A Novel Method to Prepare 5-Fluorouracil, an Anti-cancer Drug, Loaded Microspheres from Poly(N-vinyl caprolactam-co-acrylamide) and Controlled Release Studies

Abstract

Poly(N-vinyl caprolactam-co-acrylamide) co-polymers cross-linked with N,N′-methylene bisacrylamide loaded with 5-fluorouracil (5-FU) have been investigated for controlled release of 5-FU, an anticancer drug. Microspheres of poly(N-vinyl caprolactam-co-acrylamide) co-polymers cross-linked with N,N′-methylene bisacrylamide have been prepared by free radical emulsion polymerization using varying amounts of acrylamide (AAm), N-vinyl caprolactam (VCL) and N,N-methylene bisacrylamide (NNMBA). Particles were produced in the size range of 16–34 μm and 5-FU was encapsulated into these microspheres. The in situ polymerization and release kinetics of drug-loaded microspheres have been investigated in phosphate buffer solution (pH 7.4) at 25 and 37°C. Scanning electron microscopy (SEM) was used to study the surface morphology of the microspheres. In vitro release data have been affected by varying the co-polymer composition, amount of cross-linking agent and amount of drug loading in the microspheres. Microspheres with different co-polymer compositions were obtained in yields up to 80–85% with encapsulation efficiencies ranging from 69 to 79%. SEM suggested a spherical nature of particles with somewhat rough surfaces. In vitro drug release data indicated that particle size and release kinetics have been influenced by co-polymer composition, amount of cross-linking agent and amount of 5-FU loaded in the microspheres.

Keywords:

• N-VINYL CAPROLACTAM
• ACRYLAMIDE
• MICROSPHERES
• 5-FLUOROURACIL
• DRUG DELIVERY