title: Porphyrin and galactosyl conjugated micelles for targeting photodynamic therapy.
abstract: OBJECTIVE
  To study the targeting and photodynamic therapy efficiency of porphyrin and galactosyl conjugated micelles based on amphiphilic copolymer galactosyl and mono-aminoporphyrin (APP) incoporated poly(2-aminoethyl methacrylate)-polycaprolactone (Gal-APP-PAEMA-PCL).
  
  
  METHODS
  Poly(2-aminoethyl methacrylate)-polycaprolactone (PAEMA-PCL) was synthesized by the combination of ring opening polymerization and reversible addition-fragmentation chain transfer (RAFT) polymerization, and then Gal-APP-PAEMA-PCL was obtained after conjugation of lactobionic acid and 5-(4-aminophenyl)-10,15,20-triphenylporphyrin (APP) to PAEMA-PCL. The chemical structures of the copolymers were characterized, and their biological properties were evaluated in human laryngeal carcinoma (HEp2) and human hepatocellular liver carcinoma (HepG2) cells.
  
  
  RESULTS
  Both APP-PAEMA-PCL and Gal-APP-PAEMA-PCL did not exhibit dark cytotoxicity to HEp2 cells and HepG2 cells. However, Gal-APP-PAEMA-PCL was taken up selectively by HepG2 cells and had the higher phototoxicity effect. Both polymers preferentially localized within cellular vesicles that correlated to the lysosomes.
  
  
  CONCLUSIONS
  The results indicated that porphyrin and galactosyl conjugated polymer micelles exhibited higher targeting and photodynamic therapy efficacy in HepG2 cells than in HEp2 cells.
authors.affiliation: Key Laboratory of Biomedical Polymers of Ministry of Education, Department of Chemistry, Wuhan University, Wuhan, 430072, China.
authors.forename: De-Qun
authors.initials: DQ
authors.lastname: Wu
authors.forename: Ze-Yong
authors.initials: ZY
authors.lastname: Li
authors.forename: Cao
authors.initials: C
authors.lastname: Li
authors.forename: Jian-Jun
authors.initials: JJ
authors.lastname: Fan
authors.forename: Bo
authors.initials: B
authors.lastname: Lu
authors.forename: Cong
authors.initials: C
authors.lastname: Chang
authors.forename: Si-Xue
authors.initials: SX
authors.lastname: Cheng
authors.forename: Xian-Zheng
authors.initials: XZ
authors.lastname: Zhang
authors.forename: Ren-Xi
authors.initials: RX
authors.lastname: Zhuo
mesh_terms: D037263:Asialoglycoprotein Receptor / Q000378:metabolism; D045744:Cell Line, Tumor; D002470:Cell Survival / Q000187:drug effects; D004337:Drug Carriers / Q000138:chemical synthesis*; D004339:Drug Compounding / Q000379:methods; D016503:Drug Delivery Systems / Q000379:methods*; D004354:Drug Screening Assays, Antitumor; D005690:Galactose / Q000737:chemistry* / Q000493:pharmacokinetics / Q000494:pharmacology; D056945:Hep G2 Cells; D006801:Humans; D008823:Micelles; D008954:Models, Biological; D010316:Particle Size; D010778:Photochemotherapy / Q000379:methods*; D011091:Polyesters / Q000737:chemistry; D011108:Polymers / Q000138:chemical synthesis*; D011166:Porphyrins / Q000138:chemical synthesis* / Q000493:pharmacokinetics / Q000494:pharmacology
chemical_list: D037263:Asialoglycoprotein Receptor; D004337:Drug Carriers; D008823:Micelles; D011091:Polyesters; D011108:Polymers; D011166:Porphyrins; C016240:polycaprolactone; D005690:Galactose