Polyaminated pullulan, a new biodegradable and cationic pullulan derivative for mucosal drug delivery

Area of Science:

• Polymer Chemistry
• Materials Science
• Pharmaceutics

Background:

• Pullulan is a polysaccharide with potential for drug delivery.
• Developing mucoadhesive polymers is crucial for effective mucosal administration.
• Controlling drug release profiles enhances therapeutic outcomes.

Purpose of the Study:

• To synthesize novel polycationic pullulan derivatives.
• To evaluate the mucoadhesive and drug release properties of these derivatives.
• To explore their potential as excipients for mucosal drug delivery.

Main Methods:

• Activation of pullulan hydroxyl groups using mesyl chloride.
• Conjugation of activated pullulan with low-molecular weight polyamines (tris(2-aminoethyl)amine and polyethyleneimine).
• Assessment of swelling, mucoadhesion, and drug release characteristics of the modified pullulans (Pul-TAEA and Pul-PEI).

Main Results:

• Pul-TAEA and Pul-PEI showed significant swelling at pH 6.8 (240- and 370-fold weight increase).
• These derivatives exhibited substantially increased dynamic viscosity in mucus (5- and 13.3-fold).
• Mucoadhesion studies revealed marked increases in tensile strength (6- and 37.8-fold) and adhesion time (72- and 120-fold) compared to unmodified pullulan.
• Sustained drug release was achieved due to ionic interactions between cationic pullulan derivatives and an anionic model drug.

Conclusions:

• Polyaminated pullulans (Pul-TAEA and Pul-PEI) possess excellent mucoadhesive properties.
• These novel derivatives facilitate sustained drug release.
• Polyaminated pullulans represent promising excipients for advanced mucosal drug delivery systems.