Preparation and release characteristics of mesalazine loaded calcium pectin-silica gel beads based on callus cultures pectins for colon-targeted drug delivery

• Published in: International journal of biological macromolecules 2018-12, Vol.120 (Pt B), p.2225-2233
• Main Authors: Günter, Elena A., Markov, Pavel A., Melekhin, Anatoliy K., Belozerov, Vladislav S., Martinson, Ekaterina A., Litvinets, Sergey G., Popov, Sergey V.
• Format: Article
• Language: English
• Subjects: Araceae - chemistry; Colon - metabolism; Colon-targeted drug delivery; Drug Carriers - chemistry; Drug Liberation; Mesalamine - chemistry; Mesalamine - metabolism; Mesalazine; Pectin-silica gel; Pectins - chemistry; Silica Gel - chemistry
• ISSN: 0141-8130; 1879-0003
• DOI: 10.1016/j.ijbiomac.2018.07.078

The aim of this work is to produce calcium pectin-silica gel beads containing mesalazine as a drug model in order to control the drug release in the colon. The mesalazine loaded calcium pectin-silica gel beads were prepared using the ionotropic gelation method. Energy-dispersive X-ray analysis revealed that increasing the Na2SiO3 concentration led to an increase of the silicon content on the surface and in the cross-sections of the beads. The addition of Na2SiO3 to the gel formulations made from the duckweed callus culture pectin led to a decrease in the swelling degree that appeared to be related to the higher gel strength of these beads. The beads made from pectins of campion and duckweed callus cultures with adding of 22.2 mg/ml of Na2SiO3 showed the lowest release of mesalazine in simulated gastric and intestinal fluids. An increase in the reaction time up to 60 min during incubation in the cross-linking solution of CaCl2 led to a slower release of drug from the beads. An elevated release of mesalazine was achieved in the simulated colonic fluid. Prepared calcium pectin-silica gel beads containing mesalazine as a drug model can be proposed for controlled drug release in the colon. •The mesalazine loaded pectin-silicate gel beads were prepared using the ionotropic gelation method.•The pectin-silicate gel beads made from the duckweed callus culture pectin had the higher gel strength.•The pectin-silicate gel beads with the higher content of silicon showed the lowest release of mesalazine.•An elevated drug release from pectin-silicate gel beads was achieved in the simulated colonic media.