N,N-Dimethyl chitosan/heparin polyelectrolyte complex vehicle for efficient heparin delivery

Polysaccharide-based device for oral delivery of heparin (HP) was successfully prepared. Previously synthesized N,N-dimethyl chitosan (DMC) (86% dimethylated by 1H NMR spectroscopy) was complexed with HP by mixing HP and DMC aqueous solutions (both at pH 3.0). The polyelectrolyte complex (PEC) obten...

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Bibliographic Details
Published in:International journal of biological macromolecules 2015-04, Vol.75, p.186-191
Main Authors: Bueno, Pedro V.A., Souza, Paulo R., Follmann, Heveline D.M., Pereira, Antonio G.B., Martins, Alessandro F., Rubira, Adley F., Muniz, Edvani C.
Format: Article
Language:English
Subjects:
Body Fluids - chemistry
Chitosan - analogs & derivatives
Chitosan - chemical synthesis
Chitosan - chemistry
Drug Carriers - chemistry
Drug Delivery Systems
Electrolytes - chemistry
Heparin
Heparin - chemistry
Heparin - pharmacology
Models, Theoretical
N,N-Dimethyl chitosan
Polyelectrolyte complex
Proton Magnetic Resonance Spectroscopy
Spectroscopy, Fourier Transform Infrared
Thermogravimetry
X-Ray Diffraction
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Summary:Polysaccharide-based device for oral delivery of heparin (HP) was successfully prepared. Previously synthesized N,N-dimethyl chitosan (DMC) (86% dimethylated by 1H NMR spectroscopy) was complexed with HP by mixing HP and DMC aqueous solutions (both at pH 3.0). The polyelectrolyte complex (PEC) obtention was confirmed by infrared spectroscopy (FTIR), thermogravimetric analysis (TGA/DTG) and wide-angle X-ray scattering (WAXS). In vitro controlled release assays of HP from PEC were investigated in the simulated intestinal fluid (SIF) and simulated gastric fluid (SGF). The PEC efficiently protected the HP in SGF condition in which HP is degraded. On the other hand, in SIF PEC promoted the releasing of 80±1.5% of loaded HP. The promissory results indicated that the PEC based on DMC/HP presented potential as drug-carrier matrix, since biological activity of HP was improved at pH close to physiological condition.
ISSN:0141-8130
1879-0003
DOI:10.1016/j.ijbiomac.2015.01.030