PMID- 24328043
OWN - NLM
STAT- MEDLINE
DCOM- 20140902
LR  - 20181203
IS  - 1526-4602 (Electronic)
IS  - 1525-7797 (Linking)
VI  - 15
IP  - 1
DP  - 2014 Jan 13
TI  - Different insight into amphiphilic PEG-PLA copolymers: influence of 
      macromolecular architecture on the micelle formation and cellular uptake.
PG  - 403-15
LID - 10.1021/bm401812r [doi]
AB  - One constrain in the use of micellar carriers as drug delivery systems (DDSs) is 
      their low stability in aqueous solution. In this study "tree-shaped" copolymers 
      of general formula mPEG-(PLA)n (n = 1, 2 or 4; mPEG = poly(ethylene glycol) 
      monomethylether 2K or 5K Da; PLA = atactic or isotactic poly(lactide)) were 
      synthesized to evaluate the architecture and chemical composition effect on the 
      micelles formation and stability. Copolymers with mPEG/PLA ratio of about 1:1 
      wt/wt were obtained using a "core-first" synthetic route. Dynamic Light 
      Scattering (DLS), Field Emission Scanning Electron Microscopy (FESEM), and Zeta 
      Potential measurements showed that mPEG2K-(PD,LLA)2 copolymer, characterized by 
      mPEG chain of 2000 Da and two blocks of atactic PLA, was able to form 
      monodisperse and stable micelles. To analyze the interaction among micelles and 
      tumor cells, FITC conjugated mPEG-(PLA)n were synthesized. The derived micelles 
      were tested on two, histological different, tumor cell lines: HEK293t and HeLa 
      cells. Fluorescence Activated Cells Sorter (FACS) analysis showed that the FITC 
      conjugated mPEG2K-(PD,LLA)2 copolymer stain tumor cells with high efficiency. Our 
      data demonstrate that both PEG size and PLA structure control the biological 
      interaction between the micelles and biological systems. Moreover, using confocal 
      microscopy analysis, the staining of tumor cells obtained after incubation with 
      mPEG2K-(PD,LLA)2 was shown to be localized inside the tumor cells. Indeed, the 
      mPEG2K-(PD,LLA)2 paclitaxel-loaded micelles mediate a potent antitumor 
      cytotoxicity effect.
FAU - Garofalo, Cinzia
AU  - Garofalo C
AD  - Dipartimento di Medicina Sperimentale e Clinica, Universita degli Studi "Magna 
      Graecia" di Catanzaro , viale Europa, Catanzaro 88100, Italy.
FAU - Capuano, Giovanna
AU  - Capuano G
FAU - Sottile, Rosa
AU  - Sottile R
FAU - Tallerico, Rossana
AU  - Tallerico R
FAU - Adami, Renata
AU  - Adami R
FAU - Reverchon, Ernesto
AU  - Reverchon E
FAU - Carbone, Ennio
AU  - Carbone E
FAU - Izzo, Lorella
AU  - Izzo L
FAU - Pappalardo, Daniela
AU  - Pappalardo D
LA  - eng
PT  - Journal Article
PT  - Research Support, Non-U.S. Gov't
DEP - 20131223
PL  - United States
TA  - Biomacromolecules
JT  - Biomacromolecules
JID - 100892849
RN  - 0 (Macromolecular Substances)
RN  - 0 (Micelles)
RN  - 0 (Surface-Active Agents)
RN  - 0 (monomethoxypolyethyleneglycol-polylactide block copolymer)
RN  - 3WJQ0SDW1A (Polyethylene Glycols)
SB  - IM
MH  - *Cell Membrane/metabolism
MH  - HEK293 Cells
MH  - HeLa Cells
MH  - Humans
MH  - Macromolecular Substances/*chemistry/metabolism
MH  - *Micelles
MH  - Polyethylene Glycols/*chemistry/metabolism
MH  - Surface-Active Agents/*chemistry/metabolism
EDAT- 2013/12/18 06:00
MHDA- 2014/09/03 06:00
CRDT- 2013/12/17 06:00
PHST- 2013/12/17 06:00 [entrez]
PHST- 2013/12/18 06:00 [pubmed]
PHST- 2014/09/03 06:00 [medline]
AID - 10.1021/bm401812r [doi]
PST - ppublish
SO  - Biomacromolecules. 2014 Jan 13;15(1):403-15. doi: 10.1021/bm401812r. Epub 2013 
      Dec 23.