Issue 47, 2011

Design of a magnesium-pridinolum complex for polylactide–drug conjugates formation

Abstract

Polylactide conjugates of the muscle contraction agent Pridinolum (PriOH = 1,1-diphenyl-3-(1-piperidinyl)-1-propanol) were prepared directly by ring-opening polymerization of L-lactide (L-LA) mediated by the pridinolummagnesium complex [Mg(μ,η2-OPri)(η1-OPri)]2. The ancillary O,N - bifunctional drug as a ligand stabilizes the magnesium species and initiates L-LA polymerization affording a polymer chain terminated by covalently attached drug molecules to the PLLA through ester linkers to form PriO–PLLA conjugate. Up to 80% of the pridinolum can be released from the conjugate by treatment with deuterated hydrochloric acid DCl at pH = 1.5 for 10 h at 37 °C.

Graphical abstract: Design of a magnesium-pridinolum complex for polylactide–drug conjugates formation

Supplementary files

Article information

Article type
Communication
Submitted
17 Aug 2011
Accepted
07 Oct 2011
First published
03 Nov 2011

Dalton Trans., 2011,40, 12660-12662

Design of a magnesium-pridinolum complex for polylactide–drug conjugates formation

T. Han, J. Utko, L. B. Jerzykiewicz and P. Sobota, Dalton Trans., 2011, 40, 12660 DOI: 10.1039/C1DT11545F

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