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Development of N‐(2‐hydroxypropyl)methacrylamide copolymer conjugates for delivery of cancer chemotherapy
Author(s) -
Duncan Ruth,
Ulbrich Karel
Publication year - 1993
Publication title -
makromolekulare chemie. macromolecular symposia
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.257
H-Index - 76
eISSN - 1521-3900
pISSN - 0258-0322
DOI - 10.1002/masy.19930700118
Subject(s) - methacrylamide , conjugate , chemistry , doxorubicin , drug delivery , prodrug , copolymer , cancer research , combinatorial chemistry , biochemistry , chemotherapy , polymer , medicine , organic chemistry , acrylamide , mathematical analysis , mathematics , surgery
In recent years a series of N‐(2‐hydroxypropyl)methacrylamide (HPMA) copolymers have been synthesised containing antitumour agents, particularly doxorubicin (Dox) bound to the polymer carrier by peptidyl spacers designed for cleavage by lysosomal thiol‐dependent proteases, enzymes known to show increased activity in metastatic tumours. Such conjugates display a broad range of antitumour activities against leukaemic, solid tumour and metastatic models, and recent experimentation has focussed on investigating further their mechanism of action. It is believed that drug conjugation leads to reduced toxicity, passive accumulation within solid tumours due to the enhanced permeability and retention effect and subsequent controlled drug release. All these factors contribute to the improved antitumour activity seen.