Controlled Release of Oral Drugs from Cross-linked Polyvinyl Alcohol Microspheres

Abstract A new technique for the preparation of cross-linked polyvinyl alcohol (PVA) microspheres containing various drugs is described. An aqueous solution of PVA containing various concentrations of glutaraldehyde was dispersed as droplets in liquid paraffin using a suitable stabilizing agent. Cross-linking of PVA droplets with glutaraldehyde was induced by an acid catalyst (HCl) which was produced by the addition of small quantities of benzoyl chloride into the dispersion medium. Microspheres containing drugs such as aspirin, griseofulvin and nicotinic acid were prepared by carrying out the cross-linking reaction in the presence of such drugs. The drug release studies were carried out in simulated gastric and intestinal fluids without enzymes at 37°C. It was observed that increase in the cross-linking density of the microspheres reduced the drug release rate considerably, suggesting that the release profiles could be controlled by changing the cross-linking density. It was also observed that a higher rate of release was obtained from smaller beads.