Development of Albumin Coated Nanoparticulate Capecitabine Suppositories

Abstract

Background: Capecitabine (CAP), a BCS class-I drug which is used for the treatment of Colorectal Cancer (CRC). Site specific and enzyme activated drug delivery was achieved by albumin coated nanoparticles. Co-administration of Proton Pump Inhibitors (PPI) with the tablet dosage form of CAP lowers the dissolution of the CAP due to elevated gastric pH, resulting in decreased CAP absorption. To overcome this absorption, issue the albumin coated CAP NPs were administered through rectal route as suppositories dosage form.Materials and Methods: The capecitabine nanoparticles were prepared using different concentrations of Poly Lactic-co-Glycolic Acid (PLGA) polymer by salting-out technique and were characterized. Further, the optimized polymeric nanoparticles were coated with Egg Albumin (EA) using a glutaraldehyde cross-linker and characterized for their particle size, zeta potential, polydispersity index, drug content, SEM, and in vitro drug release. The suppositories were prepared by fusion moulding method using different grades of PEG as a base and evaluated for various parameters and in vitro drug release.Results and Discussion: The particle size of the optimized CAP NPs and the EA coated CAP NPs were determined to be 171.7 nm and 239.6 nm respectively. The in vitro release of CAP from the EA coated NPs and the suppository formulation shows 88.3% and 81.0% respectively.Conclusion: Capecitabine suppositories were formulated and the quality control parameters were assessed for the site specific and enzyme activated drug delivery in the management of colorectal cancer with help of literature references.

Keywords: Colorectal cancer; PPI; PLGA; Glutaraldehyde; Egg albumin; Enzyme activated