Pharmaceutical research
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Pharmaceutical research · Jul 2007
Modeling methadone pharmacokinetics in rats in presence of P-glycoprotein inhibitor valspodar.
To quantify the in vivo role of P-glycoprotein (P-gp) in the pharmacokinetics of methadone after intravenous and oral administration, using valspodar as a P-gp inhibitor. ⋯ Valspodar increased methadone's bioavailability as consequence of P-gp inhibition, which resulted in an increased analgesic effect of methadone.
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Pharmaceutical research · Jul 2007
Comparative StudyProline prodrug of melphalan targeted to prolidase, a prodrug activating enzyme overexpressed in melanoma.
To determine the bioactivation and uptake of prolidase-targeted proline prodrugs of melphalan in six cancer cell lines with variable prolidase expression and to evaluate prolidase-dependence of prodrug cytotoxicity in the cell lines compared to that of the parent drug, melphalan. ⋯ The data corroborates the specificity of prophalan-L: activation by prolidase as well as prolidase-targeted cytotoxicity of prophalan-L: in cancer cell lines. Hence, prophalan-L: , a stable prodrug of melphalan, exhibits potential for efficiently targeting melanoma with reduced systemic toxicity.