Development of a novel method for the preparation of submicron particles based on thiolated chitosan

European Journal of Pharmaceutics and Biopharmaceutics : Official Journal of Arbeitsgemeinschaft Für Pharmazeutische Verfahrenstechnik E.V
Andreas Bernkop-SchnürchAlexander Greimel

Abstract

It was the aim of this study to develop a simple method for the production of thiolated chitosan particles without being ionically crosslinked. In the first step, thiolated chitosan was ionically gelated with tripolyphosphate (TPP) and sulphate in aqueous solution forming submicron particles and microparticles, respectively. In the next step, thiol groups in and on the particles were partially oxidized forming stabilizing inter- and intramolecular disulfide bonds. As the degree of oxidation can be controlled during the production process, the share of thiol and disulfide groups can be adjusted on demand. Thereafter the polyanions were removed. Utilizing this novel preparation method stable particles of a mean size of 366 +/- 30 nm and a zeta potential of around + 11.3 +/- 1.3 mV can be produced using TPP as ionic crosslinker. On average 83% of all thiol groups were oxidized. In contrast, particles did not remain stable after removing sulphate as temporary auxiliary ionic crosslinker. Neither ionically nor covalently crosslinked particles were degraded by lysozyme under physiological conditions. Utilizing the novel method described here allows a simple production of thiolated chitosan particles without losing the cationic charge...Continue Reading

References

Jan 5, 2002·Journal of Controlled Release : Official Journal of the Controlled Release Society·A VilaM J Alonso
Oct 8, 2003·Current Pharmaceutical Biotechnology·Yoshinori KatoYoshiharu Machida
Dec 20, 2003·Journal of Controlled Release : Official Journal of the Controlled Release Society·Andreas Bernkop-SchnürchYvonne Pinter
Oct 20, 2004·Journal of Controlled Release : Official Journal of the Controlled Release Society·Verena M LeitnerAndreas Bernkop-Schnürch

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Citations

Aug 25, 2007·Nanomedicine·Karin Albrecht, Andreas Bernkop-Schnürch
Apr 7, 2010·Journal of Microencapsulation·Herbert HoyerAndreas Bernkop-Schnürch
Dec 22, 2009·Journal of Drug Targeting·Zeynep Ay SenyigitAndreas Bernkop-Schnürch
Jul 31, 2009·Drug Development and Industrial Pharmacy·Herbert HoyerAndreas Bernkop-Schnürch
Jun 19, 2012·Expert Opinion on Drug Delivery·Sabine Hauptstein, Andreas Bernkop-Schnürch
May 2, 2009·Journal of Pharmaceutical Sciences·Anchalee JintapattanakitThomas Kissel
Jul 6, 2011·International Journal of Pharmaceutics·Jan BarthelmesAndreas Bernkop-Schnürch
Feb 3, 2009·Nanomedicine : Nanotechnology, Biology, and Medicine·Firooze Aghaei MoghaddamRassoul Dinarvand
Feb 21, 2008·The Journal of Pharmacy and Pharmacology·Martin Werle, Andreas Bernkop-Schnürch
Nov 14, 2021·Advanced Science·Nathalie HockAndreas Bernkop-Schnürch

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