Pharmacokinetics and distribution of 125I-PLA-b-PEO block copolymers in rats
Language English Country Great Britain, England Media print
Document type Journal Article, Research Support, Non-U.S. Gov't
PubMed
12760566
DOI
10.1081/pdt-120018484
Knihovny.cz E-resources
- MeSH
- Chemical Phenomena MeSH
- Chemistry, Physical MeSH
- Chromatography, Gel MeSH
- Isotope Labeling MeSH
- Polylactic Acid-Polyglycolic Acid Copolymer MeSH
- Rats MeSH
- Lactic Acid chemistry MeSH
- Polyglycolic Acid chemistry MeSH
- Lactates pharmacokinetics MeSH
- Magnetic Resonance Spectroscopy MeSH
- Micelles MeSH
- Molecular Weight MeSH
- Drug Carriers pharmacokinetics MeSH
- Half-Life MeSH
- Polyethylene Glycols pharmacokinetics MeSH
- Polymers chemistry pharmacokinetics MeSH
- Rats, Wistar MeSH
- Tissue Distribution MeSH
- Inflammation metabolism MeSH
- Animals MeSH
- Check Tag
- Rats MeSH
- Male MeSH
- Animals MeSH
- Publication type
- Journal Article MeSH
- Research Support, Non-U.S. Gov't MeSH
- Names of Substances
- Polylactic Acid-Polyglycolic Acid Copolymer MeSH
- Lactic Acid MeSH
- Polyglycolic Acid MeSH
- Lactates MeSH
- Micelles MeSH
- Drug Carriers MeSH
- polyethylene oxide-polylactic acid block copolymer MeSH Browser
- Polyethylene Glycols MeSH
- Polymers MeSH
The PLA-b-PEO block copolymers were studied as potential carriers for anti-inflammatory and anticancer drugs. The copolymers were labeled with 125I, and their micelles in physiological saline were prepared by dialysis. Copolymer 1, with Mw = 12,360 (PLA/PEO = 7000/5000), formed particles of about 300 nm in diameter (Rh was 150 nm), whereas copolymer 2, with Mw = 20,470 (6000/14,000), made up micelles of about 72 nm in diameter (Rh was 35.8 nm). Their pharmacokinetic and biodistribution profiles were compared in normal rats and rats with carrageenan-induced inflammation after intravenous application of about 5 mg/kg of each copolymer. Copolymer 2, forming smaller particles, showed longer distribution and elimination half-lives. Both copolymers under study exhibited significantly higher uptake by inflammatory tissue compared with noninflammatory one. The study indicates that PLA-b-PEO copolymers, having different molecular weight of the chains, have similar biological behavior in most organs and tissues. Differences in the uptake by some organs (mainly kidney and bowels) and in activity level in blood at later time intervals were found. Significantly different clearance values are due to different ratios of hydrophobic and hydrophilic chains of the copolymers.
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