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Proceedings Paper

Protease-mediated drug delivery
Author(s): Eva F. Dickson; Rebecca L. Goyan; James C. Kennedy; M. Mackay; M.A.K. Mendes; Roy H. Pottier
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Paper Abstract

Drugs used in disease treatment can cause damage to both malignant and normal tissue. This toxicity limits the maximum therapeutic dose. Drug targeting is of high interest to increase the therapeutic efficacy of the drug without increasing systemic toxicity. Certain tissue abnormalities, disease processes, cancers, and infections are characterized by high levels of activity of specific extracellular and/or intracellular proteases. Abnormally high activity levels of specific proteases are present at sites of physical or chemical trauma, blood clots, malignant tumors, rheumatoid arthritis, inflammatory bowel disease, gingival disease, glomerulonerphritis, and acute pancreatitis. Abnormal protease activity is suspected in development of liver thrombosis, pulmonary emphysema, atherosclerosis, and muscular dystrophy. Inactiviating disease-associated proteases by the administration of appropriate protease inhibitors has had limited success. Instead, one could use such proteases to target drugs to treat the condition. Protease mediated drug delivery offers such a possibility. Solubilizing groups are attached to insoluble drugs via a polypeptide chain which is specifically cleavable by certian proteases. When the solubilized drug enounters the protease, the solubilizing moieties are cleaved, and the drug precipitates at the disease location. Thus, a smaller systemic dosage could result in a therapeutic drug concentration at the treatment site with less systemic toxicity.

Paper Details

Date Published: 15 December 2003
PDF: 3 pages
Proc. SPIE 5260, Applications of Photonic Technology 6, (15 December 2003); doi: 10.1117/12.543446
Show Author Affiliations
Eva F. Dickson, Royal Military College of Canada (Canada)
Rebecca L. Goyan, Royal Military College of Canada (Canada)
James C. Kennedy, Queens Univ. (Canada)
M. Mackay, Royal Military College of Canada (Canada)
M.A.K. Mendes, Royal Military College of Canada (Canada)
Roy H. Pottier, Royal Military College of Canada (Canada)


Published in SPIE Proceedings Vol. 5260:
Applications of Photonic Technology 6
Roger A. Lessard; George A. Lampropoulos, Editor(s)

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