In vitro 5-fluorouracil release properties investigation from pH sensitive sodium alginate coated and uncoated methyl cellulose/chitosan microspheres

Abstract

5-Fluorouracil (5-FU) has been in clinical practice for decades one of the oldest chemotherapy agents. However, intravenous administration of 5-FU requires the development of an oral controlled delivery system for improved patient compliances. For this purpose, 5-FU loaded and sodium alginate (NaAlg) coated and uncoated methyl cellulose (MC)/chitosan (CS) microspheres were prepared by emulsion crosslinking method using a mixture of water and oil. Firstly, MC/CS microspheres were prepared and then coated with NaAlg. The prepared microspheres were characterized by optical microscopy, Fourier transform infrared spectroscopy (FTIR), and differential scanning calorimetry (DSC). Microspheres were also characterized by equilibrium swelling values and drug release profiles. The in vitro drug release studies were carried out with three pH values 1.2, 6.8, and 7.4, respectively, each for 2 h. It was determined that coating the microspheres with NaAlg provides more controlled drug release, especially at pH 1.2. The effects of the preparation conditions, such as coating time, MC/CS ratio, NaAlg concentration, and crosslinker concentration on the 5-FU release were investigated.