Data from: Influence of acetylation levels on dual-modified corn starch in colon-targeted Budesonide tablet formulation

Although starch is an affordable and safe biodegradable polymer, its rapid
breakdown in the upper gastrointestinal tract renders it an unsuitable
excipient for colon-targeted oral tablets. The current study examined the
influence of varying degrees of acetylation on dual-modified (retrograded
and acetylated) corn starch as a polymer in the formulation of
colon-targeted tablets, emphasizing drug release and suitability for
direct compression, utilizing Budesonide as a model drug. Starch
acetylation was performed using acetic anhydride as the acetylating agent
and water or acetic acid as the solvent to prepare starch with low,
medium, and high degrees of substitution. Analysis techniques confirmed
the presence of acetyl groups, revealed changes in crystalline structure,
and illustrated morphological alterations post-acetylation. Among the
various degrees of substitution (DS) studied, it was evident that starch
acetylated to a high degree offered the most promising attributes as an
excipient for colon-targeted drug delivery. Specifically, tablet
formulation with a high DS of 2.01±0.03 (F4) demonstrated optimal
mechanical strength, hardness, and desirable physical properties for
achieving controlled drug release in the colon. Dissolution studies
indicated F4's effectiveness, releasing 15.24% of the drug in pH 1.2
within 2 hours, followed by 37.58% and 22.53% in pH 7.4 and pH 6.8
phosphate buffers, covering the ileo-colonic region. In conclusion, the
study emphasized the significance of the degree of substitution (DS) in
acetylation for dual-modified starch in colon-targeted tablet
formulations, highlighting its potential as an ideal option for drug
delivery applications by achieving controlled drug release in the targeted
ileo-colonic region.