Exploiting EPR in polymer drug conjugate delivery for tumor targeting.
Curr Pharm Des
; 12(36): 4785-96, 2006.
Article
em En
| MEDLINE
| ID: mdl-17168778
ABSTRACT
Treatment of tumor tissue without affecting normal cells has always been formidable task for drug delivery scientists and this task is effectively executed by polymer drug conjugate (PDC) delivery. The novelty of this concept lies in the utilization of a physical mechanism called enhanced permeability and retention (EPR) for targeting tumors. EPR is a physiological phenomenon that is customary for fast growing tumor and solves the problem of targeting the miscreant tissue. PDCs offer added advantages of reduced deleterious effects of anticancer drugs and augmentation of its formulation capability (e.g. Solubility). There are now at least eleven PDCs that have entered phase I/II/III clinical trial as anticancer drugs. PDCs once entered into the tumor tissue, taking advantage of EPR, are endocytosed into the cell either by simple or receptor mediated endocytosis. Various polymeric carriers have been used with hydrolyzable linker arm for conjugation with bioactive moiety. The hydrolyzable linkages of PDC are broken down by acid hydrolyses of lysosomes and releases the drug. High concentrations of the chemotherapeutic agent are maintained near the nucleus, the target site. Passive targeting by PDCs is due to the physiological event of EPR, which is becoming one of the major thrust areas for targeting solid tumors.
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Coleções:
01-internacional
Base de dados:
MEDLINE
Assunto principal:
Polímeros
/
Permeabilidade Capilar
/
Portadores de Fármacos
/
Sistemas de Liberação de Medicamentos
/
Antineoplásicos
Limite:
Animals
/
Humans
Idioma:
En
Revista:
Curr Pharm Des
Assunto da revista:
FARMACIA
Ano de publicação:
2006
Tipo de documento:
Article
País de afiliação:
Índia