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Modulation of Tumor-selective Vascular Blood Flow and Extravasation by the Stable Prostaglandin I 2 Analogue Beraprost Sodium.
- Source :
-
Journal of Drug Targeting . Jan2003, Vol. 11 Issue 1, p45-52. 8p. - Publication Year :
- 2003
-
Abstract
- Improved delivery of macromolecular drugs to solid tumor is known as the enhanced permeability and retention (EPR) effect of macromolecular drugs and lipids. We report here that a prostaglandin I 2 (PGI 2 ) analogue induces enhancement of tumor-selective drug delivery, while it decreases tumor blood flow, in a rat tumor model (AH136B). Beraprost sodium (BPS) is an analogue of PGI 2 that is more stable than parental PGI 2 in vivo ( t 1/2 for BPS is >1 h vs. a few seconds for PGI 2 ). Thus, BPS was administered to tumor-bearing rats to examine its effect on tumor vascular permeability as well as tumor blood flow. The amount of extravasation of the Evans blue-albumin complex in tumor tissue increased from two to three times, whereas tumor blood flow decreased almost 70%, in the group treated with BPS at 7 μg/kg compared with controls. Tissue blood flow of normal organs such as the kidney and the liver did not change to a significant extent. These findings establish a new role for BPS, not only in enhancing macromolecular drug delivery, but also in reducing the blood supply to tumor tissues. [ABSTRACT FROM AUTHOR]
- Subjects :
- *PROSTAGLANDINS
*BLOOD flow
*HEMODYNAMICS
*BLOOD circulation
*SODIUM
Subjects
Details
- Language :
- English
- ISSN :
- 1061186X
- Volume :
- 11
- Issue :
- 1
- Database :
- Academic Search Index
- Journal :
- Journal of Drug Targeting
- Publication Type :
- Academic Journal
- Accession number :
- 10724752
- Full Text :
- https://doi.org/10.1080/1061186031000086072