Cavallaro, Gennara published the artcileGlycosilated macromolecular conjugates of antiviral drugs with a polyaspartamide, Related Products of alcohols-buliding-blocks, the publication is Journal of Drug Targeting (2004), 12(9-10), 593-605, database is CAplus and MEDLINE.
Two new polymeric conjugates for specific liver targeting were prepared by conjugation of sugar moieties and antiviral drugs to α, β-poly[N-2-(hydroxyethyl)-dl-aspartamide] (PHEA). PHEA-galactopyranosylphenylthiocarbamide-mono-O-succinylganciclovir (conjugate 7) and PHEA-mannopyranosylphenylthiocarbamide-O-succinylacyclovir (conjugate 8) were synthesized according to a multi-step procedure which allowed for obtaining high product yield and process standardization. Conjugate 7 contained 7.5 and 8.5% of galactose and ganciclovir (substituent/repeating unit, mol/mol), resp., and conjugate 8 contained 14.2 and 10.8% of mannose and acyclovir, resp. In vitro studies demonstrated that both acyclovir and ganciclovir were released from the polymeric adducts at a release rate depending on the incubation medium. Though a detailed study evidenced that the two bioconjugates undergo different hydrolysis pathways, in both cases high drug release rate was found in plasma, while the glycosidic moiety was not released. Pharmacokinetic studies carried out by i.v. administration of the bioconjugates to Balb/c mice demonstrated that the conjugation of glycosidic moieties promoted the disappearance of the polymer from the blood stream. The two derivatives displayed a different pharmacokinetic profile. In particular, the mannosyl conjugation promoted the rapid disposition of the macromol. in the kidneys and in the liver, while prevented the accumulation in the spleen. On the contrary, the galactosyl derivative was found to dispose in the liver at the same extent of the naked polymer. Few considerations on the different behavior of the conjugates were reported.
Journal of Drug Targeting published new progress about 96345-79-8. 96345-79-8 belongs to alcohols-buliding-blocks, auxiliary class Sugar Units,Gal and Man, name is (2R,3S,4S,5S,6R)-2-(Hydroxymethyl)-6-(4-isothiocyanatophenoxy)tetrahydro-2H-pyran-3,4,5-triol, and the molecular formula is C13H15NO6S, Related Products of alcohols-buliding-blocks.
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