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PEG–Anticancer Drugs

  • Francesca Cateni
  • Marina Zacchigna
Chapter
Part of the Macromolecular Anticancer Therapeutics book series (CDD&D)

Abstract

The concept of polymer–anticancer conjugates was first proposed in 1975 by Ringsdorf, and the biological rationale for their design and current understanding of the mechanism of action is well known. During the past 10 years, there has been a renaissance in the field of PEG-conjugated anticancer agents. Benefits which can be achieved through application of PEGylation, i.e. the attachment of poly(ethylene glycol) to proteins and drugs, are greater solubility, longer duration of exposure, selective delivery of entrapped drug to the site of action, superior therapeutic index and the potential to overcome resistance associated with the regular anticancer agent.

In this chapter, the recent developments in the preparation and biological activity of leading anticancer agents covalently linked to linear and branched poly(ethylene glycol) of various molecular weights are reported.

Keywords

Antitumour Activity Folate Receptor Polymer Conjugate Hydrazone Bond Amino Adipic Acid 
These keywords were added by machine and not by the authors. This process is experimental and the keywords may be updated as the learning algorithm improves.

Abbreviations

Ara-C

cytosine arabinoside

BEMD

(3S)-benzoxylcarbonylethyl-morpholine-2;5-dione

BXF T 24

human bladder carcinoma

CDDP

cisplatin

CMC

N-cyclohexyl-N -(2-morpholinoethyl)carbodiimide metho-p-toluenesulfonate

CPT

camptothecin

CPT-11

irinotecan

CYP 3A4

cytochrome P450

DBM

bis(4-hydroxy)butyl maleate

DCC

N,N-dicyclohexylcarbodiimide

DDS

Drug delivery system

dFdC

gemcitabine

DHFR

dihydrofolate reductase

DLS

dynamic light scattering

DOX

doxorubicin

EDC

N-(3-dimethylaminopropyl)-N -ethylcarbodiimide

EPI

epirubicin

EPR

enhanced permeability and retention

ESEM

environmental scanning electron microscopy

FOL

folate

FR

folate receptor

FRME

folate receptor-mediated endocytosis

GF120918

P-glycoprotein blocker

GFP

green fluorescence protein

HMPA

hexamethylphosphoramide

HOBT

1-hydroxybenzotriazole

HSA

human serum albumin

KB

human nasopharyngeal carcinoma

LHRH

luteinizing hormone-releasing hormone

LLA

l-lactide

LXFL 529

human lung cancer

MACL MCF 7

human mammalian carcinoma

MDDS

micellar drug delivery system

MDR

multidrug resistant

MEXF 514

human melanoma carcinoma

mPEG

monomethoxy poly(ethylene glycol)

MTT

3-(4,5-dimethylthiazol-2yl)-2,5-diphenyltetrazoliumbromide)

MTX

methotrexate

NHS

N-hydroxysuccinimide

NLS

nuclear localization

NP

magnetic nanoparticle

PEG

poly(ethylene glycol)

P-gp

P-glycoprotein

PLA

poly(lactide)

PTX

paclitaxel

RXF 944

human renal carcinoma

SN38

7-ethyl-10-hydroxycamptothecin

Sn(Oct)2

stannous octoate

SWNH

single-wall carbon nanohorns

TEM

transmission electron microscopy

TOP1

topoisomerase I

TPT

topotecan

VS

vinyl sulfone

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Copyright information

© Springer Science+Business Media, LLC 2010

Authors and Affiliations

  • Francesca Cateni
    • 1
  • Marina Zacchigna
    • 1
  1. 1.Department of Pharmaceutical SciencesUniversity of TriesteTriesteItaly

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