Syntheses, chemical and enzymatic stability of new poly(ethylene glycol)–acyclovir prodrugs

Two known antiherpetic agents, acyclovir and valaciclovir, were coupled with activated poly(ethylene glycol). In vitro drug release studies demonstrated the conjugates to be stable in buffer solutions at pH 7.4 and 5.5, while only PEG–valacyclovir 2 was stable in a buffer solution at pH 1.2. The abi...

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Veröffentlicht in:Farmaco (Società chimica italiana : 1989) 2002-03, Vol.57 (3), p.207-214
Hauptverfasser: Zacchigna, M., Di Luca, G., Maurich, V., Boccù, E.
Format: Artikel
Sprache:eng
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Zusammenfassung:Two known antiherpetic agents, acyclovir and valaciclovir, were coupled with activated poly(ethylene glycol). In vitro drug release studies demonstrated the conjugates to be stable in buffer solutions at pH 7.4 and 5.5, while only PEG–valacyclovir 2 was stable in a buffer solution at pH 1.2. The ability of the macromolecular conjugate to release the free drug was also evaluated in plasma, in which the most stable prodrug also proved to be PEG–valacyclovir 2. The derivatives are degraded in the presence of proteolytic enzyme. The rate of hydrolysis was monitored by HPLC-analysis.
ISSN:0014-827X
1879-0569
DOI:10.1016/S0014-827X(01)01193-4