In vitro dissolution of pH sensitive microparticles for colon-specific drug delivery

Abstract

Objective: The objective of this work is to prepare oral dosage systems based on enteric materials in order to verify their possible use as Colon-Specific Drug Delivery Systems (CSDDSs).

Methodology: In particular, three different copolymers of methyl-methacrylate (MMA) - acrylic acid (AA) are synthesized with increasing percentage of MMA (from 70% to 73%) and they are used to produce microparticles by the double-emulsion solvent evaporation method. The microparticles, loaded using theophylline as model drug, are then tested for drug release under varying pH to reproduce what happens in the human GI tract.

Results: All the investigated systems have shown an effective pH sensitiveness: they show a good gastro-resistance, releasing the model drug only at higher pH, small intestine or colon, depending on the kind of used copolymer.

Conclusion: The results confirm the usefulness of both the materials and the methods proposed in this study for colon-specific delivery applications.

Keywords::

• Colon delivery
• enteric materials
• double-emulsion solvent evaporation method