei, Anhui 230009, China.
authors.forename: Chun-Yang
authors.initials: CY
authors.lastname: Sun
authors.forename: Yin-Chu
authors.initials: YC
authors.lastname: Ma
authors.forename: Zi-Yang
authors.initials: ZY
authors.lastname: Cao
authors.forename: Dong-Dong
authors.initials: DD
authors.lastname: Li
authors.forename: Feng
authors.initials: F
authors.lastname: Fan
authors.forename: Jun-Xia
authors.initials: JX
authors.lastname: Wang
authors.forename: Wei
authors.initials: W
authors.lastname: Tao
authors.forename: Xian-Zhu
authors.initials: XZ
authors.lastname: Yang
mesh_terms: D000818:Animals; D000903:Antibiotics, Antineoplastic / Q000008:administration & dosage / Q000737:chemistry; D045744:Cell Line, Tumor; D004058:Diffusion; D004317:Doxorubicin / Q000008:administration & dosage* / Q000737:chemistry; D004357:Drug Synergism; D057927:Hydrophobic and Hydrophilic Interactions; D051379:Mice; D008807:Mice, Inbred BALB C; D008819:Mice, Nude; D008823:Micelles; D053769:Nanocapsules / Q000008:administration & dosage / Q000737:chemistry* / Q000648:ultrastructure*; D009374:Neoplasms, Experimental / Q000188:drug therapy* / Q000473:pathology; D010316:Particle Size; D013499:Surface Properties; D016896:Treatment Outcome
chemical_list: D000903:Antibiotics, Antineoplastic; D008823:Micelles; D053769:Nanocapsules; D004317:Doxorubicin
keywords: cancer therapy; drug delivery; hydrophobicity; micellar core; polyphosphoester