The effect of the antioxidant on the properties of thiolated poly(aspartic acid) polymers in aqueous ocular formulations

Mária Budai-Szűcs, Gabriella Horvát, Benjámin Gyarmati, Barnabás Áron Szilágyi, A. Szilágyi, Szilvia Berkó, Rita Ambrus, P. Szabó-Révész, Giuseppina Sandri, Maria Cristina Bonferoni, Carla Caramella, Erzsébet Csányi

Research output: Contribution to journalArticle

2 Citations (Scopus)

Abstract

Thiolated polymers are a promising new group of excipients, but their stability against atmospheric oxidation has not been investigated in detail, and only a few efforts have been made to improve their stability. The oxidation of the thiol groups in solutions of thiolated polymers may result in a decrease of mucoadhesion and unpredictable in situ gelation. The aims of our work were to study the stability of aqueous solutions of thiolated polymers and the effects of stabilizing agents. We investigated thiolated poly(aspartic acid) polymers stabilized with dithiothreitol, glutathione or acetylcysteine. The effects of these antioxidants on the gel structure, mucoadhesion and drug release were determined by means of scanning electron microscopy, swelling, rheology, adhesion and drug release tests. It was concluded that the stability of polymer solutions containing antioxidants is sufficient for one day. Polymers stabilized with dithiotreitol demonstrated fast swelling and drug release, but weaker mucoadhesion as compared with the other samples. Polymers stabilized with glutathione displayed the weakest cohesive properties, resulting in fast and uncontrolled drug release and moderate mucoadhesion. Acetylcysteine-stabilized polymers exhibited an optimum cross-linked structure, with free thiol groups ensuring polymer-mucin interactions, resulting in the best mucoadhesive properties.

Original languageEnglish
Pages (from-to)178-187
Number of pages10
JournalEuropean Journal of Pharmaceutics and Biopharmaceutics
Volume113
DOIs
Publication statusPublished - Apr 1 2017

Fingerprint

Aspartic Acid
Polymers
Antioxidants
Excipients
Acetylcysteine
Sulfhydryl Compounds
Glutathione
Rheology
Dithiothreitol
Mucins
Electron Scanning Microscopy
Gels
Drug Liberation

Keywords

  • Drug release
  • Mucoadhesion
  • Rheology
  • Stability
  • Thiolated polymer

ASJC Scopus subject areas

  • Biotechnology
  • Pharmaceutical Science

Cite this

The effect of the antioxidant on the properties of thiolated poly(aspartic acid) polymers in aqueous ocular formulations. / Budai-Szűcs, Mária; Horvát, Gabriella; Gyarmati, Benjámin; Szilágyi, Barnabás Áron; Szilágyi, A.; Berkó, Szilvia; Ambrus, Rita; Szabó-Révész, P.; Sandri, Giuseppina; Bonferoni, Maria Cristina; Caramella, Carla; Csányi, Erzsébet.

In: European Journal of Pharmaceutics and Biopharmaceutics, Vol. 113, 01.04.2017, p. 178-187.

Research output: Contribution to journalArticle

Budai-Szűcs, M, Horvát, G, Gyarmati, B, Szilágyi, BÁ, Szilágyi, A, Berkó, S, Ambrus, R, Szabó-Révész, P, Sandri, G, Bonferoni, MC, Caramella, C & Csányi, E 2017, 'The effect of the antioxidant on the properties of thiolated poly(aspartic acid) polymers in aqueous ocular formulations', European Journal of Pharmaceutics and Biopharmaceutics, vol. 113, pp. 178-187. https://doi.org/10.1016/j.ejpb.2016.12.026
Budai-Szűcs, Mária ; Horvát, Gabriella ; Gyarmati, Benjámin ; Szilágyi, Barnabás Áron ; Szilágyi, A. ; Berkó, Szilvia ; Ambrus, Rita ; Szabó-Révész, P. ; Sandri, Giuseppina ; Bonferoni, Maria Cristina ; Caramella, Carla ; Csányi, Erzsébet. / The effect of the antioxidant on the properties of thiolated poly(aspartic acid) polymers in aqueous ocular formulations. In: European Journal of Pharmaceutics and Biopharmaceutics. 2017 ; Vol. 113. pp. 178-187.
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