Synthesis and charactersiation of chitosan conjugate; design and evaluation of membrane moderated type transdermal drug delivery system

Abstract

The purpose of the present research investigation was to synthesis, characterisation of chitosan conjugates and its effect on drug permeation from transdermal rate controlling membrane. Chitosan conjugate was synthesised by conjugation with thioglycolic acid. The prepared chitosan conjugate was characterised by determining the charring point, Fourier transmission-infrared and differential scanning calorimetric analysis. The rate controlling membranes were prepared by various proportions of chitosan and chitosan conjugate, to moderate drug permeation through rate controlling membrane. The membrane moderated transdermal system consists of reservoir to hold the drug gel was prepared by 20% w/v ethylcellulose with a cavity in its center. An impermeable backing layer was prepared by 2% w/v ethylcellulose. Gel consists of carvedilol was prepared by sodium alginate and sodium carboxymethylcellulose in ethanol:water solvent system The rate controlling membranes prepared were evaluated by various parameters like thickness, folding endurance, swelling index, moisture content, moisture uptake, water vapor transmission rate, tensile strength test, measurement of gel strength, in vitro permeation study, ex vivo permeation study, compatibility study using differential scanning calorimetry and stability studies. All physical parameters evident that prepared membranes have good folding endurance and sufficient tensile strength. As the proportion of chitosan conjugate increases in membrane swelling index, moisture content, moisture uptake and permeability coefficient increases. The gel strength of chitosan conjugate was considerable less compared with chitosan.

Cationic Polymers in Regenerative Medicine

“…For instance, carbodiimide-mediated amide bond formation has been used to synthesize chitosan conjugates with covalently attached thiol moieties, which were meant to enhance the permeation properties of the polymer. 109 Moreover, using a similar synthetic route, chitosan-N-inulin graft copolymers with varying degrees of substitution were synthesized by Janciauskaite et al as surface conditioners. 110 Zhang et al conjugated polyhydroxy fatty acids with cationic polymers such as PEI and chitosan as novel carriers for gene delivery utilizing carbodiimide chemistry.…”