DEVELOPMENT OF CELLULOSE ACETATE PHTHALATE COATED PECTIN MICROPARTICLES LOADED WITH MESALAMINE AND SACCHAROMYCES BOULARDII INTENDED FOR SPECIFIC COLONIC DRUG DELIVERY

Abstract

The present work was focused on delivering mesalamine along with probiotic, specifically to the colonic site. Mesalamine and probiotic were encapsulated in natural polysaccharide pectin microparticles and coated with the Cellulose acetate phthalate (CAP) as an enteric-coated polymer. The major concern of this research is to protect the drug and probiotic release from the gastric environment and target to colonic region. By using nitric oxide assay, the IC50 value of both probiotics (Saccharomyces boulardii and Lactobacillus acidophilus) was determined. Pectin microparticles were prepared by dehydration technique followed by coating with oil-in-oil solvent evaporation. For the drug and polymer compatibility, FTIR determination was done. The release of drug and probiotic was determined with and without rat cecal content. Furtherly pharmacokinetic studies were done to assess the drug concentration in Wistar rat's blood fluid. The nitricoxide assay confirmed that Saccharomyces boulardii has high nitric oxide scavenging ability. The FTIR graphs confirmed that no chemical reaction was observed within the drug and polymer. The observed in-vitro results of coated microparticles release have been confirmed that the coated formulation has the potential to release the drug and probiotic at the colonic site. Further pharmacokinetic studies revealed a lower value of Cmax in the case of CAP coated microparticles formulation in comparison to uncoated ones which evidenced the lower systemic exposure of the drug.