Prodrugs for improving tumor targetability and efficiency.

Abstract:

:As the mainstay in the treatment of various cancers for several decades, chemotherapy is successful but still faces challenges including non-selectivity and high toxicity. Improving the selectivity is therefore a critical step to improve the therapeutic efficacy of chemotherapy. Prodrug is one of the most promising approaches to increase the selectivity and efficacy of a chemotherapy drug. The classical prodrug approach is to improve the pharmaceutical properties (solubility, stability, permeability, irritation, distribution, etc.) via a simple chemical modification. This review will focus on various targeted prodrug designs that have been developed to increase the selectivity of chemotherapy drugs. Various tumor-targeting ligands, transporter-associated ligands, and polymers can be incorporated in a prodrug to enhance the tumor uptake. Prodrugs can also be activated by enzymes that are specifically expressed at a higher level in tumors, leading to a selective anti-tumor effect. This can be achieved by conjugating the enzyme to a tumor-specific antibody, or delivering a vector expressing the enzyme into tumor cells.

journal_name

Adv Drug Deliv Rev

authors

Mahato R,Tai W,Cheng K

doi

10.1016/j.addr.2011.02.002

subject

Has Abstract

pub_date

2011-07-18 00:00:00

pages

659-70

issue

8

eissn

0169-409X

issn

1872-8294

pii

S0169-409X(11)00018-4

journal_volume

63

pub_type

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