title: Polymeric micelles with small lipophilic moieties for drug delivery.
abstract: The aim of this study was to develop a new polymeric micelle delivery system for antitumor drugs. An amphiphile of methoxypoly(ethylene glycol)-histidine-di(cinnamic acid) (PEGHC) with a small lipophilic moiety instead of a hydrophobic biodegradable polymer chain was synthesized and characterized. The PEGHC self-assembled into micelles. The critical micelle concentration (CMC) was tested. 9-Nitro-20(s)-camptothecin (9-NC) was used as a model drug for encapsulation. The size and morphology of both blank and 9-NC loaded micelles were characterized by dynamic light scattering (DLS) and transmission electron microscopy (TEM). The release profile of 9-NC loaded micelles was studied. HepG2 liver cancer cells were incubated with the drug-loaded micelles to investigate the in vitro anticancer efficiency. The results showed that the 9-NC loaded micelles exhibited high accumulated release rate (>85%) and efficient in vitro anticancer activity.
authors.affiliation: National Engineering Research Center for Biomaterials, Sichuan University, Chengdu 610064, China.
authors.forename: Dong
authors.initials: D
authors.lastname: Li
authors.affiliation: National Engineering Research Center for Biomaterials, Sichuan University, Chengdu 610064, China.
authors.forename: Yan
authors.initials: Y
authors.lastname: Liang
authors.affiliation: National Engineering Research Center for Biomaterials, Sichuan University, Chengdu 610064, China.
authors.forename: Yusi
authors.initials: Y
authors.lastname: Lai
authors.affiliation: National Engineering Research Center for Biomaterials, Sichuan University, Chengdu 610064, China.
authors.forename: Gang
authors.initials: G
authors.lastname: Wang
authors.affiliation: National Engineering Research Center for Biomaterials, Sichuan University, Chengdu 610064, China. Electronic address: bhe@scu.edu.cn.
authors.forename: Bin
authors.initials: B
authors.lastname: He
authors.affiliation: National Engineering Research Center for Biomaterials, Sichuan University, Chengdu 610064, China. Electronic address: zwgu@scu.edu.cn.
authors.forename: Zhongwei
authors.initials: Z
authors.lastname: Gu
mesh_terms: D000970:Antineoplastic Agents / Q000737:chemistry / Q000494:pharmacology*; D002166:Camptothecin / Q000031:analogs & derivatives* / Q000737:chemistry / Q000494:pharmacology; D049109:Cell Proliferation / Q000187:drug effects; D002470:Cell Survival / Q000187:drug effects; D004305:Dose-Response Relationship, Drug; D016503:Drug Delivery Systems; D004354:Drug Screening Assays, Antitumor; D056945:Hep G2 Cells; D006801:Humans; D057927:Hydrophobic and Hydrophilic Interactions; D008823:Micelles; D015394:Molecular Structure; D011108:Polymers / Q000138:chemical synthesis / Q000737:chemistry*; D013329:Structure-Activity Relationship
chemical_list: D000970:Antineoplastic Agents; D008823:Micelles; D011108:Polymers; C079905:rubitecan; D002166:Camptothecin
keywords: 9-nitro-20(s)-camptothecin; Cellular uptake; Cytotoxicity; Drug delivery; Micelle