Paramylon and synthesis of its ionic derivatives: Applications as pharmaceutical tablet disintegrants and as colloid flocculants

Abstract

Paramylon, a high molecular weight polysaccharide, is a linear and unbranched (1 → 3)-β-d-glucan. Despite its numerous biological benefits, the poor aqueous solubility of crystalline paramylon is a drawback that has hampered some of its applications. In an effort to make this biomaterial amenable to practical uses, cationic and anionic paramylon derivatives were obtained. The degrees of substitution of both products were determined. The products were characterized by FT-IR spectrocopy, ESI mass spectrometry, ¹H, ¹³C and ¹H-¹³C NMR and SEM microscopy. These techniques confirmed the success of the substitution reactions. ¹H NMR analysis was used to develop alternative methods for an approximate estimation of the degree of substitution. ¹H-¹³C HSQC NMR spectra were assigned for both derivatives. New applications of native, cationic and anionic paramylon were found. Native paramylon showed similar performance as pharmaceutical tablet disintegrant than sodium croscarmellose. Cationic paramylon behavior as colloid flocculant was comparable with commercial cationic polyacrylamides. The anionic derivative could eventually be used in the formulation of matrix controlled release systems or as a suspending agent.

Keywords: Carboxymethylation; Cationization; Colloid flocculation; Paramylon; Pharmaceutical applications; Tablet disintegrant.