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

Area of Science:

• Biomaterials Science
• Polymer Chemistry
• Drug Delivery Systems

Background:

• Heparin (HP) is a crucial anticoagulant drug with poor oral bioavailability.
• Developing effective oral delivery systems for heparin remains a significant challenge in pharmaceutical research.
• Chitosan derivatives offer potential for creating advanced drug delivery matrices.

Purpose of the Study:

• To prepare and characterize a novel polysaccharide-based device for oral heparin delivery.
• To evaluate the stability and release profile of heparin from the developed system under simulated physiological conditions.
• To assess the potential of the N,N-dimethyl chitosan/heparin complex as an oral drug carrier.

Main Methods:

• Synthesis and characterization of N,N-dimethyl chitosan (DMC) using (1)H NMR spectroscopy.
• Formation of a polyelectrolyte complex (PEC) between DMC and heparin (HP) at pH 3.0.
• Confirmation of PEC formation via FTIR, TGA/DTG, and WAXS.
• In vitro release studies of HP from PEC in simulated gastric fluid (SGF) and simulated intestinal fluid (SIF).

Main Results:

• Successful preparation and confirmation of the DMC/HP polyelectrolyte complex.
• The PEC effectively protected heparin from degradation in simulated gastric fluid (SGF).
• Approximately 80% of loaded heparin was released from the PEC in simulated intestinal fluid (SIF).

Conclusions:

• The N,N-dimethyl chitosan/heparin (DMC/HP) polyelectrolyte complex shows significant potential as an oral drug carrier for heparin.
• The system demonstrates protective capabilities in the gastric environment and controlled release in the intestinal environment.
• Improved biological activity of heparin at physiological pH suggests suitability for oral administration.