Preparation and characterization of novel derivatives of chitosan and trimethyl chitosan conjugated with dipeptides and vitamin B12 as candidates for oral delivery of insulin

作者：Omid Nersi Jafary; Babanejad Niloofar; Amini Hossein; Amini Mohsen; Tehrani Morteza Rafiee; Dorkoosh Farid^*

来源：Journal of Polymer Research, 2014, 21(8): 510.

DOI：10.1007/s10965-014-0510-8

• Chitosan
• Trimethyl chitosan
• Didpeptide
• Vitamine B12
• Oral drug delivery
• Insulin

Chitosan and its derivatives are widely used in drug delivery systems due to their bio-degradebility, bio-compatibility and absorption enhancing properties. Many peptide and protein derived therapeutics cannot be administered through oral rout because of the proteolytic condition of gastro-intestinal tract and their low bio-availability. Insulin is a peptide drug which is widely used in diabetics as repeated daily injection. Due to the fact that there are receptors for didpeptides and vitamine B12 in small intestine, in this research work novel derivatives of chitosan and trimethyl chitosan conjugated with glycyl-glycine, alanyl-alaninie and vitamine B12 were synthesized and characterized. The structure of conjugates as well as substitution of different functional groups was confirmed by different instrumental analytical methods such as Fourier transform infrared, magnetic resonance, and X-ray diffraction spectroscopy. Nano-particles of aforementioned loaded with insulin were prepared and their size, surface electrical charge and morphology characterized and their release profile were studied. The results are promising and reveal that these new chitosan and trimethyl chitosan derivatives are potential vehicles for protein and peptide drug molecules.

• 出版日期2014-7-4