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KMID : 1137820070280040484
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의공학회지
2007 Volume.28 No. 4 p.484 ~ p.493
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Synthesis and Drug-Releasing Behavior of Various Polymeric Prodrugs of PGE1 with PEG and Its Derivative as Polymer Carriers
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Lee Chan-Woo
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Abstract
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Two polymeric prodrugs of PGE1 (prodrugs IVg and PNg) were newly synthesized. The drug conjugation proceeded in quantitative yield without decomposition of PGE1 to PGA1. With two types conjugates, PEG-PGE1 and PN-PGE1 with different spacer groups, we first discovered a possibility of slow release of PGE1 in blood circulatory system. PGE1 is conjugated with PEG and PN through the long alkylene spacers, and their availability as polymeric prodrugs is evaluated. Their drug-releasing behavior was examined both in phosphate buffer (pH=7.4) and rat plasma. Each prodrug was known to be highly stabile in the buffer solution. The drug-releasing rate became much faster in rat plasma than in the buffer solution due to the acceleration by the plasma enzymes. The drug-release was found to reach a plateau in rat plasma because the released PGE1 or its derivatives may be captured or decomposed by the plasma proteins. The slower drug-releasing rate of pro drug PNg in rat plasma is reasonably attributed to the molecular aggregation due to the hydrophobic bonding between the PGE1 moieties and spacers
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KEYWORD
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decomposition, blood circulatory system, drug-releasing, prostaglandin E1, prodrug, hydrophobic
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