Behaviour of macromolecular drug carrier poly(N-vinyl pyrrolidone-co- maleic acid) and its bioconjugates at different pH values investigated by gel permeation chromatography

E. Gyöffy, J. Pató, A. Horváth, J. Érchegyi, I. Teplán, Gy Kéri, M. Idei

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Abstract

Anionic poly(N-vinyl pyrrolidone-co-maleic acid) [referred later in the text as P], which is utilized in Drug Delivery Systems as macromolecular carrier of drugs was analysed by gel permeation chromatography. Anilide and quinoxaline derivatives were coupled to this drug-carrier to form conjugates, which were also analysed with gel permeation chromatography. Conjugate P-D1 was prepared by coupling the anilide derivative D1 [2-cyano 3-hydroxy 5- amino 2 pentenoyc (4-trifluoromethyl anilide)] to the carboxyl groups of the drug-carrier P, while conjugate P-D2 was prepared by coupling the quinoxaline derivative D2 [(6',7' dimethyl-l'-quinoxalinyl) 4-(2'amino) acetanilide] to the carboxyl groups of the drug-carrier P. Gel-chromatographic properties of the carrier P and its conjugates have been investigated on Biosil TSK 125 SW column in 0.25 N triethyl ammonium phosphate buffer of different pH values (2.25; 4.70 and 6.0). Applying appropriate pH (4.70) the method allowed us to differentiate between conjugate molecules carrying strong or weak residual carboxyl groups. Strong molecular dispersity resulting in wide, tailed chromatographic profiles could be detected in the case of the conjugates. Various distributions of the residual charges along the polymer chains, as well as presence of residual carboxyl groups of different acidity could be responsible for this molecular dispersity.

Original languageEnglish
Pages (from-to)2341-2353
Number of pages13
JournalJournal of Liquid Chromatography and Related Technologies
Volume21
Issue number15
DOIs
Publication statusPublished - Jan 1 1998

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ASJC Scopus subject areas

  • Analytical Chemistry
  • Biochemistry
  • Pharmaceutical Science
  • Clinical Biochemistry

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