title: [Preliminary study on synthesis of novel amphiphilic molecules and their application as drug vectors].
abstract: OBJECTIVE
  To synthesize three amphiphilic molecules (TEG-R1, TEG-R2, TEG-R3), with branched oligo polyethylene glycol as hydrophilic fractions and aliphatic chains (containing six, eight and twelve carbon atoms respectively) as hydrophobic fractions, and study them as insoluble drug vectors.
  
  
  METHODS
  Three compounds were successfully through acylation, substitution reaction, reduction reaction and esterification. Their structures were verified by NMR analysis; and the critical micelle concentrations (CMC) of TEG-R1, TEG-R2, TEG-R3 were determined by pyrene fluorescence probe spectrometry. Transmission electronic microscopy (TEM) photos displayed the state of the aqueous solution. The self-assembly solution evaporation method was adopted to prepare drug loading podophyllotoxin micelles, and characterize their grain size, in order to detect the hemolysis of the three amphiphilic molecules.
  
  
  RESULTS
  Nuclear magnetism showed the successful synthesis of three amphiphilic molecules, with critical micelle concentrations of TEG-R1, TEG-R2, TEG-R3 of 50, 50, 10 mg x L(1), respectively. Transmission electronic microscopy (TEM) photos displayed a spherical-like state, with diameter of 20-50 nm. All of the three amphiphilic molecules could be prepared into drug-loading micelles, with the range of grain sizes between 100-200 nm. Hemdytic experiment showed that, among the amphiphilic molecules of the graft six-carbon aliphatic chain, TEG-R1 could not cause hemolysis.
  
  
  CONCLUSIONS
  All of the three amphiphilic molecules are micellized in water solution, and can be used as insoluble drug vectors. Among them, TEG-R1 could not cause hemolysis, and is expected to become a new-type drug vector.
authors.affiliation: Institute of Medicinal Plant Development, Peking Union Medical College and Chinese Academy of Medical Science, Beijing 100193, China. zqrujing@126.com
authors.forename: Ru-Jing
authors.initials: RJ
authors.lastname: Ai
authors.forename: Xiang-Tao
authors.initials: XT
authors.lastname: Wang
authors.forename: Jing
authors.initials: J
authors.lastname: Zhao
authors.forename: Zhi-Tao
authors.initials: ZT
authors.lastname: Li
authors.forename: Yi-Fei
authors.initials: YF
authors.lastname: Guo
mesh_terms: D004337:Drug Carriers / Q000138:chemical synthesis* / Q000737:chemistry; D057927:Hydrophobic and Hydrophilic Interactions; D008823:Micelles; D046529:Microscopy, Electron, Transmission; D011108:Polymers / Q000138:chemical synthesis* / Q000737:chemistry
chemical_list: D004337:Drug Carriers; D008823:Micelles; D011108:Polymers